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Literature for peptidase S08.012: PfSUB1 peptidase

Summary Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates

(Topics flags: A Assay, S Structure, T Target, K Knockout, I Inhibitor, E Expression, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)

    2025
  1. Puszko,A.K., Batista,F.A., Ejjoummany,A., Bouillon,A., Maurel,M., Adler,P., Legru,A., Martinez,M., Ortega Varga,L., Hadjadj,M., Alzari,P.M., Blondel,A., Haouz,A., Barale,J.C. and Hernandez,J.F.
    Towards Improved Peptidic alpha-Ketoamide Inhibitors of the Plasmodial Subtilisin-Like SUB1: Exploration of N-Terminal Extensions and Cyclic Constraints
    ChemMedChem (2025) , e202400924-e202400924. PubMed  Europe PubMed DOI
    2. 2024
  2. Legru,A., Batista,F.A., Puszko,A.K., Bouillon,A., Maurel,M., Martinez,M., Ejjoummany,A., Ortega Varga,L., Adler,P., Mechaly,A., Hadjadj,M., Sosnowski,P., Hopfgartner,G., Alzari,P.M., Blondel,A., Haouz,A., Barale,J.C. and Hernandez,J.F.
    Insights from structure-activity relationships and the binding mode of peptidic alpha-ketoamide inhibitors of the malaria drug target subtilisin-like SUB1
    Eur J Med Chem (2024) 269, 116308-116308. PubMed  Europe PubMed DOI  I
  3. Martinez,M., Bouillon,A., Brule,S., Raynal,B., Haouz,A., Alzari,P.M. and Barale,J.C.
    Prodomain-driven enzyme dimerization: a pH-dependent autoinhibition mechanism that controls Plasmodium Sub1 activity before merozoite egress
    MBio (2024) 15, e0019824-e0019824. PubMed  Europe PubMed DOI  PMC  EPMC
  4. Withers-Martinez,C., George,R., Maslen,S., Jean,L., Hackett,F., Skehel,M. and Blackman,M.J.
    The malaria parasite egress protease SUB1 is activated through precise, plasmepsin X-mediated cleavage of the SUB1 prodomain
    Biochim Biophys Acta Gen Subj (2024) 1868, 130665-130665. PubMed  Europe PubMed DOI
    5. 2023
  5. Martinez,M., Batista,F.A., Maurel,M., Bouillon,A., Ortega Varga,L., Wehenkel,A.M., Le Chevalier-Sontag,L., Blondel,A., Haouz,A., Hernandez,J.F., Alzari,P.M. and Barale,J.C.
    3D structures of the Plasmodium vivax subtilisin-like drug target SUB1 reveal conformational changes to accommodate a substrate-derived alpha-ketoamide inhibitor
    Acta Crystallogr D Struct Biol (2023) 79, 721-734. PubMed  Europe PubMed DOI  I
  6. Mukherjee,S., Nasamu,A.S., Rubiano,K. and Goldberg,D.E.
    Activation of the Plasmodium egress effector subtilisin-like protease 1 is achieved by plasmepsin X destruction of the propiece
    bioRxiv (2023) PubMed  Europe PubMed DOI  PMC  EPMC  K
    7. 2022
  7. Lidumniece,E., Withers-Martinez,C., Hackett,F., Blackman,M.J. and Jirgensons,A.
    Subtilisin-like Serine Protease 1 (SUB1) as an Emerging Antimalarial Drug Target: Current Achievements in Inhibitor Discovery
    J Med Chem (2022) 65, 12535-12545. PubMed  Europe PubMed DOI
    8. 2021
  8. Lidumniece,E., Withers-Martinez,C., Hackett,F., Collins,C.R., Perrin,A.J., Koussis,K., Bisson,C., Blackman,M.J. and Jirgensons,A.
    Peptidic boronic acids are potent cell-permeable inhibitors of the malaria parasite egress serine protease SUB1
    Proc Natl Acad Sci U S A (2021) 118 PubMed  Europe PubMed DOI  PMC  EPMC  I
    9. 2020
  9. Burrows,J.N. and Soldati-Favre,D.
    Targeting plasmepsins - an Achilles' Heel of the malaria parasite
    Cell Host Microbe (2020) 27, 496-498. PubMed  Europe PubMed DOI  I
  10. Fierro,M.A., Asady,B., Brooks,C.F., Cobb,D.W., Villegas,A., Moreno,S.N.J. and Muralidharan,V.
    An endoplasmic reticulum CREC family protein regulates the egress proteolytic cascade in malaria parasites
    MBio (2020) 11 PubMed  Europe PubMed DOI
  11. Tarr,S.J., Withers-Martinez,C., Flynn,H.R., Snijders,A.P., Masino,L., Koussis,K., Conway,D.J. and Blackman,M.J.
    A malaria parasite subtilisin propeptide-like protein is a potent inhibitor of the egress protease SUB1
    Biochem J (2020) 477, 525-540. PubMed  Europe PubMed DOI
    12. 2019
  12. Pace,T., Grasso,F., Camarda,G., Suarez,C., Blackman,M.J., Ponzi,M. and Olivieri,A.
    The Plasmodium berghei serine protease PbSUB1 plays an important role in male gamete egress
    Cell Microbiol (2019) , e13028-e13028. PubMed  Europe PubMed DOI
  13. Zogota,R., Kinena,L., Withers-Martinez,C., Blackman,M.J., Bobrovs,R., Pantelejevs,T., Kanepe-Lapsa,I., Ozola,V., Jaudzems,K., Suna,E. and Jirgensons,A.
    Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
    Eur J Med Chem (2019) 163, 344-352. PubMed  Europe PubMed DOI
    14. 2018
  14. Thomas,J.A., Tan,M.S.Y., Bisson,C., Borg,A., Umrekar,T.R., Hackett,F., Hale,V.L., Vizcay-Barrena,G., Fleck,R.A., Snijders,A.P., Saibil,H.R. and Blackman,M.J.
    A protease cascade regulates release of the human malaria parasite Plasmodium falciparum from host red blood cells
    Nat Microbiol (2018) 3, 447-455. PubMed  Europe PubMed DOI
    15. 2017
  15. Collins,C.R., Hackett,F., Atid,J., Tan,M.S.Y. and Blackman,M.J.
    The Plasmodium falciparum pseudoprotease SERA5 regulates the kinetics and efficiency of malaria parasite egress from host erythrocytes
    PLoS Pathog (2017) 13, e1006453-e1006453. PubMed  Europe PubMed DOI  PMC  EPMC
    16. 2016
  16. Brogi,S., Giovani,S., Brindisi,M., Gemma,S., Novellino,E., Campiani,G., Blackman,M.J. and Butini,S.
    In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors
    J Mol Graph Model (2016) 64, 121-130. PubMed  Europe PubMed DOI  I
  17. Subathra Devi,C., Verma,P., Srivastava,S., Ravikumar,P., Kalwani,V., Tandon,A. and Mohanasrinivasan,V.
    Development of a novel malarial vaccine design: a hypothetical approach
    Curr Drug Discov Technol (2016) 11, 239-242. PubMed  Europe PubMed  I
    18. 2015
  18. Das,S., Hertrich,N., Perrin,A.J., Withers-Martinez,C., Collins,C.R., Jones,M.L., Watermeyer,J.M., Fobes,E.T., Martin,S.R., Saibil,H.R., Wright,G.J., Treeck,M., Epp,C. and Blackman,M.J.
    Processing of Plasmodium falciparum merozoite surface protein MSP1 activates a spectrin-binding function enabling parasite egress from RBCs
    Cell Host Microbe (2015) 18, 433-444. PubMed  Europe PubMed DOI
  19. Giovani,S., Penzo,M., Butini,S., Brindisi,M., Gemma,S., Novellino,E., Campiani,G., Blackman,M.J. and Brogi,S.
    Plasmodium falciparum subtilisin-like protease 1: discovery of potent difluorostatone-based inhibitors
    Chem Soc Rev (2015) 5, 22431-22448. DOI  I
  20. Kher,S.S., Penzo,M., Fulle,S., Ebejer,J.P., Finn,P.W., Blackman,M.J. and Jirgensons,A.
    Quinoxaline-based inhibitors of malarial protease PfSUB1
    Chem Heterocycl Compd (2015) 50, 1457-1463. DOI  I
    21. 2014
  21. Alam,A.
    Serine proteases of malaria parasite Plasmodium falciparum: potential as antimalarial drug targets
    Interdiscip Perspect Infect Dis (2014) 2014, 453186-453186. PubMed  Europe PubMed DOI  PMC  EPMC  V
  22. Bastianelli,G., Bouillon,A., Nguyen,C., Le-Nguyen,D., Nilges,M. and Barale,J.C.
    Computational design of protein-based inhibitors of Plasmodium vivax subtilisin-like 1 protease
    PLoS ONE (2014) 9, e109269-e109269. PubMed  Europe PubMed DOI  PMC  EPMC
  23. Giganti,D., Bouillon,A., Tawk,L., Robert,F., Martinez,M., Crublet,E., Weber,P., Girard-Blanc,C., Petres,S., Haouz,A., Hernandez,J.F., Mercereau-Puijalon,O., Alzari,P.M. and Barale,J.C.
    A novel Plasmodium-specific prodomain fold regulates the malaria drug target SUB1 subtilase
    Nat Commun (2014) 5, 4833-4833. PubMed  Europe PubMed DOI  S
  24. Giovani,S., Penzo,M., Brogi,S., Brindisi,M., Gemma,S., Novellino,E., Savini,L., Blackman,M.J., Campiani,G. and Butini,S.
    Rational design of the first difluorostatone-based PfSUB1 inhibitors
    Bioorg Med Chem Lett (2014) 24, 3582-3586. PubMed  Europe PubMed DOI  I
  25. Kher,S.S., Penzo,M., Fulle,S., Finn,P.W., Blackman,M.J. and Jirgensons,A.
    Substrate derived peptidic alpha-ketoamides as inhibitors of the malarial protease PfSUB1
    Bioorg Med Chem Lett (2014) 24, 4486-4489. PubMed  Europe PubMed DOI  I
  26. Withers-Martinez,C., Strath,M., Hackett,F., Haire,L.F., Howell,S.A., Walker,P.A., Christodoulou,E., Evangelos,C., Dodson,G.G. and Blackman,M.J.
    The malaria parasite egress protease SUB1 is a calcium-dependent redox switch subtilisin
    Nat Commun (2014) 5, 3726-3726. PubMed  Europe PubMed DOI  S
    27. 2013
  27. Agarwal,S., Singh,M.K., Garg,S., Chitnis,C.E. and Singh,S.
    Ca(2+)-mediated exocytosis of subtilisin-like protease 1: a key step in egress of Plasmodium falciparum merozoites
    Cell Microbiol (2013) 15, 910-921. PubMed  Europe PubMed DOI
  28. Bouillon,A., Giganti,D., Benedet,C., Gorgette,O., Petres,S., Crublet,E., Girard-Blanc,C., Witkowski,B., Menard,D., Nilges,M., Mercereau-Puijalon,O., Stoven,V. and Barale,J.C.
    In silico screening on the three-dimensional model of the Plasmodium vivax SUB1 protease leads to the validation of a novel anti-parasite compound
    J Biol Chem (2013) 288, 18561-18573. PubMed  Europe PubMed DOI  I
  29. Collins,C.R., Hackett,F., Strath,M., Penzo,M., Withers-Martinez,C., Baker,D.A. and Blackman,M.J.
    Malaria parasite cGMP-dependent protein kinase regulates blood stage merozoite secretory organelle discharge and egress
    PLoS Pathog (2013) 9, e1003344-e1003344. PubMed  Europe PubMed DOI  PMC  EPMC
  30. Fulle,S., Withers-Martinez,C., Blackman,M.J., Morris,G.M. and Finn,P.W.
    Molecular determinants of binding to the Plasmodium subtilisin-like protease 1
    J Chem Inf Model (2013) 53, 573-583. PubMed  Europe PubMed DOI
  31. Suarez,C., Volkmann,K., Gomes,A.R., Billker,O. and Blackman,M.J.
    The malarial serine protease SUB1 plays an essential role in parasite liver stage development
    PLoS Pathog (2013) 9, e1003811-e1003811. PubMed  Europe PubMed DOI  PMC  EPMC
  32. Tawk,L., Lacroix,C., Gueirard,P., Kent,R., Gorgette,O., Thiberge,S., Mercereau-Puijalon,O., Menard,R. and Barale,J.C.
    A key role for Plasmodium subtilisin-like SUB1 protease in egress of malaria parasites from host hepatocytes
    J Biol Chem (2013) 288, 33336-33346. PubMed  Europe PubMed DOI
    33. 2012
  33. Gemma,S., Giovani,S., Brindisi,M., Tripaldi,P., Brogi,S., Savini,L., Fiorini,I., Novellino,E., Butini,S., Campiani,G., Penzo,M. and Blackman,M.J.
    Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1
    Bioorg Med Chem Lett (2012) 22, 5317-5321. PubMed  Europe PubMed DOI  I
  34. Ruecker,A., Shea,M., Hackett,F., Suarez,C., Hirst,E.M., Milutinovic,K., Withers-Martinez,C. and Blackman,M.J.
    Proteolytic activation of the essential parasitophorous vacuole cysteine protease SERA6 accompanies malaria parasite egress from its host erythrocyte
    J Biol Chem (2012) 287, 37949-37963. PubMed  Europe PubMed DOI
  35. Silmon de Monerri,N.C., Ruecker,A. and Blackman,M.J.
    Plasmodium subtilisins
    [ISSN:978-0-12-407742-3] (2012) 3, 3260-3265. DOI
  36. Withers-Martinez,C., Suarez,C., Fulle,S., Kher,S., Penzo,M., Ebejer,J.P., Koussis,K., Hackett,F., Jirgensons,A., Finn,P. and Blackman,M.J.
    Plasmodium subtilisin-like protease 1 (SUB1): insights into the active-site structure, specificity and function of a pan-malaria drug target
    Int J Parasitol (2012) 42, 597-612. PubMed  Europe PubMed DOI  I
    37. 2011
  37. Bastianelli,G., Bouillon,A., Nguyen,C., Crublet,E., Petres,S., Gorgette,O., Le-Nguyen,D., Barale,J.C. and Nilges,M.
    Computational reverse-engineering of a spider-venom derived peptide active against Plasmodium falciparum SUB1
    PLoS ONE (2011) 6, e21812-e21812. PubMed  Europe PubMed DOI  PMC  EPMC  I
  38. Moneriz,C., Mestres,J., Bautista,J.M., Diez,A. and Puyet,A.
    Multi-targeted activity of maslinic acid as an antimalarial natural compound
    FEBS J (2011) 278, 2951-2961. PubMed  Europe PubMed DOI  I
  39. Silmon de Monerri,N.C., Flynn,H.R., Campos,M.G., Hackett,F., Koussis,K., Withers-Martinez,C., Skehel,J.M. and Blackman,M.J.
    Global identification of multiple substrates for Plasmodium falciparum SUB1, an essential malarial processing protease
    Infect Immun (2011) 79, 1086-1097. PubMed  Europe PubMed DOI
    40. 2010
  40. Child,M.A., Epp,C., Bujard,H. and Blackman,M.J.
    Regulated maturation of malaria merozoite surface protein-1 is essential for parasite growth
    Mol Microbiol (2010) 78, 187-202. PubMed  Europe PubMed DOI
    41. 2009
  41. Koussis,K., Withers-Martinez,C., Yeoh,S., Child,M., Hackett,F., Knuepfer,E., Juliano,L., Woehlbier,U., Bujard,H. and Blackman,M.J.
    A multifunctional serine protease primes the malaria parasite for red blood cell invasion
    EMBO J (2009) 28, 725-735. PubMed  Europe PubMed DOI  PMC  EPMC
    42. 2008
  42. Arastu-Kapur,S., Ponder,E.L., Fonovic,U.P., Yeoh,S., Yuan,F., Fonovic,M., Grainger,M., Phillips,C.I., Powers,J.C. and Bogyo,M.
    Identification of proteases that regulate erythrocyte rupture by the malaria parasite Plasmodium falciparum
    Nat Chem Biol (2008) 4, 203-213. PubMed  Europe PubMed DOI  I
  43. Blackman,M.J.
    Malarial proteases and host cell egress: an 'emerging' cascade
    Cell Microbiol (2008) 10, 1925-1934. PubMed  Europe PubMed DOI  PMC  EPMC  T
    44. 2007
  44. Janse,C.J. and Waters,A.P.
    The exoneme helps malaria parasites to break out of blood cells
    Cell (2007) 131, 1036-1038. PubMed  Europe PubMed DOI
  45. Yeoh,S., O'Donnell,R.A., Koussis,K., Dluzewski,A.R., Ansell,K.H., Osborne,S.A., Hackett,F., Withers-Martinez,C., Mitchell,G.H., Bannister,L.H., Bryans,J.S., Kettleborough,C.A. and Blackman,M.J.
    Subcellular discharge of a serine protease mediates release of invasive malaria parasites from host erythrocytes
    Cell (2007) 131, 1072-1083. PubMed  Europe PubMed DOI
    46. 2005
  46. [YEAR:22-9-2005]Jean,L., Withers-Martinez,C., Hackett,F. and Blackman,M.J.
    Unique insertions within Plasmodium falciparum subtilisin-like protease-1 are crucial for enzyme maturation and activity
    Mol Biochem Parasitol (22-9-2005) 144, 187-197. PubMed  Europe PubMed DOI
    47. 2004
  47. Blackman,M.J.
    Plasmodium subtilisins
    [ISSN:0-12-079610-4] (2004) 2, 1841-1844.  V
  48. Withers-Martinez,C., Jean,L. and Blackman,M.J.
    Subtilisin-like proteases of the malaria parasite
    Mol Microbiol (2004) 53, 55-63. PubMed  Europe PubMed DOI
    49. 2003
  49. [YEAR:1-8-2003]Jean,L., Hackett,F., Martin,S.R. and Blackman,M.J.
    Functional characterization of the propeptide of Plasmodium falciparum subtilisin-like protease-1
    J Biol Chem (1-8-2003) 278, 28572-28579. PubMed  Europe PubMed DOI
    50. 2002
  50. [YEAR:8-10-2002]Blackman,M.J., Corrie,J.E., Croney,J.C., Kelly,G., Eccleston,J.F. and Jameson,D.M.
    Structural and biochemical characterization of a fluorogenic rhodamine-labeled malarial protease substrate
    Biochemistry (8-10-2002) 41, 12244-12252. PubMed  Europe PubMed DOI  A
  51. [YEAR:16-8-2002]Withers-Martinez,C., Saldanha,J.W., Ely,B., Hackett,F., O'Connor,T. and Blackman,M.J.
    Expression of recombinant Plasmodium falciparum subtilisin-like protease-1 in insect cells. Characterization, comparison with the parasite protease, and homology modeling
    J Biol Chem (16-8-2002) 277, 29698-29709. PubMed  Europe PubMed DOI  E
    52. 2000
  52. Blackman,M.J.
    Proteases involved in erythrocyte invasion by the malaria parasite: function and potential as chemotherapeutic targets
    Curr Drug Targets (2000) 1, 59-83. PubMed  Europe PubMed
  53. [YEAR:7-1-2000]Sajid,M., Withers-Martinez,C. and Blackman,M.J.
    Maturation and specificity of Plasmodium falciparum subtilisin-like protease-1, a malaria merozoite subtilisin-like serine protease
    J Biol Chem (7-1-2000) 275, 631-641. PubMed  Europe PubMed DOI
    54. 1999
  54. Withers-Martinez,C., Carpenter,E.P., Hackett,F., Ely,B., Sajid,M., Grainger,M. and Blackman,M.J.
    PCR-based gene synthesis as an efficient approach for expression of the A+T-rich malaria genome
    Protein Eng (1999) 12, 1113-1120. PubMed  Europe PubMed
    55. 1998
  55. [YEAR:4-9-1998]Blackman,M.J., Fujioka,H., Stafford,W.H., Sajid,M., Clough,B., Fleck,S.L., Aikawa,M., Grainger,M. and Hackett,F.
    A subtilisin-like protein in secretory organelles of Plasmodium falciparum merozoites
    J Biol Chem (4-9-1998) 273, 23398-23409. PubMed  Europe PubMed DOI
    56. 1993
  56. Blackman,M.J., Chappel,J.A., Shai,S. and Holder,A.A.
    A conserved parasite serine protease processes the Plasmodium falciparum merozoite surface protein-1
    Mol Biochem Parasitol (1993) 62, 103-114. PubMed  Europe PubMed DOI

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