Literature for peptidase C01.034: cathepsin S

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(References are filtered for relevance to Inhibitor. To remove the filter click here. See explanation.)

2025

Bentley,D., Mannino,M., Manchester,M., Teixeira,P.C., Reis,B., Boyce,M. and Nagel,S. A randomized, double-blind, placebo-controlled, multiple dose, parallel study to investigate the effects of a cathepsin S inhibitor in celiac disease Clin Transl Sci (2025) 18, e13901-e13901. PubMed Europe PubMed DOI PMC EPMC I
Previti,S., Iraci,N., Calcaterra,E., Ettari,R. and Zappala,M. A Second Opportunity for the Peptide-Based Analogues with gamma-Lactam at the P1 Position: Human Cathepsin S Inhibition Pharmaceuticals (Basel) (2025) 18 PubMed Europe PubMed DOI PMC EPMC I
Yang,C., Fu,L., Li,R., Tang,H., Chen,Z., Gan,S., Sun,J., Li,S., Li,J. and Yao,L. Cathepsin S mediates the disruption of airway epithelial Pannexin 1 via an Akt-dependent pathway in an LPS-induced murine model of acute lung injury Exp Cell Res (2025) 450, 114663-114663. PubMed Europe PubMed DOI I

2024

Zhang,Y., Yang,L., Gan,Y., Zhao,C., Zhou,C., Chen,J., Yin,Y., Xia,S., Yang,H., Bao,X., Zhang,M., Xu,Y. and Li,J. Benzydamine attenuates microglia-mediated neuroinflammation and ischemic brain injury by targeting cathepsin s Int Immunopharmacol (2024) 146, 113824-113824. PubMed Europe PubMed DOI I

2023

Abdoli,M., Krasniqi,V., Bonardi,A., Gutschow,M., Supuran,C.T. and Zalubovskis,R. 4-Cyanamido-substituted benzenesulfonamides act as dual carbonic anhydrase and cathepsin inhibitors Bioorg Chem (2023) 139, 106725-106725. PubMed Europe PubMed DOI I
Fuchs,N., Meta,M., Lantzberg,B., Bros,M., Ling Kuan,S., Weil,T. and Schirmeister,T. Subnanomolar Cathepsin S Inhibitors with High Selectivity: Optimizing Covalent Reversible alpha-Fluorovinylsulfones and alpha-Sulfonates as Potential Immunomodulators in Cancer ChemMedChem (2023) 18, e202300160-e202300160. PubMed Europe PubMed DOI I
Huang,H., Zhang,Y., Xu,X., Liu,Y., Zhao,J., Ma,L., Lei,J., Ge,W., Li,N., Ma,E., Li,Y. and Yuan,L. Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells Bioorg Med Chem Lett (2023) 80, 129087-129087. PubMed Europe PubMed DOI I

2021

Oldak,L., Sankiewicz,A., Zelazowska-Rutkowska,B., Cylwik,B., Lukaszewski,Z., Skoczylas,M. and Gorodkiewicz,E. Two SPRi biosensors for the determination of cathepsin S in blood plasma Talanta (2021) 225, 121900-121900. PubMed Europe PubMed DOI I

2020

Ahmad,S., Bhagwati,S., Kumar,S., Banerjee,D. and Siddiqi,M.I. Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors J Mol Graph Model (2020) 96, 107512-107512. PubMed Europe PubMed DOI I
Cianni,L., Rocho,F.D.R., Rosini,F., Bonatto,V., Ribeiro,J.F.R., Lameira,J., Leitao,A., Shamim,A. and Montanari,C.A. Optimization strategy of single-digit nanomolar cross-class inhibitors of mammalian and protozoa cysteine proteases Bioorg Chem (2020) 101, 104039-104039. PubMed Europe PubMed DOI I
Lai,C.H., Chang,J.Y., Wang,K.C., Lee,F.T., Wu,H.L. and Cheng,T.L. Pharmacological inhibition of cathepsin S suppresses abdominal aortic aneurysm in mice Eur J Vasc Endovasc Surg (2020) PubMed Europe PubMed DOI U I
Lemke,C., Cianni,L., Feldmann,C., Gilberg,E., Yin,J., Dos Reis Rocho,F., De Vita,D., Bartz,U., Bajorath,J., Montanari,C.A. and Gutschow,M. N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization Bioorg Med Chem Lett (2020) 30, 127420-127420. PubMed Europe PubMed DOI I
van Dalen,F.J., Bakkum,T., Van Leeuwen,T., Groenewold,M., Deu,E., Koster,A.J., van Kasteren,S.I. and Verdoes,M. Application of a Highly Selective Cathepsin S Two-step Activity-Based Probe in Multicolor Bio-Orthogonal Correlative Light-Electron Microscopy Front Chem (2020) 8, 628433-628433. PubMed Europe PubMed DOI PMC EPMC I

2019

Chaput,L., Selwa,E., Elisee,E. and Iorga,B.I. Blinded evaluation of cathepsin S inhibitors from the D3RGC3 dataset using molecular docking and free energy calculations J Comput Aided Mol Des (2019) 33, 93-103. PubMed Europe PubMed DOI I
He,X., Man,V.H., Ji,B., Xie,X.Q. and Wang,J. Calculate protein-ligand binding affinities with the extended linear interaction energy method: application on the cathepsin S set in the D3R Grand Challenge 3 J Comput Aided Mol Des (2019) 33, 105-117. PubMed Europe PubMed DOI I
Klinngam,W., Janga,S.R., Lee,C., Ju,Y., Yarber,F., Shah,M., Guo,H., Wang,D., MacKay,J.A., Edman,M.C. and Hamm-Alvarez,S.F. Inhibition of cathepsin S reduces lacrimal gland inflammation and increases tear flow in a mouse model of Sjogren's syndrome Sci Rep (2019) 9, 9559-9559. PubMed Europe PubMed DOI I
Shockey,W.A., Kieslich,C.A., Wilder,C.L., Watson,V. and Platt,M.O. Dynamic model of protease state and inhibitor trafficking to predict protease activity in breast cancer cells Cell Mol Bioeng (2019) 12, 275-288. PubMed Europe PubMed DOI PMC EPMC I
Small,D.M., Brown,R.R., Doherty,D.F., Abladey,A., Zhou-Suckow,Z., Delaney,R.J., Kerrigan,L., Dougan,C.M., Borensztajn,K.S., Holsinger,L., Booth,R., Scott,C.J., Lopez-Campos,G., Elborn,J.S., Mall,M.A., Weldon,S. and Taggart,C.C. Targeting of cathepsin S reduces cystic fibrosis-like lung disease Eur Respir J (2019) 53, 1801523-1801523. PubMed Europe PubMed DOI K I

2018

Chen,C.Y., Chen,C.Y., Liu,C.C. and Chen,C.P. Omega-3 polyunsaturated fatty acids reduce preterm labor by inhibiting trophoblast cathepsin S and inflammasome activation Clin Sci (Lond) (2018) 132, 2221-2239. PubMed Europe PubMed DOI I
Kubo,K., Kawato,Y., Nakamura,K., Nakajima,Y., Nakagawa,T.Y., Hanaoka,K., Oshima,S., Fukahori,H., Inami,M., Morokata,T. and Higashi,Y. Effective suppression of donor specific antibody production by cathepsin S inhibitors in a mouse transplantation model Eur J Pharmacol (2018) 838, 145-152. PubMed Europe PubMed DOI I
Tber,Z., Wartenberg,M., Jacques,J.E., Roy,V., Lecaille,F., Warszycki,D., Bojarski,A.J., Lalmanach,G. and Agrofoglio,L.A. Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs Bioorg Med Chem (2018) 26, 4310-4319. PubMed Europe PubMed DOI I
Yuan,L., Sheng,L., He,W., Zou,C., Hu,B., Liu,J., Ge,W., Liu,Y., Wang,J. and Ma,E. Discovery of novel cathepsin inhibitors with potent anti-metastatic effects in breast cancer cells Bioorg Chem (2018) 81, 672-680. PubMed Europe PubMed DOI I

2017

Ahmad,S. and Siddiqi,M.I. Insights from molecular modeling into the selective inhibition of cathepsin S by its inhibitor J Mol Model (2017) 23, 92-92. PubMed Europe PubMed DOI I
Galibert,M., Wartenberg,M., Lecaille,F., Saidi,A., Mavel,S., Joulin-Giet,A., Korkmaz,B., Bromme,D., Aucagne,V., Delmas,A.F. and Lalmanach,G. Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S Eur J Med Chem (2017) 144, 201-210. PubMed Europe PubMed DOI I
Hsieh,M.J., Lin,C.W., Chen,M.K., Chien,S.Y., Lo,Y.S., Chuang,Y.C., Hsi,Y.T., Lin,C.C., Chen,J.C. and Yang,S.F. Inhibition of cathepsin S confers sensitivity to methyl protodioscin in oral cancer cells via activation of p38 MAPK/JNK signaling pathways Sci Rep (2017) 7, 45039-45039. PubMed Europe PubMed DOI I
Tato,M., Kumar,S.V., Liu,Y., Mulay,S.R., Moll,S., Popper,B., Eberhard,J.N., Thomasova,D., Rufer,A.C., Gruner,S., Haap,W., Hartmann,G. and Anders,H.J. Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury Sci Rep (2017) 7, 2775-2775. PubMed Europe PubMed DOI PMC EPMC I
Thanei,S., Theron,M., Silva,A.P., Reis,B., Branco,L., Schirmbeck,L., Kolb,F.A., Haap,W., Schindler,T. and Trendelenburg,M. Cathepsin S inhibition suppresses autoimmune-triggered inflammatory responses in macrophages Biochem Pharmacol (2017) 146, 151-164. PubMed Europe PubMed DOI I
Yan,X., Wu,C., Chen,T., Santos,M.M., Liu,C.L., Yang,C., Zhang,L., Ren,J., Liao,S., Guo,H., Sukhova,G.K. and Shi,G.P. Cathepsin S inhibition changes regulatory T-cell activity in regulating bladder cancer and immune cell proliferation and apoptosis Mol Immunol (2017) 82, 66-74. PubMed Europe PubMed DOI I

2016

Hewitt,E., Pitcher,T., Rizoska,B., Tunblad,K., Henderson,I., Sahlberg,B.L., Grabowska,U., Classon,B., Edenius,C., Malcangio,M. and Lindstrom,E. Selective cathepsin S inhibition with MIV-247 attenuates mechanical allodynia and enhances the antiallodynic effects of gabapentin and pregabalin in a mouse model of neuropathic pain J Pharmacol Exp Ther (2016) 358, 387-396. PubMed Europe PubMed DOI I
Huang,C.C., Lee,C.C., Lin,H.H. and Chang,J.Y. Cathepsin S attenuates endosomal EGFR signalling: a mechanical rationale for the combination of cathepsin S and EGFR tyrosine kinase inhibitors Sci Rep (2016) 6, 29256-29256. PubMed Europe PubMed DOI PMC EPMC I
Ihmaid,S.K., Ahmed,H.E., Zayed,M.F. and Abadleh,M.M. Self organizing map-based classification of cathepsin K and S inhibitors with different selectivity profiles using different structural molecular fingerprints: design and application for discovery of novel hits Molecules (2016) 21, 175-175. PubMed Europe PubMed DOI I
Plebanek,E., Chevrier,F., Roy,V., Garenne,T., Lecaille,F., Warszycki,D., Bojarski,A.J., Lalmanach,G. and Agrofoglio,L.A. Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S Eur J Med Chem (2016) 121, 12-20. PubMed Europe PubMed DOI I
Wilkinson,R.D., Young,A., Burden,R.E., Williams,R. and Scott,C.J. A bioavailable cathepsin S nitrile inhibitor abrogates tumor development Mol Cancer (2016) 15, 29-29. PubMed Europe PubMed DOI PMC EPMC I

2015

Barlow,N., Nasser,Y., Zhao,P., Sharma,N., Guerrero-Alba,R., Edgington-Mitchell,L.E., Lieu,T., Veldhuis,N.A., Poole,D.P., Conner,J.W., Lindstrom,E., Craig,A.W., Graham,B., Vanner,S.J. and Bunnett,N.W. Demonstration of elevated levels of active cathepsin S in dextran sulfate sodium colitis using a new activatable probe Neurogastroenterol Motil (2015) 27, 1675-1680. PubMed Europe PubMed DOI L I
Figueiredo,J.L., Aikawa,M., Zheng,C., Aaron,J., Lax,L., Libby,P., de Lima Filho,J.L., Gruener,S., Fingerle,J., Haap,W., Hartmann,G. and Aikawa,E. Selective cathepsin S inhibition attenuates atherosclerosis in apolipoprotein E-deficient mice with chronic renal disease Am J Pathol (2015) 185, 1156-1166. PubMed Europe PubMed DOI I
Kohl,F., Schmitz,J., Furtmann,N., Schulz-Fincke,A.C., Mertens,M.D., Kuppers,J., Benkhoff,M., Tobiasch,E., Bartz,U., Bajorath,J., Stirnberg,M. and Gutschow,M. Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors Org Biomol Chem (2015) 13, 10310-10323. PubMed Europe PubMed DOI I
Rupanagudi,K.V., Kulkarni,O.P., Lichtnekert,J., Darisipudi,M.N., Mulay,S.R., Schott,B., Gruner,S., Haap,W., Hartmann,G. and Anders,H.J. Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming Ann Rheum Dis (2015) 74, 452-463. PubMed Europe PubMed DOI I

2014

Battu,M.B., Chandra,A.M., Sriram,D. and Yogeeswari,P. Pharmacophore-based 3DQSAR and molecular docking studies to identify new non-peptidic inhibitors of cathepsin S Curr Med Chem (2014) 21, 1910-1921. PubMed Europe PubMed I
Bernard,N.J. Connective tissue diseases. Inhibiting cathepsin S to treat SLE and lupus nephritis Nat Rev Rheumatol (2014) 10, 66-66. PubMed Europe PubMed DOI I
Chua,K.C., Pietsch,M., Zhang,X., Hautmann,S., Chan,H.Y., Bruning,J.B., Gutschow,M. and Abell,A.D. Macrocyclic protease inhibitors with reduced peptide character Angew Chem Int Ed Engl (2014) 53, 7828-7831. PubMed Europe PubMed DOI I
Jadhav,P.K., Schiffler,M.A., Gavardinas,K., Kim,E.J., Matthews,D.P., Staszak,M.A., Coffey,D.S., Shaw,B.W., Cassidy,K.C., Brier,R.A., Zhang,Y., Christie,R.M., Matter,W.F., Qing,K., Durbin,J.D., Wang,Y. and Deng,G.G. Discovery of cathepsin S inhibitor LY3000328 for the treatment of abdominal aortic aneurysm ACS Med Chem Lett (2014) 5, 1138-1142. PubMed Europe PubMed DOI PMC EPMC I
Kim,M., Jeon,J., Baek,J., Choi,J., Park,E.J., Song,J., Bang,H., Suh,K.H., Kim,Y.H., Kim,J., Kim,D., Min,K.H. and Lee,K.-O. Synthesis of vinyl sulfone-tethered proline derivatives as highly selective cathepsin S inhibitors Bull Korean Chem Soc (2014) 35, 345-346. DOI I
Lafarge,J.C., Pini,M., Pelloux,V., Orasanu,G., Hartmann,G., Venteclef,N., Sulpice,T., Shi,G.P., Clement,K. and Guerre-Millo,M. Cathepsin S inhibition lowers blood glucose levels in mice Diabetologia (2014) 57, 1674-1683. PubMed Europe PubMed DOI I
Payne,C.D., Deeg,M.A., Chan,M., Tan,L.H., LaBell,E.S., Shen,T. and DeBrota,D.J. Pharmacokinetics and pharmacodynamics of the cathepsin S inhibitor, LY3000328, in healthy subjects Br J Clin Pharmacol (2014) 78, 1334-1342. PubMed Europe PubMed DOI I
Tsai,J.Y., Lee,M.J., Chang,M.D., Wang,H.C., Lin,C.C. and Huang,H. Effects of novel human cathepsin S inhibitors on cell migration in human cancer cells J Enzyme Inhib Med Chem (2014) 29, 538-546. PubMed Europe PubMed DOI I

2013

Feth,M.P., Heyse,W., Baumgartner,B., Nagel,N., Tappertzhofen,C., Olpp,T., Jurascheck,J., Ulrich,J., Helmdach,L. and Petzoldt,C. From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor Eur J Pharm Biopharm (2013) 83, 436-448. PubMed Europe PubMed DOI I
Hilpert,H., Mauser,H., Humm,R., Anselm,L., Kuehne,H., Hartmann,G., Gruener,S., Banner,D.W., Benz,J., Gsell,B., Kuglstatter,A., Stihle,M., Thoma,R., Sanchez,R.A., Iding,H., Wirz,B. and Haap,W. Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds J Med Chem (2013) 56, 9789-9801. PubMed Europe PubMed DOI I
Huang,C.C., Chen,K.L., Cheung,C.H. and Chang,J.Y. Autophagy induced by cathepsin S inhibition induces early ROS production, oxidative DNA damage, and cell death via xanthine oxidase Free Radic Biol Med (2013) 65, 1473-1486. PubMed Europe PubMed DOI I
Kim,M., Jeon,J., Song,J., Suh,K.H., Kim,Y.H., Min,K.H. and Lee,K.O. Synthesis of proline analogues as potent and selective cathepsin S inhibitors Bioorg Med Chem Lett (2013) 23, 3140-3144. PubMed Europe PubMed DOI I
Pehere,A.D., Pietsch,M., Gutschow,M., Neilsen,P.M., Pedersen,D.S., Nguyen,S., Zvarec,O., Sykes,M.J., Callen,D.F. and Abell,A.D. Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors Chemistry (2013) 19, 7975-7981. PubMed Europe PubMed DOI I
Wiener,J.J., Wickboldt,A.T., Nguyen,S., Sun,S., Rynberg,R., Rizzolio,M., Karlsson,L., Edwards,J.P. and Grice,C.A. Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region Bioorg Med Chem Lett (2013) 23, 1070-1074. PubMed Europe PubMed DOI I
Xu,J., Wang,H., Ding,K., Lu,X., Li,T., Wang,J., Wang,C. and Wang,J. Inhibition of cathepsin S produces neuroprotective effects after traumatic brain injury in mice Mediators Inflamm (2013) 2013, 187873-187873. PubMed Europe PubMed DOI PMC EPMC I

2012

Chen,K.L., Chang,W.S., Cheung,C.H., Lin,C.C., Huang,C.C., Yang,Y.N., Kuo,C.P., Kuo,C.C., Chang,Y.H., Liu,K.J., Wu,C.M. and Chang,J.Y. Targeting cathepsin S induces tumor cell autophagy via the EGFR-Erk signaling pathway Cancer Lett (2012) 317, 89-98. PubMed Europe PubMed DOI I
Frizler,M., Schmitz,J., Schulz-Fincke,A.C. and Gutschow,M. Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F J Med Chem (2012) 55, 5982-5986. PubMed Europe PubMed DOI I
Fujii,H., Ivison,S.M., Shimizu,H., Kajiwara,R., Kariminia,A., Yan,M., Dutz,J.P. and Schultz,K.R. Inhibition of cathepsin S reduces allogeneic T cell priming but not graft-versus-host disease against minor histocompatibility antigens Biol Blood Marrow Transplant (2012) 18, 546-556. PubMed Europe PubMed DOI I
Moss,N., Xiong,Z., Burke,M., Cogan,D., Gao,D.A., Haverty,K., Heim-Riether,A., Hickey,E.R., Nagaraja,R., Netherton,M., O'Shea,K., Ramsden,P., Schwartz,R., Shih,D.T., Ward,Y., Young,E. and Zhang,Q. Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement Bioorg Med Chem Lett (2012) 22, 7189-7193. PubMed Europe PubMed DOI I

2011

Baugh,M., Black,D., Westwood,P., Kinghorn,E., McGregor,K., Bruin,J., Hamilton,W., Dempster,M., Claxton,C., Cai,J., Bennett,J., Long,C., McKinnon,H., Vink,P., Hoed,L., Gorecka,M., Vora,K., Grant,E., Percival,M.D., Boots,A.M. and van Lierop,M.J. Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity J Autoimmun (2011) 36, 201-209. PubMed Europe PubMed DOI I
Deschamps,K., Cromlish,W., Weicker,S., Lamontagne,S., Huszar,S.L., Gauthier,J.Y., Mudgett,J.S., Guimond,A., Romand,R., Frossard,N., Percival,M.D., Slipetz,D. and Tan,C.M. Genetic and pharmacological evaluation of cathepsin S in a mouse model of asthma Am J Respir Cell Mol Biol (2011) 45, 81-87. PubMed Europe PubMed DOI K I
Jiang,C., Sun,W., Zhou,X.P. and Yang,X.H. Cathepsin S inhibitors and the structure-activity relationship: research advances J Int Pharm Res (2011) 38, 182-188. I
Kerns,J.K., Nie,H., Bondinell,W., Widdowson,K.L., Yamashita,D.S., Rahman,A., Podolin,P.L., Carpenter,D.C., Jin,Q., Riflade,B., Dong,X., Nevins,N., Keller,P.M., Mitchell,L. and Tomaszek,T. Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent Bioorg Med Chem Lett (2011) 21, 4409-4415. PubMed Europe PubMed DOI I
Lee-Dutra,A., Wiener,D.K. and Sun,S. Cathepsin S inhibitors: 2004 - 2010 Expert Opin Ther Pat (2011) 21, 311-337. PubMed Europe PubMed DOI V I
Loser,R. Cathepsin S inhibitors: WO2010070615 Expert Opin Ther Pat (2011) 21, 585-591. PubMed Europe PubMed DOI I
Veilleux,A., Black,W.C., Gauthier,J.Y., Mellon,C., Percival,M.D., Tawa,P. and Falgueyret,J.P. Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: cellular distribution in human leukocyte populations and evidence of diurnal modulation Anal Biochem (2011) 411, 43-49. PubMed Europe PubMed DOI I

2010

Ameriks,M.K., Bembenek,S.D., Burdett,M.T., Choong,I.C., Edwards,J.P., Gebauer,D., Gu,Y., Karlsson,L., Purkey,H.E., Staker,B.L., Sun,S., Thurmond,R.L. and Zhu,J. Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors Bioorg Med Chem Lett (2010) 20, 4060-4064. PubMed Europe PubMed DOI I
Cai,J., Robinson,J., Belshaw,S., Everett,K., Fradera,X., van Zeeland,M., van Berkom,L., van Rijnsbergen,P., Popplestone,L., Baugh,M., Dempster,M., Bruin,J., Hamilton,W., Kinghorn,E., Westwood,P., Kerr,J., Rankovic,Z., Arbuckle,W., Bennett,D.J., Jones,P.S., Long,C., Martin,I., Uitdehaag,J.C. and Meulemans,T. Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors Bioorg Med Chem Lett (2010) 20, 6890-6894. PubMed Europe PubMed DOI I
Cai,J., Baugh,M., Black,D., Long,C., Jonathan Bennett,D., Dempster,M., Fradera,X., Gillespie,J., Andrews,F., Boucharens,S., Bruin,J., Cameron,K.S., Cumming,I., Hamilton,W., Jones,P.S., Kaptein,A., Kinghorn,E., Maidment,M., Martin,I., Mitchell,A., Rankovic,Z., Robinson,J., Scullion,P., Uitdehaag,J.C., Vink,P., Westwood,P., van Zeeland,M., van Berkom,L., Bastiani,M. and Meulemans,T. 6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors Bioorg Med Chem Lett (2010) 20, 4350-4354. PubMed Europe PubMed DOI I
Cai,J., Bennett,D.J., Rankovic,Z., Dempster,M., Fradera,X., Gillespie,J., Cumming,I., Finlay,W., Baugh,M., Boucharens,S., Bruin,J., Cameron,K.S., Hamilton,W., Kerr,J., Kinghorn,E., McGarry,G., Robinson,J., Scullion,P., Uitdehaag,J.C., van Zeeland,M., Potin,D., Saniere,L., Fouquet,A., Chevallier,F., Deronzier,H., Dorleans,C. and Nicolai,E. 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors Bioorg Med Chem Lett (2010) 20, 4447-4450. PubMed Europe PubMed DOI I
Cai,J., Fradera,X., van Zeeland,M., Dempster,M., Cameron,K.S., Bennett,D.J., Robinson,J., Popplestone,L., Baugh,M., Westwood,P., Bruin,J., Hamilton,W., Kinghorn,E., Long,C. and Uitdehaag,J.C. 4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important Bioorg Med Chem Lett (2010) 20, 4507-4510. PubMed Europe PubMed DOI I
Chen,J.C., Uang,B.J., Lyu,P.C., Chang,J.Y., Liu,K.J., Kuo,C.C., Hsieh,H.P., Wang,H.C., Cheng,C.S., Chang,Y.H., Chang,M.D., Chang,W.S. and Lin,C.C. Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis J Med Chem (2010) 53, 4545-4549. PubMed Europe PubMed DOI I
Frizler,M., Stirnberg,M., Sisay,M.T. and Gutschow,M. Development of nitrile-based peptidic inhibitors of cysteine cathepsins Curr Top Med Chem (2010) 10, 294-322. PubMed Europe PubMed DOI T I
Isabel,E., Bateman,K.P., Chauret,N., Cromlish,W., Desmarais,S., Duong,l.T., Falgueyret,J.P., Gauthier,J.Y., Lamontagne,S., Lau,C.K., Leger,S., LeRiche,T., Levesque,J.F., Li,C.S., Masse,F., McKay,D.J., Mellon,C., Nicoll-Griffith,D.A., Oballa,R.M., Percival,M.D., Riendeau,D., Robichaud,J., Rodan,G.A., Rodan,S.B., Seto,C., Therien,M., Truong,V.L., Wesolowski,G., Young,R.N., Zamboni,R. and Black,W.C. The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor Bioorg Med Chem Lett (2010) 20, 887-892. PubMed Europe PubMed DOI I
Lee-Dutra,A., Wiener,D.K., Arienti,K.L., Liu,J., Mani,N., Ameriks,M.K., Axe,F.U., Gebauer,D., Desai,P.J., Nguyen,S., Randal,M., Thurmond,R.L., Sun,S., Karlsson,L., Edwards,J.P., Jones,T.K. and Grice,C.A. Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: Part 1 Bioorg Med Chem Lett (2010) 20, 2370-2374. PubMed Europe PubMed DOI I
Piovan,L., Alves,M.F.M., Juliano,L., Bromme,D., Cunha,R.L.O.R. and Andrade,L.H. Chemoenzymatic synthesis of organoselenium(IV) compounds and their evaluation as cysteine protease inhibitors J Braz Chem Soc (2010) 21, 2108-2118. I
Samokhin,A.O., Lythgo,P.A., Gauthier,J.Y., Percival,M.D. and Bromme,D. Pharmacological inhibition of cathepsin S decreases atherosclerotic lesions in Apoe-/- mice J Cardiovasc Pharmacol (2010) 56, 98-105. PubMed Europe PubMed DOI I
Wiener,D.K., Lee-Dutra,A., Bembenek,S., Nguyen,S., Thurmond,R.L., Sun,S., Karlsson,L., Grice,C.A., Jones,T.K. and Edwards,J.P. Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors Bioorg Med Chem Lett (2010) 20, 2379-2382. PubMed Europe PubMed DOI I
Wiener,J.J., Wickboldt,A.T., Jr., Wiener,D.K., Lee-Dutra,A., Edwards,J.P., Karlsson,L., Nguyen,S., Sun,S., Jones,T.K. and Grice,C.A. Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions Bioorg Med Chem Lett (2010) 20, 2375-2378. PubMed Europe PubMed DOI I
Wiener,J.J., Sun,S. and Thurmond,R.L. Recent advances in the design of cathepsin S inhibitors Curr Top Med Chem (2010) 10, 717-732. PubMed Europe PubMed DOI V I

2009

Ameriks,M.K., Axe,F.U., Bembenek,S.D., Edwards,J.P., Gu,Y., Karlsson,L., Randal,M., Sun,S., Thurmond,R.L. and Zhu,J. Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements Bioorg Med Chem Lett (2009) 19, 6131-6134. PubMed Europe PubMed DOI S I
Ameriks,M.K., Cai,H., Edwards,J.P., Gebauer,D., Gleason,E., Gu,Y., Karlsson,L., Nguyen,S., Sun,S., Thurmond,R.L. and Zhu,J. Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: Optimization of cellular potency Bioorg Med Chem Lett (2009) 19, 6135-6139. PubMed Europe PubMed DOI I
Ayesa,S., Lindquist,C., Agback,T., Benkestock,K., Classon,B., Henderson,I., Hewitt,E., Jansson,K., Kallin,A., Sheppard,D. and Samuelsson,B. Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity Bioorg Med Chem (2009) 17, 1307-1324. PubMed Europe PubMed DOI I
Bethel,P.A., Gerhardt,S., Jones,E.V., Kenny,P.W., Karoutchi,G.I., Morley,A.D., Oldham,K., Rankine,N., Augustin,M., Krapp,S., Simader,H. and Steinbacher,S. Design of selective cathepsin inhibitors Bioorg Med Chem Lett (2009) 19, 4622-4625. PubMed Europe PubMed DOI I
Clark,A.K., Yip,P.K. and Malcangio,M. The liberation of fractalkine in the dorsal horn requires microglial cathepsin S J Neurosci (2009) 29, 6945-6954. PubMed Europe PubMed DOI PMC EPMC I

2008

Irie,O., Ehara,T., Iwasaki,A., Yokokawa,F., Sakaki,J., Hirao,H., Kanazawa,T., Teno,N., Horiuchi,M., Umemura,I., Gunji,H., Masuya,K., Hitomi,Y., Iwasaki,G., Nonomura,K., Tanabe,K., Fukaya,H., Kosaka,T., Snell,C.R. and Hallett,A. Discovery of selective and nonpeptidic cathepsin S inhibitors Bioorg Med Chem Lett (2008) 18, 3959-3962. PubMed Europe PubMed DOI I
Irie,O., Yokokawa,F., Ehara,T., Iwasaki,A., Iwaki,Y., Hitomi,Y., Konishi,K., Kishida,M., Toyao,A., Masuya,K., Gunji,H., Sakaki,J., Iwasaki,G., Hirao,H., Kanazawa,T., Tanabe,K., Kosaka,T., Hart,T.W. and Hallett,A. 4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors Bioorg Med Chem Lett (2008) 18, 4642-4646. PubMed Europe PubMed DOI I
Irie,O., Kosaka,T., Ehara,T., Yokokawa,F., Kanazawa,T., Hirao,H., Iwasaki,A., Sakaki,J., Teno,N., Hitomi,Y., Iwasaki,G., Fukaya,H., Nonomura,K., Tanabe,K., Koizumi,S., Uchiyama,N., Bevan,S.J., Malcangio,M., Gentry,C., Fox,A.J., Yaqoob,M., Culshaw,A.J. and Allan,H. Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain J Med Chem (2008) 51, 5502-5505. PubMed Europe PubMed DOI I
Irie,O., Kosaka,T., Kishida,M., Sakaki,J., Masuya,K., Konishi,K., Yokokawa,F., Ehara,T., Iwasaki,A., Iwaki,Y., Hitomi,Y., Toyao,A., Gunji,H., Teno,N., Iwasaki,G., Hirao,H., Kanazawa,T., Tanabe,K., Hiestand,P.C., Malcangio,M., Fox,A.J., Bevan,S.J., Yaqoob,M., Culshaw,A.J., Hart,T.W. and Hallett,A. Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2 Bioorg Med Chem Lett (2008) 18, 5280-5284. PubMed Europe PubMed DOI I
Markt,P., McGoohan,C., Walker,B., Kirchmair,J., Feldmann,C., De Martino,G., Spitzer,G., Distinto,S., Schuster,D., Wolber,G., Laggner,C. and Langer,T. Discovery of novel cathepsin S inhibitors by pharmacophore-based virtual high-throughput screening J Chem Inf Model (2008) 48, 1693-1705. PubMed Europe PubMed DOI I

2007

Bekkali,Y., Thomson,D.S., Betageri,R., Emmanuel,M.J., Hao,M.H., Hickey,E., Liu,W., Patel,U., Ward,Y.D., Young,E.R., Nelson,R., Kukulka,A., Brown,M.L., Crane,K., White,D., Freeman,D.M., Labadia,M.E., Wildeson,J. and Spero,D.M. Identification of a novel class of succinyl-nitrile-based cathepsin S inhibitors Bioorg Med Chem Lett (2007) 17, 2465-2469. PubMed Europe PubMed DOI I
Chatterjee,A.K., Liu,H., Tully,D.C., Guo,J., Epple,R., Russo,R., Williams,J., Roberts,M., Tuntland,T., Chang,J., Gordon,P., Hollenbeck,T., Tumanut,C., Li,J. and Harris,J.L. Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S Bioorg Med Chem Lett (2007) 17, 2899-2903. PubMed Europe PubMed DOI I
Clark,A.K., Yip,P.K., Grist,J., Gentry,C., Staniland,A.A., Marchand,F., Dehvari,M., Wotherspoon,G., Winter,J., Ullah,J., Bevan,S. and Malcangio,M. Inhibition of spinal microglial cathepsin S for the reversal of neuropathic pain Proc Natl Acad Sci U S A (2007) 104, 10655-10660. PubMed Europe PubMed DOI PMC EPMC I
Gauthier,J.Y., Black,W.C., Courchesne,I., Cromlish,W., Desmarais,S., Houle,R., Lamontagne,S., Li,C.S., Masse,F., McKay,D.J., Ouellet,M., Robichaud,J., Truchon,J.F., Truong,V.L., Wang,Q. and Percival,M.D. The identification of potent, selective, and bioavailable cathepsin S inhibitors Bioorg Med Chem Lett (2007) 17, 4929-4933. PubMed Europe PubMed DOI I
Inagaki,H., Tsuruoka,H., Hornsby,M., Lesley,S.A., Spraggon,G. and Ellman,J.A. Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode J Med Chem (2007) 50, 2693-2699. PubMed Europe PubMed DOI I
Wei,J., Pio,B.A., Cai,H., Meduna,S.P., Sun,S., Gu,Y., Jiang,W., Thurmond,R.L., Karlsson,L. and Edwards,J.P. Pyrazole-based cathepsin S inhibitors with improved cellular potency Bioorg Med Chem Lett (2007) 17, 5525-5528. PubMed Europe PubMed DOI I

2006

[YEAR:10-1-2006]Alper,P.B., Liu,H., Chatterjee,A.K., Nguyen,K.T., Tully,D.C., Tumanut,C., Li,J., Harris,J.L., Tuntland,T., Chang,J., Gordon,P., Hollenbeck,T. and Karanewsky,D.S. Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl Bioorg Med Chem Lett (10-1-2006) 16, 1486-1490. PubMed Europe PubMed DOI I
[YEAR:28-3-2006]Desai,S.N., White,D.M., O'shea,K.M., Brown,M.L., Cywin,C.L., Spero,D.M. and Panzenbeck,M.J. An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity Eur J Pharmacol (28-3-2006) 538, 168-174. PubMed Europe PubMed DOI I
[YEAR:1-2-2006]Grice,C.A., Tays,K., Khatuya,H., Gustin,D.J., Butler,C.R., Wei,J., Sehon,C.A., Sun,S., Gu,Y., Jiang,W., Thurmond,R.L., Karlsson,L. and Edwards,J.P. The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors Bioorg Med Chem Lett (1-2-2006) 16, 2209-2212. PubMed Europe PubMed DOI I
Link,J.O. and Zipfel,S. Advances in cathepsin S inhibitor design Curr Opin Drug Discov Devel (2006) 9, 471-482. PubMed Europe PubMed T I
[YEAR:19-10-2006]Patterson,A.W., Wood,W.J., Hornsby,M., Lesley,S., Spraggon,G. and Ellman,J.A. Identification of selective, nonpeptidic nitrile inhibitors of cathepsin S using the substrate activity screening method J Med Chem (19-10-2006) 49, 6298-6307. PubMed Europe PubMed DOI I
[YEAR:27-1-2006]Tully,D.C., Liu,H., Alper,P.B., Chatterjee,A.K., Epple,R., Roberts,M.J., Williams,J.A., Nguyen,K.T., Woodmansee,D.H., Tumanut,C., Li,J., Spraggon,G., Chang,J., Tuntland,T., Harris,J.L. and Karanewsky,D.S. Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3 Bioorg Med Chem Lett (27-1-2006) 16, 1975-1980. PubMed Europe PubMed DOI S I
[YEAR:27-7-2006]Tully,D.C., Liu,H., Chatterjee,A.K., Alper,P.B., Epple,R., Williams,J.A., Roberts,M.J., Woodmansee,D.H., Masick,B.T., Tumanut,C., Li,J., Spraggon,G., Hornsby,M., Chang,J., Tuntland,T., Hollenbeck,T., Gordon,P., Harris,J.L. and Karanewsky,D.S. Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers Bioorg Med Chem Lett (27-7-2006) 16, 5112-5117. PubMed Europe PubMed DOI I
[YEAR:27-7-2006]Tully,D.C., Liu,H., Chatterjee,A.K., Alper,P.B., Williams,J.A., Roberts,M.J., Mutnick,D., Woodmansee,D.H., Hollenbeck,T., Gordon,P., Chang,J., Tuntland,T., Tumanut,C., Li,J., Harris,J.L. and Karanewsky,D.S. Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors Bioorg Med Chem Lett (27-7-2006) 16, 5107-5111. PubMed Europe PubMed DOI I

2005

[YEAR:15-3-2005]Gustin,D.J., Sehon,C.A., Wei,J., Cai,H., Meduna,S.P., Khatuya,H., Sun,S., Gu,Y., Jiang,W., Thurmond,R.L., Karlsson,L. and Edwards,J.P. Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors Bioorg Med Chem Lett (15-3-2005) 15, 1687-1691. PubMed Europe PubMed DOI I
[YEAR:15-11-2005]Liu,H., Tully,D.C., Epple,R., Bursulaya,B., Li,J., Harris,J.L., Williams,J.A., Russo,R., Tumanut,C., Roberts,M.J., Alper,P.B., He,Y. and Karanewsky,D.S. Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1 Bioorg Med Chem Lett (15-11-2005) 15, 4979-4984. PubMed Europe PubMed DOI I
Thurmond,R.L., Sun,S., Karlsson,L. and Edwards,J.P. Cathepsin S inhibitors as novel immunomodulators Curr Opin Investig Drugs (2005) 6, 473-482. PubMed Europe PubMed I
Yasuda,Y., Kaleta,J. and Bromme,D. The role of cathepsins in osteoporosis and arthritis: rationale for the design of new therapeutics Adv Drug Deliv Rev (2005) 57, 973-993. PubMed Europe PubMed DOI T I

2004

Marquis,R.W. Inhibition of the cysteine protease cathepsin K (EC 3.4.22.38) Annu Rep Med Chem (2004) 39, 79-98. DOI V I
[YEAR:23-9-2004]Thurmond,R.L., Beavers,M.P., Cai,H., Meduna,S.P., Gustin,D.J., Sun,S., Almond,H.J., Karlsson,L. and Edwards,J.P. Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S J Med Chem (23-9-2004) 47, 4799-4801. PubMed Europe PubMed DOI I
[YEAR:17-10-2004]Thurmond,R.L., Sun,S., Sehon,C.A., Baker,S.M., Cai,H., Gu,Y., Jiang,W., Riley,J.P., Williams,K.N., Edwards,J.P. and Karlsson,L. Identification of a potent and selective noncovalent cathepsin S inhibitor J Pharmacol Exp Ther (17-10-2004) 308, 268-276. PubMed Europe PubMed DOI I

2002

Saegusa,K., Ishimaru,N., Yanagi,K., Arakaki,R., Ogawa,K., Saito,I., Katunuma,N. and Hayashi,Y. Cathepsin S inhibitor prevents autoantigen presentation and autoimmunity J Clin Invest (2002) 110, 361-369. PubMed Europe PubMed DOI PMC EPMC I
[YEAR:5-12-2002]Ward,Y.D., Thomson,D.S., Frye,L.L., Cywin,C.L., Morwick,T., Emmanuel,M.J., Zindell,R., McNeil,D., Bekkali,Y., Giradot,M., Hrapchak,M., DeTuri,M., Crane,K., White,D., Pav,S., Wang,Y., Hao,M.H., Grygon,C.A., Labadia,M.E., Freeman,D.M., Davidson,W., Hopkins,J.L., Brown,M.L., Spero,D.M. and Giradot,M. Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors J Med Chem (5-12-2002) 45, 5471-5482. PubMed Europe PubMed DOI I

2000

[YEAR:28-8-2000]Walker,B., Lynas,J.F., Meighan,M.A. and Bromme,D. Evaluation of dipeptide alpha-keto-beta-aldehydes as new inhibitors of cathepsin S Biochem Biophys Res Commun (28-8-2000) 275, 401-405. PubMed Europe PubMed DOI I

1998

McGrath,M.E., Palmer,J.T., Bromme,D. and Somoza,J.R. Crystal structure of human cathepsin S Protein Sci (1998) 7, 1294-1302. PubMed Europe PubMed DOI PMC EPMC S I

1994

Gour-Salin,B.J., Lachance,P., Bonneau,P.R., Storer,A.C., Kirschke,H. and Bromme,D. E-64 analogs as inhibitors of cathepsin L and cathepsin S: importance of the S2-P2 interactions for potency and selectivity Bioorg Chem (1994) 22, 227-241. I

1993

Shaw,E., Mohanty,S., Colic,A., Stoka,V. and Turk,V. The affinity-labelling of cathepsin S with peptidyl diazomethyl ketones. Comparison with the inhibition of cathepsin L and calpain FEBS Lett (1993) 334, 340-342. PubMed Europe PubMed DOI I