Literature for peptidase S01.247: epitheliasin

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Literature Substrates Inhibitors

(Topics flags: M Mutation, T Target, R Splicing, K Knockout, I Inhibitor, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)

2026

Banas,V., Seehra,K., Mahoney,M., Alisio,C., Kyriukha,Y., Weiland,E., Fath,M., Han,Z., Bricker,T., Tartell,M., Whelan,S., Boon,A.C.M. and Janetka,J.W.
Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N1
Eur J Med Chem (2026) 302, 118385-118385. PubMed Europe PubMed DOI

2025

Akagi,M., Ohta,K., Sakuma,M., Naruse,T., Ishida,Y., Niwata,C., Yamakado,N., Nakagawa,T., Ono,S., Nishi,H., Shigeishi,H. and Aikawa,T.
TMPRSS2 expression in oral mucosal cells induced by transfected double-stranded RNA and IL-1beta
J Oral Biosci (2025) , 100619-100619. PubMed Europe PubMed DOI
Baby,K., Vithalkar,M.P., Dastidar,S.G., Mukhopadhyay,C., Hamdy,R., Soliman,S.S.M. and Nayak,Y.
Exploring TMPRSS2 Drug Target to Combat Influenza and Coronavirus Infection
Scientifica (Cairo) (2025) 2025, 3687892-3687892. PubMed Europe PubMed DOI PMC EPMC V
Bach,M.L. and Jensen,B.L.
Effects and regulation of ACE2 and TMPRSS2 abundance in healthy humans and in patients with SARS-CoV-2
Biochem Soc Trans (2025) PubMed Europe PubMed DOI
Barros de Lima,G., Nencioni,E., Thimoteo,F., Perea,C., Pinto,R.F.A. and Sasaki,S.D.
TMPRSS2 as a Key Player in Viral Pathogenesis: Influenza and Coronaviruses
Biomolecules (2025) 15 PubMed Europe PubMed DOI PMC EPMC V
Elez,K., Hempel,T., Shrimp,J.H., Moor,N., Raich,L., Rocha,C., Winter,R., Le,T., Pohlmann,S., Hoffmann,M., Hall,M.D. and Noe,F.
Simulations and active learning enable efficient identification of an experimentally-validated broad coronavirus inhibitor
Nat Commun (2025) 16, 6949-6949. PubMed Europe PubMed DOI PMC EPMC I
Gabaev,I., Rowland,A., Jovanovic,E., Gawden-Bone,C.M., Crozier,T.W.M., Teixeira-Silva,A., Greenwood,E.J.D., Gerber,P.P., Wit,N., Nathan,J.A., Matheson,N.J. and Lehner,P.J.
CRISPR-Cas9 genetic screens reveal regulation of TMPRSS2 by the Elongin BC-VHL complex
Sci Rep (2025) 15, 11907-11907. PubMed Europe PubMed DOI PMC EPMC
Jung,J., Sung,J.S., Kwon,S., Bae,H.E., Kang,M.J., Jose,J., Lee,M. and Pyun,J.C.
Transmembrane protease serine 2 (TMPRSS2) inhibitors screened from an Fv-antibody library for preventing SARS-CoV-2 infection
RSC Med Chem (2025) PubMed Europe PubMed DOI PMC EPMC
Koyou,H.L., Salleh,M.N., Jelemie,C.S., Badrin,M.J.Q., Prastiyanto,M.E. and Ramachandran,V.
TMPRSS2: A Key Host Factor in SARS-CoV-2 Infection and Potential Therapeutic Target
Medeni Med J (2025) 26, 101-109. PubMed Europe PubMed DOI PMC EPMC K
Lusvarghi,S., Vassell,R., Williams,B., Baha,H., Neerukonda,S.N. and Weiss,C.D.
Capture of fusion-intermediate conformations of SARS-CoV-2 spike requires receptor binding and cleavage at either the S1/S2 or S2' site
PLoS Pathog (2025) 21, e1012808-e1012808. PubMed Europe PubMed DOI
Milewska,A., Konkel,R., Hoffmann,M., Pohlmann,S., Szczepanski,A., Frohlich,T., Popowicz,G., Overlinge,D., Mazur-Marzec,H. and Pyrc,K.
Spumigins produced by Nodularia spumigena are natural serine protease inhibitors with anti-SARS-CoV-2 activity
Virology (2025) 615, 110763-110763. PubMed Europe PubMed DOI I
Rocha,C., Arora,P., Zhang,L., Sidarovich,A., Graichen,L., Moldenhauer,A.S., Pohlmann,S. and Hoffmann,M.
Amino acid residues 655 and 969 in the spike protein of Omicron subvariant BA.1 control use of TMPRSS2 versus Cathepsin L dependent entry pathways and cell tropism
PLoS ONE (2025) 20, e0328879-e0328879. PubMed Europe PubMed DOI PMC EPMC
Tang,X., Lu,L., Li,X. and Huang,P.
Bridging Cancer and COVID-19: The Complex Interplay of ACE2 and TMPRSS2
Cancer Med (2025) 14, e70829-e70829. PubMed Europe PubMed DOI PMC EPMC V
Vegh,B., Kocsis,A., Dobo,J., Balczer,J., Kiss,B., Pal,G. and Gal,P.
Efficient production of fully active, SARS-CoV-2-priming, wildtype TMPRSS2 ectodomain via co-expression of HAI-2 allows for both auto- and cross-activation mechanisms
Biochem J (2025) 482, 1993-2010. PubMed Europe PubMed DOI
Verhulst,E., de Bruyn,M., Berckmans,P., Sim,Y., Augustyns,K., Pintelon,I., Berg,M., Van Wielendaele,P., Lambeir,A.M., Sterckx,Y.G., Nelissen,I. and De Meester,I.
Human Transmembrane Serine Protease 2 (TMPRSS2) on Human Seminal Fluid Extracellular Vesicles Is Proteolytically Active
J Extracell Vesicles (2025) 14, e70061-e70061. PubMed Europe PubMed DOI PMC EPMC
Zhao,Z., Yang,Q., Liu,X., Li,M., Duan,Y., Du,M., Zhou,A., Liu,H., He,Y., Wang,W., Lu,Y., Zhang,X., Wang,H., Yang,X., Zhang,H., Chen,X., Rao,Z. and Yang,H.
The crystal structure of coronavirus RBD-TMPRSS2 complex provides basis for the discovery of therapeutic antibodies
Nat Commun (2025) 16, 6636-6636. PubMed Europe PubMed DOI PMC EPMC

2024

Al-Saigh,N.N., Harb,A.A. and Abdalla,S.
Receptors Involved in COVID-19-Related Anosmia: An Update on the Pathophysiology and the Mechanistic Aspects
Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC V
Bach,M.L., Laftih,S., Andresen,J.K., Pedersen,R.M., Andersen,T.E., Madsen,L.W., Madsen,K., Hinrichs,G.R., Zachar,R., Svenningsen,P., Lund,L., Johansen,I.S., Hansen,L.F., Palarasah,Y. and Jensen,B.L.
ACE2 and TMPRSS2 in human kidney tissue and urine extracellular vesicles with age, sex, and COVID-19
Pflugers Arch (2024) PubMed Europe PubMed DOI
Bashar,N.A.S., Gohar,N.M.A., Tantawy,A.A. and Kamel,M.H.M.
Evaluation of relationship between TMPRSS2 p.(Val197Met) variant and COVID-19 susceptibility and severity
BMC Infect Dis (2024) 24, 112-112. PubMed Europe PubMed DOI PMC EPMC
Bestle,D., Bittel,L., Werner,A.D., Kamper,L., Dolnik,O., Krahling,V., Steinmetzer,T. and Bottcher-Friebertshauser,E.
Novel proteolytic activation of Ebolavirus glycoprotein GP by TMPRSS2 and cathepsin L at an uncharted position can compensate for furin cleavage
Virus Res (2024) 347, 199430-199430. PubMed Europe PubMed DOI K
Calcagnile,M., Damiano,F., Lobreglio,G., Siculella,L., Bozzetti,M.P., Forgez,P., Malgoyre,A., Libert,N., Bucci,C., Alifano,M. and Alifano,P.
In silico evidence that substitution of glycine for valine (p.G8V) in a common variant of TMPRSS2 isoform 1 increases accessibility to an endocytic signal: Implication for SARS-cov-2 entry into host cells and susceptibility to COVID-19
Biochimie (2024) 225, 89-98. PubMed Europe PubMed DOI
Chen,Y., Ou,X., Li,P., Zan,F., Tan,L. and Qian,Z.
Identification of the critical residues of TMPRSS2 for entry and host range of human coronavirus HKU1
J Virol (2024) , e0158724-e0158724. PubMed Europe PubMed DOI
Costa,T.F.R., Catta-Preta,C.M.C., Goundry,A., Carvalho,D.B., Rodrigues,N.S., Vivarini,A.C., de Abreu,M.F., Reis,F.C.G. and Lima,A.P.C.A.
The ecotin-like peptidase inhibitor of Trypanosoma cruzi prevents TMPRSS2-PAR2-TLR4 crosstalk downmodulating infection and inflammation
FASEB J (2024) 38, e23566-e23566. PubMed Europe PubMed DOI K
D'Anna,L., Froux,A., Rainot,A., Spinello,A., Perricone,U., Barbault,F., Grandemange,S., Barone,G., Terenzi,A. and Monari,A.
Resolving the Structure of a Guanine Quadruplex in TMPRSS2 Messenger RNA by Circular Dichroism and Molecular Modeling
Chemistry (2024) , e202403572-e202403572. PubMed Europe PubMed DOI
De Magis,A., Schult,P., Schonleber,A., Linke,R., Ludwig,K.U., Kummerer,B.M. and Paeschke,K.
TMPRSS2 isoform 1 downregulation by G-quadruplex stabilization induces SARS-CoV-2 replication arrest
BMC Biol (2024) 22, 5-5. PubMed Europe PubMed DOI PMC EPMC
de Oliveira-Simoes,F.A., Victorino da Silva Amatto,I., Langer Marciano,C., Rosa-Garzon,N.G.D., Noma Okamoto,D., Juliano,M.A., Juliano,L. and Cabral,H.
Biochemical characterization, stability, and kinetics of three substrates of the recombinant TMPRSS2 serine protease domain
Prep Biochem Biotechnol (2024) , 1-9. PubMed Europe PubMed DOI
Farooqi,A.A., Turgambayeva,A., Almabayeva,A., Zhanaliyeva,M., Orakbay,L., Shabanbayeva,Z., Narmanova,O. and Syzdykbayev,M.K.
Mechanistic Insights and Molecular Diagnostics of TMPRSS2-ERG: Overview of the Journey from Regulation of Signaling Landscape in Fusion Positive Prostate Cancer to Appraisal as a Diagnostic Marker
Front Biosci (Landmark Ed) (2024) 29, 343-343. PubMed Europe PubMed DOI
Fernandez,I., Saunders,N., Duquerroy,S., Bolland,W.H., Arbabian,A., Baquero,E., Blanc,C., Lafaye,P., Haouz,A., Buchrieser,J., Schwartz,O. and Rey,F.A.
Structural basis of TMPRSS2 zymogen activation and recognition by the HKU1 seasonal coronavirus
Cell (2024) 187, 4246-4260. PubMed Europe PubMed DOI
Heindl,M.R., Rupp,A.L., Schwerdtner,M., Bestle,D., Harbig,A., De Rocher,A., Schmacke,L.C., Staker,B., Steinmetzer,T., Stein,D.A., Moulton,H.M. and Bottcher-Friebertshauser,E.
ACE2 acts as a novel regulator of TMPRSS2-catalyzed proteolytic activation of influenza A virus in airway cells
J Virol (2024) 98, e0010224-e0010224. PubMed Europe PubMed DOI PMC EPMC K
Jin,Z., Zhang,Y., Chen,W., Li,H., Shi,L., Wang,D., Zhu,R. and Zhang,C.
Intracellular autoactivation and surface location of hepsin, TMPRSS2, and TMPRSS13
Life Sci (2024) , 123299-123299. PubMed Europe PubMed DOI
Kakizaki,M., Hashimoto,R., Nagata,N., Yamamoto,T., Okura,T., Katoh,H., Kitai,Y., Akahori,Y., Shirato,K., Ryo,A., Takayama,K. and Takeda,M.
The respective roles of TMPRSS2 and cathepsins for SARS-CoV-2 infection in human respiratory organoids
J Virol (2024) , e0185324-e0185324. PubMed Europe PubMed DOI
Kundrapu,D.B., Chaitanya,A.K., Manaswi,K., Kumari,S. and Malla,R.
Quercetin and taxifolin inhibits TMPRSS2 activity and its interaction with EGFR in paclitaxel-resistant breast cancer cells: An in silico and in vitro study
Chem Biol Drug Des (2024) 104, e14600-e14600. PubMed Europe PubMed DOI I
Kwon,T., Artiaga,B.L., McDowell,C.D., Whitworth,K.M., Wells,K.D., Prather,R.S., Delhon,G., Cigan,M., White,S.N., Retallick,J., Gaudreault,N.N., Morozov,I. and Richt,J.A.
Gene editing of pigs to control influenza A virus infections
Emerg Microbes Infect (2024) , 2387449-2387449. PubMed Europe PubMed DOI
McCallum,M., Park,Y.J., Stewart,C., Sprouse,K.R., Addetia,A., Brown,J., Tortorici,M.A., Gibson,C., Wong,E., Ieven,M., Telenti,A. and Veesler,D.
Human coronavirus HKU1 recognition of the TMPRSS2 host receptor
Cell (2024) 187, 4231-4245. PubMed Europe PubMed DOI
McCallum,M., Park,Y.J., Stewart,C., Sprouse,K.R., Brown,J., Tortorici,M.A., Gibson,C., Wong,E., Ieven,M., Telenti,A. and Veesler,D.
Human coronavirus HKU1 recognition of the TMPRSS2 host receptor
bioRxiv (2024) PubMed Europe PubMed DOI PMC EPMC
Meng,R., Zhong,X., Gong,Y., Shi,Y., Li,J., Wu,Z., Duan,Q., Zhang,X., Mei,Y., Zhu,J., Peng,Z., Li,Y. and Song,D.
Discovery and development of novel 10,12-disubstituted aloperine derivatives against HCoV-OC43 by targeting allosteric site of host TMPRSS2
Bioorg Chem (2024) 147, 107317-107317. PubMed Europe PubMed DOI
Mohan,E.C., Savarraj,J.P.J., Colpo,G.D., Morales,D., Finger,C.E., McAlister,A., Ahnstedt,H., Choi,H., McCullough,L.D. and Manwani,B.
Aromatase, testosterone, TMPRSS2: determinants of COVID-19 severity
Biol Sex Differ (2024) 15, 84-84. PubMed Europe PubMed DOI PMC EPMC
Parsons,R.J. and Acharya,P.
Prying the lid open: Atomic-level insights on sialoglycan-TMPRSS2 coordination in HKU1 entry
Cell (2024) 187, 4147-4149. PubMed Europe PubMed DOI
Qu,B., Miskey,C., Gomer,A., Kleinert,R.D.V., Ibanez,S.C., Eberle,R., Ebenig,A., Postmus,D., Nocke,M.K., Herrmann,M., Itotia,T.K., Herrmann,S.T., Heinen,N., Hock,S., Hastert,F.D., von Rhein,C., Schurmann,C., Li,X., van Zandbergen,G., Widera,M., Ciesek,S., Schnierle,B.S., Tarr,A.W., Steinmann,E., Goffinet,C., Pfaender,S., Locker,J.K., Muhlebach,M.D., Todt,D. and Brown,R.J.P.
TMPRSS2-mediated SARS-CoV-2 uptake boosts innate immune activation, enhances cytopathology, and drives convergent virus evolution
Proc Natl Acad Sci U S A (2024) 121, e2407437121-e2407437121. PubMed Europe PubMed DOI PMC EPMC
Saunders,N. and Schwartz,O.
[TMPRSS2 is the receptor of seasonal coronavirus HKU1]
Med Sci (Paris) (2024) 40, 335-337. PubMed Europe PubMed DOI
Schwerdtner,M., Schmacke,L.C., Nave,J., Limburg,H., Steinmetzer,T., Stein,D.A., Moulton,H.M. and Bottcher-Friebertshauser,E.
Unveiling the Role of TMPRSS2 in the Proteolytic Activation of Pandemic and Zoonotic Influenza Viruses and Coronaviruses in Human Airway Cells
Viruses (2024) 16 PubMed Europe PubMed DOI PMC EPMC K
Tanriverdi,O., Alkan,A., Karaoglu,T., Kitapli,S. and Yildiz,A.
COVID-19 and Carcinogenesis: Exploring the Hidden Links
Cureus (2024) 16, e68303-e68303. PubMed Europe PubMed DOI PMC EPMC V
Wu,A., Shi,K., Wang,J., Zhang,R. and Wang,Y.
Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors
Eur J Med Chem (2024) 263, 115923-115923. PubMed Europe PubMed DOI V
Yang,H., Zhou,J.N., Zhang,X.M., Ling,D.D., Sun,Y.B., Li,C.Y., Zhou,Q.Q., Shi,G.N., Wang,S.H., Lin,X.S., Fan,T., Wang,H.Y., Zeng,Q., Jia,Y.L., Xi,J.F., Jin,Y.G., Pei,X.T. and Yue,W.
Nanoengineered Red Blood Cells Loaded with TMPRSS2 and Cathepsin L Inhibitors Block SARS-CoV-2 Pseudovirus Entry into Lung ACE2(+) Cells
Adv Mater (2024) , e2310306-e2310306. PubMed Europe PubMed DOI
Yang,H., Xu,H., Lin,X., Cai,Z., Xia,Y., Wang,Y., Chen,Z., Zhang,K., Wu,Y., Wang,J., Awadasseid,A. and Zhang,W.
Design, synthesis and biological evaluation of novel TMPRSS2-PROTACs with florosubstituted 4-guanidino-N-phenylbenzamide derivative ligands
Bioorg Med Chem (2024) 116, 117982-117982. PubMed Europe PubMed DOI
Zhou,R., He,L., Zhang,J., Zhang,X., Li,Y., Zhan,X. and Tao,L.
Molecular basis of TMPRSS2 recognition by Paeniclostridium sordellii hemorrhagic toxin
Nat Commun (2024) 15, 1976-1976. PubMed Europe PubMed DOI PMC EPMC

2023

Dos Santos Nascimento,I.J. and de Moura,R.O.
Would the Development of a Multitarget Inhibitor of 3CLpro and TMPRSS2 be Promising in the Fight Against SARS-CoV-2?
Med Chem (2023) 19, 405-412. PubMed Europe PubMed DOI V
Drazdauskiene,U., Kapustina,Z., Medziune,J., Dubovskaja,V., Sabaliauskaite,R., Jarmalaite,S. and Lubys,A.
Fusion sequencing via terminator-assisted synthesis (FTAS-seq) identifies TMPRSS2 fusion partners in prostate cancer
Mol Oncol (2023) 17, 993-1006. PubMed Europe PubMed DOI PMC EPMC
Farkas,B., Minneci,M., Misevicius,M. and Rozas,I.
A Tale of Two Proteases: M(Pro) and TMPRSS2 as Targets for COVID-19 Therapies
Pharmaceuticals (Basel) (2023) 16 PubMed Europe PubMed DOI PMC EPMC V
Gioukaki,C., Georgiou,A., Gkaralea,L.E., Kroupis,C., Lazaris,A.C., Alamanis,C. and Thomopoulou,G.E.
Unravelling the Role of P300 and TMPRSS2 in Prostate Cancer: A Literature Review
Int J Mol Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC V
Koistinen,H., Kovanen,R.M., Hollenberg,M.D., Dufour,A., Radisky,E.S., Stenman,U.H., Batra,J., Clements,J., Hooper,J.D., Diamandis,E., Schilling,O., Rannikko,A. and Mirtti,T.
The roles of proteases in prostate cancer
IUBMB Life (2023) 75, 493-513. PubMed Europe PubMed DOI PMC EPMC V
Li,Y., Wang,K., Sun,H., Wu,S., Wang,H., Shi,Y., Li,X., Yan,H., Yang,G., Wu,M., Li,Y., Ding,X., Si,S., Jiang,J., Du,Y., Li,Y. and Hong,B.
Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2
Antiviral Res (2023) 214, 105606-105606. PubMed Europe PubMed DOI PMC EPMC I
Lie,L.K., Synowiec,A., Mazur,J., Rabalski,L. and Pyrc,K.
An engineered A549 cell line expressing CD13 and TMPRSS2 is permissive to clinical isolate of human coronavirus 229E
Virology (2023) 588, 109889-109889. PubMed Europe PubMed DOI
Salaun,C., Tomkinson,N.C.O. and Chamberlain,L.H.
The endoplasmic reticulum-localized enzyme zDHHC6 mediates S-acylation of short transmembrane constructs from multiple type I and II membrane proteins
J Biol Chem (2023) 299, 105201-105201. PubMed Europe PubMed DOI PMC EPMC
Saunders,N., Fernandez,I., Planchais,C., Michel,V., Rajah,M.M., Baquero Salazar,E., Postal,J., Porrot,F., Guivel-Benhassine,F., Blanc,C., Chauveau-Le Friec,G., Martin,A., Grzelak,L., Oktavia,R.M., Meola,A., Ahouzi,O., Hoover-Watson,H., Prot,M., Delaune,D., Cornelissen,M., Deijs,M., Meriaux,V., Mouquet,H., Simon-Loriere,E., van der Hoek,L., Lafaye,P., Rey,F., Buchrieser,J. and Schwartz,O.
TMPRSS2 is a functional receptor for human coronavirus HKU1
Nature (2023) 624, 207-214. PubMed Europe PubMed DOI
Yang,H., Lin,X., Yu,Q., Awadasseid,A. and Zhang,W.
Repurposing and discovery of transmembrane serine protease 2 (TMPRSS2) inhibitors as prophylactic therapies for new coronavirus disease 2019 (COVID-19)
Pharmazie (2023) 78, 217-224. PubMed Europe PubMed DOI V
Zhang,W., Golynker,I., Brosh,R., Fajardo,A., Zhu,Y., Wudzinska,A.M., Ordonez,R., Ribeiro-Dos-Santos,A.M., Carrau,L., Damani-Yokota,P., Yeung,S.T., Khairallah,C., Vela Gartner,A., Chalhoub,N., Huang,E., Ashe,H.J., Khanna,K.M., Maurano,M.T., Kim,S.Y., tenOever,B.R. and Boeke,J.D.
Mouse genome rewriting and tailoring of three important disease loci
Nature (2023) 623, 423-431. PubMed Europe PubMed DOI PMC EPMC

2022

Chen,Y., Yang,W.H., Chen,H.F., Huang,L.M., Gao,J.Y., Lin,C.W., Wang,Y.C., Yang,C.S., Liu,Y.L., Hou,M.H., Tsai,C.L., Chou,Y.Z., Huang,B.Y., Hung,C.F., Hung,Y.L., Wang,W.J., Su,W.C., Kumar,V., Wu,Y.C., Chao,S.W., Chang,C.S., Chen,J.S., Chiang,Y.P., Cho,D.Y., Jeng,L.B., Tsai,C.H. and Hung,M.C.
Tafenoquine and its derivatives as inhibitors for the severe acute respiratory syndrome coronavirus 2
J Biol Chem (2022) 298, 101658-101658. PubMed Europe PubMed DOI PMC EPMC I
David,A., Parkinson,N., Peacock,T.P., Pairo-Castineira,E., Khanna,T., Cobat,A., Tenesa,A., Sancho-Shimizu,V., Casanova,J.L., Abel,L., Barclay,W.S., Baillie,J.K. and Sternberg,M.J.
A common TMPRSS2 variant has a protective effect against severe COVID-19
Curr Res Transl Med (2022) 70, 103333-103333. PubMed Europe PubMed DOI PMC EPMC
de Andrade,C.C., Silva,A.T.P., Vasconcelos,L.R.S., Oliveira,P.R.S., de Souza,C.D.F., da Costa Armstrong,A. and do Carmo,R.F.
A Polymorphism in the TMPRSS2 Gene Increases the Risk of Death in Older Patients Hospitalized with COVID-19
Viruses (2022) 14 PubMed Europe PubMed DOI PMC EPMC
Dieter,C., de Almeida Brondani,L., Lemos,N.E., Schaeffer,A.F., Zanotto,C., Ramos,D.T., Girardi,E., Pellenz,F.M., Camargo,J.L., Moresco,K.S., da Silva,L.L., Aubin,M.R., de Oliveira,M.S., Rech,T.H., Canani,L.H., Gerchman,F., Leitao,C.B. and Crispim,D.
Polymorphisms in ACE1, TMPRSS2, IFIH1, IFNAR2, and TYK2 Genes Are Associated with Worse Clinical Outcomes in COVID-19
Genes (Basel) (2022) 14 PubMed Europe PubMed DOI PMC EPMC
Fraser,B.J., Beldar,S., Seitova,A., Hutchinson,A., Mannar,D., Li,Y., Kwon,D., Tan,R., Wilson,R.P., Leopold,K., Subramaniam,S., Halabelian,L., Arrowsmith,C.H. and Benard,F.
Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation
Nat Chem Biol (2022) 18, 963-971. PubMed Europe PubMed DOI
Giannareas,N., Zhang,Q., Yang,X., Na,R., Tian,Y., Yang,Y., Ruan,X., Huang,D., Yang,X., Wang,C., Zhang,P., Manninen,A., Wang,L. and Wei,G.H.
Extensive germline-somatic interplay contributes to prostate cancer progression through HNF1B co-option of TMPRSS2-ERG
Nat Commun (2022) 13, 7320-7320. PubMed Europe PubMed DOI PMC EPMC
Govender,N., Khaliq,O., Moodley,J. and Naicker,T.
Unravelling the Mechanistic Role of ACE2 and TMPRSS2 in Hypertension: A Risk Factor for COVID-19
Curr Hypertens Rev (2022) 18, 130-137. PubMed Europe PubMed DOI V
Iwata-Yoshikawa,N., Kakizaki,M., Shiwa-Sudo,N., Okura,T., Tahara,M., Fukushi,S., Maeda,K., Kawase,M., Asanuma,H., Tomita,Y., Takayama,I., Matsuyama,S., Shirato,K., Suzuki,T., Nagata,N. and Takeda,M.
Essential role of TMPRSS2 in SARS-CoV-2 infection in murine airways
Nat Commun (2022) 13, 6100-6100. PubMed Europe PubMed DOI PMC EPMC
Karimian,A., Behjati,M. and Karimian,M.
Molecular mechanisms involved in anosmia induced by SARS-CoV-2, with a focus on the transmembrane serine protease TMPRSS2
Arch Virol (2022) 167, 1931-1946. PubMed Europe PubMed DOI PMC EPMC V
Lee,J.H., Lee,C.E., Yoo,Y., Shin,E., An,J., Park,S.Y., Song,W.J., Kwon,H.S., Cho,Y.S., Moon,H.B. and Kim,T.B.
Soluble ACE2 and TMPRSS2 Levels in the Serum of Asthmatic Patients
J Korean Med Sci (2022) 37, e65-e65. PubMed Europe PubMed DOI PMC EPMC
Liu,G., Du,W., Sang,X., Tong,Q., Wang,Y., Chen,G., Yuan,Y., Jiang,L., Cheng,W., Liu,D., Tian,Y. and Fu,X.
RNA G-quadruplex in TMPRSS2 reduces SARS-CoV-2 infection
Nat Commun (2022) 13, 1444-1444. PubMed Europe PubMed DOI PMC EPMC
Mantzourani,C., Vasilakaki,S., Gerogianni,V.E. and Kokotos,G.
The discovery and development of transmembrane serine protease 2 (TMPRSS2) inhibitors as candidate drugs for the treatment of COVID-19
Expert Opin Drug Discov (2022) 17, 231-246. PubMed Europe PubMed DOI PMC EPMC V I
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2021

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Alpha 1 Antitrypsin is an Inhibitor of the SARS-CoV-2-Priming Protease TMPRSS2
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Expression of ACE2 and TMPRSS2 Proteins in the Upper and Lower Aerodigestive Tracts of Rats: Implications on COVID 19 Infections
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2020

TMPRSS2 enzymatic activity
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Ethnic differences in alpha-1 antitrypsin deficiency allele frequencies may partially explain national differences in COVID-19 fatality rates
FASEB J (2020) 34, 14160-14165. PubMed Europe PubMed DOI PMC EPMC
Shrimp,J.H., Kales,S.C., Sanderson,P.E., Simeonov,A., Shen,M. and Hall,M.D.
An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19
bioRxiv (2020) PubMed Europe PubMed DOI PMC EPMC I
Shrimp,J.H., Kales,S.C., Sanderson,P.E., Simeonov,A., Shen,M. and Hall,M.D.
An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19
ACS Pharmacol Transl Sci (2020) 3, 997-1007. PubMed Europe PubMed DOI PMC EPMC I
Singh,H., Choudhari,R., Nema,V. and Khan,A.A.
ACE2 and TMPRSS2 polymorphisms in various diseases with special reference to its impact on COVID-19 disease
Microb Pathog (2020) 150, 104621-104621. PubMed Europe PubMed DOI PMC EPMC
Singh,N., Decroly,E., Khatib,A.M. and Villoutreix,B.O.
Structure-based drug repositioning over the human TMPRSS2 protease domain: search for chemical probes able to repress SARS-CoV-2 Spike protein cleavages
Eur J Pharm Sci (2020) 153, 105495-105495. PubMed Europe PubMed DOI PMC EPMC
Stanton,B.A., Hampton,T.H. and Ashare,A.
SARS-CoV-2 (COVID-19) and Cystic Fibrosis
Am J Physiol Lung Cell Mol Physiol (2020) 319, L408-L415. PubMed Europe PubMed DOI
Strope,J.D., Chau,C.H. and Figg,W.D.
Are sex discordant outcomes in COVID-19 related to sex hormones?
Semin Oncol (2020) 47, 335-340. PubMed Europe PubMed DOI PMC EPMC
Sungnak,W., Huang,N., Becavin,C. and Berg,M.
SARS-CoV-2 Entry Genes Are Most Highly Expressed in Nasal Goblet and Ciliated Cells within Human Airways
ArXiv (2020) PubMed Europe PubMed PMC EPMC
Taglauer,E., Benarroch,Y., Rop,K., Barnett,E., Sabharwal,V., Yarrington,C. and Wachman,E.M.
Consistent localization of SARS-CoV-2 spike glycoprotein and ACE2 over TMPRSS2 predominance in placental villi of 15 COVID-19 positive maternal-fetal dyads
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Taneera,J., El-Huneidi,W., Hamad,M., Mohammed,A.K., Elaraby,E. and Hachim,M.Y.
Expression Profile of SARS-CoV-2 Host Receptors in Human Pancreatic Islets Revealed Upregulation of ACE2 in Diabetic Donors
Biology (Basel) (2020) 9 PubMed Europe PubMed DOI PMC EPMC
Ten Hove,A.S., Brinkman,D.J., Li Yim,A.Y.F., Verseijden,C., Hakvoort,T.B.M., Admiraal,I., Welting,O., van Hamersveld,P.H.P., Sinniger,V., Bonaz,B., Luyer,M.D. and de Jonge,W.J.
The role of nicotinic receptors in SARS-CoV-2 receptor ACE2 expression in intestinal epithelia
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Thunders,M. and Delahunt,B.
Gene of the month: TMPRSS2 (transmembrane serine protease 2)
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Tomchaney,M., Contoli,M., Mayo,J., Baraldo,S., Shuaizhi,L., Cabel,C.R., Bull,D.A., Lick,S., Malo,J., Knoper,S., Kim,S.S., Tram,J., Rojas-Quintero,J., Kraft,M., Ledford,J., Tesfaigzi,Y., Martinez,F.D., Thorne,C.A., Kheradmand,F., Campos,S.K., Papi,A. and Polverino,F.
Paradoxical effects of cigarette smoke and COPD on SARS-CoV2 infection and disease
bioRxiv (2020) PubMed Europe PubMed DOI PMC EPMC
Umadevi,P., Manivannan,S., Fayad,A.M. and Shelvy,S.
In silico analysis of phytochemicals as potential inhibitors of proteases involved in SARS-CoV-2 infection
J Biomol Struct Dyn (2020) , 1-9. PubMed Europe PubMed DOI I
Vargas-Alarcon,G., Posadas-Sanchez,R. and Ramirez-Bello,J.
Variability in genes related to SARS-CoV-2 entry into host cells (ACE2, TMPRSS2, TMPRSS11A, ELANE, and CTSL) and its potential use in association studies
Life Sci (2020) 260, 118313-118313. PubMed Europe PubMed DOI PMC EPMC
Varma,P., Lybrand,Z.R., Antopia,M.C. and Hsieh,J.
Novel Targets of SARS-CoV-2 Spike Protein in Human Fetal Brain Development Suggest Early Pregnancy Vulnerability
Front Neurosci (2020) 14, 614680-614680. PubMed Europe PubMed DOI PMC EPMC
Vivek-Ananth,R.P., Rana,A., Rajan,N., Biswal,H.S. and Samal,A.
In Silico Identification of Potential Natural Product Inhibitors of Human Proteases Key to SARS-CoV-2 Infection
Molecules (2020) 25 PubMed Europe PubMed DOI
Vo,T., Paudel,K., Choudhary,I., Patial,S. and Saini,Y.
Ozone exposure upregulates the expression of host susceptibility protein TMPRSS2 to SARS-CoV-2
bioRxiv (2020) PubMed Europe PubMed DOI PMC EPMC
Voinsky,I. and Gurwitz,D.
Smoking and COVID-19: Similar bronchial ACE2 and TMPRSS2 expression and higher TMPRSS4 expression in current versus never smokers
Drug Dev Res (2020) 81, 1073-1080. PubMed Europe PubMed DOI PMC EPMC
Wang,B., Kovalchuk,A., Li,D., Rodriguez-Juarez,R., Ilnytskyy,Y., Kovalchuk,I. and Kovalchuk,O.
In search of preventive strategies: novel high-CBD Cannabis sativa extracts modulate ACE2 expression in COVID-19 gateway tissues
Aging (Albany NY) (2020) 12, 22425-22444. PubMed Europe PubMed DOI
Wang,S.C., Chen,Y., Wang,Y.C., Wang,W.J., Yang,C.S., Tsai,C.L., Hou,M.H., Chen,H.F., Shen,Y.C. and Hung,M.C.
Tannic acid suppresses SARS-CoV-2 as a dual inhibitor of the viral main protease and the cellular TMPRSS2 protease
Am J Cancer Res (2020) 10, 4538-4546. PubMed Europe PubMed PMC EPMC
Weatherbee,B.A.T., Glover,D.M. and Zernicka-Goetz,M.
Expression of SARS-CoV-2 receptor ACE2 and the protease TMPRSS2 suggests susceptibility of the human embryo in the first trimester
Open Biol (2020) 10, 200162-200162. PubMed Europe PubMed DOI
Wu,C., Ye,D., Mullick,A.E., Li,Z., Danser,A.H.J., Daugherty,A. and Lu,H.S.
Effects of Renin-Angiotensin Inhibition on ACE2 and TMPRSS2 Expression: Insights into COVID-19
Hypertension (2020) 76, e29-e30. PubMed Europe PubMed DOI PMC EPMC
Wu,C.Y., Lin,Y.S., Yang,Y.H., Shu,L.H., Cheng,Y.C. and Liu,H.T.
GB-2 inhibits ACE2 and TMPRSS2 expression: In vivo and in vitro studies
Biomed Pharmacother (2020) 132, 110816-110816. PubMed Europe PubMed DOI PMC EPMC
Wu,C.Y., Lin,Y.S., Yang,Y.H., Shu,L.H., Cheng,Y.C. and Liu,H.T.
Potential Simultaneous Inhibitors of Angiotensin-Converting Enzyme 2 and Transmembrane Protease, Serine 2
Front Pharmacol (2020) 11, 584158-584158. PubMed Europe PubMed DOI PMC EPMC
Yang,C., Keshavjee,S. and Liu,M.
Alpha-1 Antitrypsin for COVID-19 Treatment: Dual Role in Antiviral Infection and Anti-Inflammation
Front Pharmacol (2020) 11, 615398-615398. PubMed Europe PubMed DOI PMC EPMC
Zarubin,A., Stepanov,V., Markov,A., Kolesnikov,N., Marusin,A., Khitrinskaya,I., Swarovskaya,M., Litvinov,S., Ekomasova,N., Dzhaubermezov,M., Maksimova,N., Sukhomyasova,A., Shtygasheva,O., Khusnutdinova,E., Radzhabov,M. and Kharkov,V.
Structural Variability, Expression Profile, and Pharmacogenetic Properties of TMPRSS2 Gene as a Potential Target for COVID-19 Therapy
Genes (Basel) (2020) 12 PubMed Europe PubMed DOI PMC EPMC I
Zhang,S., Liu,Y., Wang,X., Yang,L., Li,H., Wang,Y., Liu,M., Zhao,X., Xie,Y., Yang,Y., Zhang,S., Fan,Z., Dong,J., Yuan,Z., Ding,Z., Zhang,Y. and Hu,L.
SARS-CoV-2 binds platelet ACE2 to enhance thrombosis in COVID-19
J Hematol Oncol (2020) 13, 120-120. PubMed Europe PubMed DOI PMC EPMC
Zheng,M., Zhao,X., Zheng,S., Chen,D., Du,P., Li,X., Jiang,D., Guo,J.T., Zeng,H. and Lin,H.
Bat SARS-Like WIV1 coronavirus uses the ACE2 of multiple animal species as receptor and evades IFITM3 restriction via TMPRSS2 activation of membrane fusion
Emerg Microbes Infect (2020) 9, 1567-1579. PubMed Europe PubMed DOI
Zhou,L., Xu,Z., Castiglione,G.M., Soiberman,U.S., Eberhart,C.G. and Duh,E.J.
ACE2 and TMPRSS2 are expressed on the human ocular surface, suggesting susceptibility to SARS-CoV-2 infection
Ocul Surf (2020) 18, 537-544. PubMed Europe PubMed DOI PMC EPMC
Zhou,L., Huntington,K., Zhang,S., Carlsen,L., So,E.Y., Parker,C., Sahin,I., Safran,H., Kamle,S., Lee,C.M., Lee,C.G., Elias,J.A., Campbell,K.S., Naik,M.T., Atwood,W.J., Youssef,E., Pachter,J.A., Navaraj,A., Seyhan,A.A., Liang,O. and El-Deiry,W.S.
Natural Killer cell activation, reduced ACE2, TMPRSS2, cytokines G-CSF, M-CSF and SARS-CoV-2-S pseudovirus infectivity by MEK inhibitor treatment of human cells
bioRxiv (2020) PubMed Europe PubMed DOI PMC EPMC
Zhou,L., Niu,Z., Jiang,X., Zhang,Z., Zheng,Y., Wang,Z., Zhu,Y., Gao,L., Huang,H., Wang,X. and Sun,Q.
SARS-CoV-2 Targets by the pscRNA Profiling of ACE2, TMPRSS2 and Furin Proteases
iScience (2020) 23, 101744-101744. PubMed Europe PubMed DOI PMC EPMC
Zhou,L., Huntington,K., Zhang,S., Carlsen,L., So,E.Y., Parker,C., Sahin,I., Safran,H., Kamle,S., Lee,C.M., Geun Lee,C., Elias,A., Campbell,S., Naik,T., Atwood,J., Youssef,E., Pachter,A., Navaraj,A., Seyhan,A., Liang,O. and El-Deiry,W.S.
MEK inhibitors reduce cellular expression of ACE2, pERK, pRb while stimulating NK-mediated cytotoxicity and attenuating inflammatory cytokines relevant to SARS-CoV-2 infection
Oncotarget (2020) 11, 4201-4223. PubMed Europe PubMed DOI PMC EPMC
Zipeto,D., Palmeira,J.D.F., Arganaraz,G.A. and Arganaraz,E.R.
ACE2/ADAM17/TMPRSS2 Interplay May Be the Main Risk Factor for COVID-19
Front Immunol (2020) 11, 576745-576745. PubMed Europe PubMed DOI PMC EPMC V

2019

Iwata-Yoshikawa,N., Okamura,T., Shimizu,Y., Hasegawa,H., Takeda,M. and Nagata,N.
TMPRSS2 contributes to virus spread and immunopathology in the airways of murine models after coronavirus infection
J Virol (2019) 93, e01815-18-e01815-18. PubMed Europe PubMed DOI K
Lambertz,R.L.O., Gerhauser,I., Nehlmeier,I., Leist,S.R., Kollmus,H., Pohlmann,S. and Schughart,K.
Tmprss2 knock-out mice are resistant to H10 influenza A virus pathogenesis
J Gen Virol (2019) 100, 1073-1078. PubMed Europe PubMed DOI K
Limburg,H., Harbig,A., Bestle,D., Stein,D.A., Moulton,H.M., Jaeger,J., Janga,H., Hardes,K., Koepke,J., Schulte,L., Koczulla,A.R., Schmeck,B., Klenk,H.D. and Bottcher-Friebertshauser,E.
TMPRSS2 is the major activating protease of influenza A virus in primary human airway cells and influenza B virus in human type II pneumocytes
J Virol (2019) 93, e00649-19-e00649-19. PubMed Europe PubMed DOI

2018

Shirato,K., Kawase,M. and Matsuyama,S.
Wild-type human coronaviruses prefer cell-surface TMPRSS2 to endosomal cathepsins for cell entry
Virology (2018) 517, 9-15. PubMed Europe PubMed DOI

2017

Laporte,M. and Naesens,L.
Airway proteases: an emerging drug target for influenza and other respiratory virus infections
Curr Opin Virol (2017) 24, 16-24. PubMed Europe PubMed DOI
Reid,J.C., Matsika,A., Davies,C.M., He,Y., Broomfield,A., Bennett,N.C., Magdolen,V., Srinivasan,B., Clements,J.A. and Hooper,J.D.
Pericellular regulation of prostate cancer expressed kallikrein-related peptidases and matrix metalloproteinases by cell surface serine proteases
Am J Cancer Res (2017) 7, 2257-2274. PubMed Europe PubMed PMC EPMC
Reinke,L.M., Spiegel,M., Plegge,T., Hartleib,A., Nehlmeier,I., Gierer,S., Hoffmann,M., Hofmann-Winkler,H., Winkler,M. and Pohlmann,S.
Different residues in the SARS-CoV spike protein determine cleavage and activation by the host cell protease TMPRSS2
PLoS ONE (2017) 12, e0179177-e0179177. PubMed Europe PubMed DOI
Shen,L.W., Mao,H.J., Wu,Y.L., Tanaka,Y. and Zhang,W.
TMPRSS2: A potential target for treatment of influenza virus and coronavirus infections
Biochimie (2017) 142, 1-10. PubMed Europe PubMed DOI T
Tanabe,L.M. and List,K.
The role of type II transmembrane serine protease-mediated signaling in cancer
FEBS J (2017) 284, 1421-1436. PubMed Europe PubMed DOI I
Zmora,P., Molau-Blazejewska,P., Bertram,S., Walendy-Gnirss,K., Nehlmeier,I., Hartleib,A., Moldenhauer,A.S., Konzok,S., Dehmel,S., Sewald,K., Brinkmann,C., Curths,C., Knauf,S., Gruber,J., Matz-Rensing,K., Dahlmann,F., Braun,A. and Pohlmann,S.
Non-human primate orthologues of TMPRSS2 cleave and activate the influenza virus hemagglutinin
PLoS ONE (2017) 12, e0176597-e0176597. PubMed Europe PubMed DOI

2016

Hoffmann,M., Kruger,N., Zmora,P., Wrensch,F., Herrler,G. and Pohlmann,S.
The hemagglutinin of bat-associated influenza viruses is activated by TMPRSS2 for pH-dependent entry into bat but not human cells
PLoS ONE (2016) 11, e0152134-e0152134. PubMed Europe PubMed DOI PMC EPMC
Kuhn,N., Bergmann,S., Kosterke,N., Lambertz,R.L., Keppner,A., van den Brand,J.M., Pohlmann,S., Weiss,S., Hummler,E., Hatesuer,B. and Schughart,K.
The proteolytic activation of (H3N2) influenza A virus hemagglutinin is facilitated by different type II transmembrane serine proteases
J Virol (2016) 90, 4298-4307. PubMed Europe PubMed DOI
Paszti-Gere,E., Czimmermann,E., Ujhelyi,G., Balla,P., Maiwald,A. and Steinmetzer,T.
In vitro characterization of TMPRSS2 inhibition in IPEC-J2 cells
J Enzyme Inhib Med Chem (2016) 31, 123-129. PubMed Europe PubMed DOI I
Sakai,K., Ami,Y., Nakajima,N., Nakajima,K., Kitazawa,M., Anraku,M., Takayama,I., Sangsriratanakul,N., Komura,M., Sato,Y., Asanuma,H., Takashita,E., Komase,K., Takehara,K., Tashiro,M., Hasegawa,H., Odagiri,T. and Takeda,M.
TMPRSS2 independency for haemagglutinin cleavage in vivo differentiates influenza B virus from influenza A virus
Sci Rep (2016) 6, 29430-29430. PubMed Europe PubMed DOI PMC EPMC
Shirato,K., Kanou,K., Kawase,M. and Matsuyama,S.
Clinical isolates of human coronavirus 229E bypass the endosome for cell entry
J Virol (2016) 91, e01387-16-e01387-16. PubMed Europe PubMed DOI

2015

Esumi,M., Ishibashi,M., Yamaguchi,H., Nakajima,S., Tai,Y., Kikuta,S., Sugitani,M., Takayama,T., Tahara,M., Takeda,M. and Wakita,T.
Transmembrane serine protease TMPRSS2 activates hepatitis C virus infection
Hepatology (2015) 61, 437-446. PubMed Europe PubMed DOI
Ko,C.J., Huang,C.C., Lin,H.Y., Juan,C.P., Lan,S.W., Shyu,H.Y., Wu,S.R., Hsiao,P.W., Huang,H.P., Shun,C.T. and Lee,M.S.
Androgen-induced TMPRSS2 activates matriptase and promotes extracellular matrix degradation, prostate cancer cell invasion, tumor growth, and metastasis
Cancer Res (2015) 75, 2949-2960. PubMed Europe PubMed DOI
Lam,D.K., Dang,D., Flynn,A.N., Hardt,M. and Schmidt,B.L.
TMPRSS2, a novel membrane-anchored mediator in cancer pain
Pain (2015) 156, 923-930. PubMed Europe PubMed DOI T
Zmora,P., Moldenhauer,A.S., Hofmann-Winkler,H. and Pohlmann,S.
TMPRSS2 isoform 1 activates respiratory viruses and is expressed in viral target cells
PLoS ONE (2015) 10, e0138380-e0138380. PubMed Europe PubMed DOI R

2014

Heurich,A., Hofmann-Winkler,H., Gierer,S., Liepold,T., Jahn,O. and Pohlmann,S.
TMPRSS2 and ADAM17 cleave ACE2 differentially and only proteolysis by TMPRSS2 augments entry driven by the severe acute respiratory syndrome coronavirus spike protein
J Virol (2014) 88, 1293-1307. PubMed Europe PubMed DOI
Lucas,J.M., Heinlein,C., Kim,T., Hernandez,S.A., Malik,M.S., True,L.D., Morrissey,C., Corey,E., Montgomery,B., Mostaghel,E., Clegg,N., Coleman,I., Brown,C.M., Schneider,E.L., Craik,C., Simon,J.A., Bedalov,A. and Nelson,P.S.
The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis
Cancer Discov (2014) 4, 1310-1325. PubMed Europe PubMed DOI T
Phillips,R.
Prostate cancer: TMPRSS2 promotes metastasis through proteolysis
Nat Rev Urol (2014) 11, 546-546. PubMed Europe PubMed DOI
Sakai,K., Ami,Y., Tahara,M., Kubota,T., Anraku,M., Abe,M., Nakajima,N., Sekizuka,T., Shirato,K., Suzaki,Y., Ainai,A., Nakatsu,Y., Kanou,K., Nakamura,K., Suzuki,T., Komase,K., Nobusawa,E., Maenaka,K., Kuroda,M., Hasegawa,H., Kawaoka,Y., Tashiro,M. and Takeda,M.
The host protease TMPRSS2 plays a major role in in vivo replication of emerging H7N9 and seasonal influenza viruses
J Virol (2014) 88, 5608-5616. PubMed Europe PubMed DOI
Tarnow,C., Engels,G., Arendt,A., Schwalm,F., Sediri,H., Preuss,A., Nelson,P.S., Garten,W., Klenk,H.D., Gabriel,G. and Bottcher-Friebertshauser,E.
TMPRSS2 is a host factor that is essential for pneumotropism and pathogenicity of H7N9 influenza A virus in mice
J Virol (2014) 88, 4744-4751. PubMed Europe PubMed DOI
Velaeti,S., Dimitriadis,E., Kontogianni-Katsarou,K., Savvani,A., Sdrolia,E., Pantazi,G., Stefanakis,S., Trangas,T., Pandis,N. and Petraki,K.
Detection of TMPRSS2-ERG fusion gene in benign prostatic hyperplasia
Tumour Biol (2014) 35, 9597-9602. PubMed Europe PubMed DOI
Wang,S., Kollipara,R.K., Srivastava,N., Li,R., Ravindranathan,P., Hernandez,E., Freeman,E., Humphries,C.G., Kapur,P., Lotan,Y., Fazli,L., Gleave,M.E., Plymate,S.R., Raj,G.V., Hsieh,J.T. and Kittler,R.
Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer
Proc Natl Acad Sci U S A (2014) 111, 4251-4256. PubMed Europe PubMed DOI I

2013

Abe,M., Tahara,M., Sakai,K., Yamaguchi,H., Kanou,K., Shirato,K., Kawase,M., Noda,M., Kimura,H., Matsuyama,S., Fukuhara,H., Mizuta,K., Maenaka,K., Ami,Y., Esumi,M., Kato,A. and Takeda,M.
TMPRSS2 is an activating protease for respiratory parainfluenza viruses
J Virol (2013) 87, 11930-11935. PubMed Europe PubMed DOI
Bertram,S., Dijkman,R., Habjan,M., Heurich,A., Gierer,S., Glowacka,I., Welsch,K., Winkler,M., Schneider,H., Hofmann-Winkler,H., Thiel,V. and Pohlmann,S.
TMPRSS2 activates the human coronavirus 229E for cathepsin-independent host cell entry and is expressed in viral target cells in the respiratory epithelium
J Virol (2013) 87, 6150-6160. PubMed Europe PubMed DOI
Galloway,S.E., Reed,M.L., Russell,C.J. and Steinhauer,D.A.
Influenza HA subtypes demonstrate divergent phenotypes for cleavage activation and pH of fusion: implications for host range and adaptation
PLoS Pathog (2013) 9, e1003151-e1003151. PubMed Europe PubMed DOI PMC EPMC
Hatesuer,B., Bertram,S., Mehnert,N., Bahgat,M.M., Nelson,P.S., Pohlman,S. and Schughart,K.
Tmprss2 is essential for influenza H1N1 virus pathogenesis in mice
PLoS Pathog (2013) 9, e1003774-e1003774. PubMed Europe PubMed DOI PMC EPMC K
Meyer,D., Sielaff,F., Hammami,M., Bottcher-Friebertshauser,E., Garten,W. and Steinmetzer,T.
Identification of the first synthetic inhibitors of the type II transmembrane serine protease TMPRSS2 suitable for inhibition of influenza virus activation
Biochem J (2013) 452, 331-343. PubMed Europe PubMed DOI I
Shirato,K., Kawase,M. and Matsuyama,S.
Middle East respiratory syndrome coronavirus infection mediated by the transmembrane serine protease TMPRSS2
J Virol (2013) 87, 12552-12561. PubMed Europe PubMed DOI I

2012

Bottcher-Friebertshauser,E., Lu,Y., Meyer,D., Sielaff,F., Steinmetzer,T., Klenk,H.D. and Garten,W.
Hemagglutinin activating host cell proteases provide promising drug targets for the treatment of influenza A and B virus infections
Vaccine (2012) 30, 7374-7380. PubMed Europe PubMed DOI I
Rao,N.V. and Hoidal,J.R.
Epitheliasin
[ISSN:978-0-12-407742-3] (2012) 3, 3003-3007. DOI
St John,J., Powell,K., Conley-Lacomb,M.K. and Chinni,S.R.
TMPRSS2-ERG fusion gene expression in prostate tumor cells and its clinical and biological significance in prostate cancer progression
J Cancer Sci Ther (2012) 4, 94-101. PubMed Europe PubMed DOI PMC EPMC

2011

Antalis,T.M., Bugge,T.H. and Wu,Q.
Membrane-anchored serine proteases in health and disease
Prog Mol Biol Transl Sci (2011) 99, 1-50. PubMed Europe PubMed DOI V
Bottcher-Friebertshauser,E., Stein,D.A., Klenk,H.D. and Garten,W.
Inhibition of influenza virus infection in human airway cell cultures by an antisense peptide-conjugated morpholino oligomer targeting the hemagglutinin-activating protease TMPRSS2
J Virol (2011) 85, 1554-1562. PubMed Europe PubMed DOI
Glowacka,I., Bertram,S., Muller,M.A., Allen,P., Soilleux,E., Pfefferle,S., Steffen,I., Tsegaye,T.S., He,Y., Gnirss,K., Niemeyer,D., Schneider,H., Drosten,C. and Pohlmann,S.
Evidence that TMPRSS2 activates the severe acute respiratory syndrome coronavirus spike protein for membrane fusion and reduces viral control by the humoral immune response
J Virol (2011) 85, 4122-4134. PubMed Europe PubMed DOI
Swanson,T.A., Krueger,S.A., Galoforo,S., Thibodeau,B.J., Martinez,A.A., Wilson,G.D. and Marples,B.
TMPRSS2/ERG fusion gene expression alters chemo- and radio-responsiveness in cell culture models of androgen independent prostate cancer
Prostate (2011) 71, 1548-1558. PubMed Europe PubMed DOI M

2010

Bertram,S., Glowacka,I., Blazejewska,P., Soilleux,E., Allen,P., Danisch,S., Steffen,I., Choi,S.Y., Park,Y., Schneider,H., Schughart,K. and Pohlmann,S.
TMPRSS2 and TMPRSS4 facilitate trypsin-independent spread of influenza virus in Caco-2 cells
J Virol (2010) 84, 10016-10025. PubMed Europe PubMed DOI
Bertram,S., Glowacka,I., Steffen,I., Kuhl,A. and Pohlmann,S.
Novel insights into proteolytic cleavage of influenza virus hemagglutinin
Rev Med Virol (2010) 20, 298-310. PubMed Europe PubMed DOI
Bottcher-Friebertshauser,E., Freuer,C., Sielaff,F., Schmidt,S., Eickmann,M., Uhlendorff,J., Steinmetzer,T., Klenk,H.D. and Garten,W.
Cleavage of influenza virus hemagglutinin by airway proteases TMPRSS2 and HAT differs in subcellular localization and susceptibility to protease inhibitors
J Virol (2010) 84, 5605-5614. PubMed Europe PubMed DOI
Chen,Y.W., Lee,M.S., Lucht,A., Chou,F.P., Huang,W., Havighurst,T.C., Kim,K., Wang,J.K., Antalis,T.M., Johnson,M.D. and Lin,C.Y.
TMPRSS2, a serine protease expressed in the prostate on the apical surface of luminal epithelial cells and released into semen in prostasomes, is misregulated in prostate cancer cells
Am J Pathol (2010) 176, 2986-2996. PubMed Europe PubMed DOI
Matsuyama,S., Nagata,N., Shirato,K., Kawase,M., Takeda,M. and Taguchi,F.
Efficient activation of the severe acute respiratory syndrome coronavirus spike protein by the transmembrane protease TMPRSS2
J Virol (2010) 84, 12658-12664. PubMed Europe PubMed DOI

2009

Bottcher,E., Freuer,C., Steinmetzer,T., Klenk,H.D. and Garten,W.
MDCK cells that express proteases TMPRSS2 and HAT provide a cell system to propagate influenza viruses in the absence of trypsin and to study cleavage of HA and its inhibition
Vaccine (2009) 27, 6324-6329. PubMed Europe PubMed DOI
Chaipan,C., Kobasa,D., Bertram,S., Glowacka,I., Steffen,I., Tsegaye,T.S., Takeda,M., Bugge,T.H., Kim,S., Park,Y., Marzi,A. and Pohlmann,S.
Proteolytic activation of the 1918 influenza virus hemagglutinin
J Virol (2009) 83, 3200-3211. PubMed Europe PubMed DOI PMC EPMC

2008

Lucas,J.M., True,L., Hawley,S., Matsumura,M., Morrissey,C., Vessella,R. and Nelson,P.S.
The androgen-regulated type II serine protease TMPRSS2 is differentially expressed and mislocalized in prostate adenocarcinoma
J Pathol (2008) 215, 118-125. PubMed Europe PubMed DOI
Narod,S.A., Seth,A. and Nam,R.
Fusion in the ETS gene family and prostate cancer
Br J Cancer (2008) 99, 847-851. PubMed Europe PubMed DOI PMC EPMC
Shirogane,Y., Takeda,M., Iwasaki,M., Ishiguro,N., Takeuchi,H., Nakatsu,Y., Tahara,M., Kikuta,H. and Yanagi,Y.
Efficient multiplication of human metapneumovirus in Vero cells expressing the transmembrane serine protease TMPRSS2
J Virol (2008) 82, 8942-8946. PubMed Europe PubMed DOI PMC EPMC

2006

Bottcher,E., Matrosovich,T., Beyerle,M., Klenk,H.D., Garten,W. and Matrosovich,M.
Proteolytic activation of influenza viruses by serine proteases TMPRSS2 and HAT from human airway epithelium
J Virol (2006) 80, 9896-9898. PubMed Europe PubMed DOI
Kim,T.S., Heinlein,C., Hackman,R.C. and Nelson,P.S.
Phenotypic analysis of mice lacking the Tmprss2-encoded protease
Mol Cell Biol (2006) 26, 965-975. PubMed Europe PubMed DOI PMC EPMC K

2005

[YEAR:15-6-2005]Wilson,S., Greer,B., Hooper,J., Zijlstra,A., Walker,B., Quigley,J. and Hawthorne,S.
The membrane-anchored serine protease, TMPRSS2, activates PAR-2 in prostate cancer cells
Biochem J (15-6-2005) 388, 967-972. PubMed Europe PubMed DOI PMC EPMC

2004

Rao,N.V. and Hoidal,J.R.
Epitheliasin
[ISSN:0-12-079610-4] (2004) 2, 1704-1706. V

2003

Szabo,R., Wu,Q., Dickson,R.B., Netzel-Arnett,S., Antalis,T.M. and Bugge,T.H.
Type II transmembrane serine proteases
Thromb Haemost (2003) 90, 185-193. PubMed Europe PubMed DOI V

2001

[YEAR:15-2-2001]Afar,D.E., Vivanco,I., Hubert,R.S., Kuo,J., Chen,E., Saffran,D.C., Raitano,A.B. and Jakobovits,A.
Catalytic cleavage of the androgen-regulated TMPRSS2 protease results in its secretion by prostate and prostate cancer epithelia
Cancer Res (15-2-2001) 61, 1686-1692. PubMed Europe PubMed
Jacquinet,E., Rao,N.V., Rao,G.V., Wang,Z.M., Albertine,K.H. and Hoidal,J.R.
Cloning and characterization of the cDNA and gene for human epitheliasin
Eur J Biochem (2001) 268, 2687-2699. PubMed Europe PubMed DOI
Vaarala,M.H., Porvari,K.S., Kellokumpu,S., Kyllonen,A.P. and Vihko,P.T.
Expression of transmembrane serine protease TMPRSS2 in mouse and human tissues
J Pathol (2001) 193, 134-140. PubMed Europe PubMed DOI
[YEAR:1-12-2001]Vaarala,M.H., Porvari,K., Kyllonen,A., Lukkarinen,O. and Vihko,P.
The TMPRSS2 gene encoding transmembrane serine protease is overexpressed in a majority of prostate cancer patients: Detection of mutated TMPRSS2 form in a case of aggressive disease
Int J Cancer (1-12-2001) 94, 705-710. PubMed Europe PubMed DOI

2000

[YEAR:18-2-2000]Jacquinet,E., Rao,N.V., Rao,G.V. and Hoidal,J.R.
Cloning, genomic organization, chromosomal assignment and expression of a novel mosaic serine proteinase: epitheliasin
FEBS Lett (18-2-2000) 468, 93-100. PubMed Europe PubMed DOI

1999

[YEAR:1-9-1999]Lin,B., Ferguson,C., White,J.T., Wang,S., Vessella,R., True,L.D., Hood,L. and Nelson,P.S.
Prostate-localized and androgen-regulated expression of the membrane-bound serine protease TMPRSS2
Cancer Res (1-9-1999) 59, 4180-4184. PubMed Europe PubMed

1997

Paoloni-Giacobino,A., Chen,H., Peitsch,M.C., Rossier,C. and Antonarakis,S.E.
Cloning of the TMPRSS2 gene, which encodes a novel serine protease with transmembrane, LDLRA, and SRCR domains and maps to 21q22.3
Genomics (1997) 44, 309-320. PubMed Europe PubMed DOI