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Literature for peptidase C01.036: cathepsin K

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

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    2025
  1. Gawor,J., Gawor,D.Z., Druet,I., Salindre,J., Gajosz,A., Kowalczyk,P., Dam,N., Tierny,D., Dubruque,M. and Hanf,R.
    Cathepsin K inhibition by VBX1000 alleviates canine periodontitis
    Front Vet Sci (2025) 12, 1656782-1656782. PubMed  Europe PubMed DOI  PMC  EPMC  I
  2. Lee,J., Jung,G.N., Jung,K.J., Kim,J.W., Ma,M.J., Lee,Y., Yu,J.H., Min,S.H. and Lee,J.H.
    Pyrrolopyrimidines: A promising scaffold for the development of novel cathepsin K inhibitors
    Eur J Med Chem (2025) 302, 118323-118323. PubMed  Europe PubMed DOI  I
    3. 2024
  3. Janin,Y.L.
    On the origins of SARS-CoV-2 main protease inhibitors
    RSC Med Chem (2024) 15, 81-118. PubMed  Europe PubMed DOI  PMC  EPMC  V  I
  4. Wang,Y., Guan,T., Xiong,H., Hu,W., Zhu,X., Ma,Y. and Zhang,Z.
    Synthesis and Biological Evaluation of Novel Piperidine-3-Carboxamide Derivatives as Anti-Osteoporosis Agents Targeting Cathepsin K
    Molecules (2024) 29 PubMed  Europe PubMed DOI  PMC  EPMC  I
    5. 2022
  5. Rocho,F.R., Bonatto,V., Lameiro,R.F., Lameira,J., Leitao,A. and Montanari,C.A.
    A patent review on cathepsin K inhibitors to treat osteoporosis (2011 - 2021)
    Expert Opin Ther Pat (2022) , 1-13. PubMed  Europe PubMed DOI  I
    6. 2021
  6. Gontijo,T.B., Lima,P.S., Icimoto,M.Y., Neves,R.L., de Alvarenga,E.C., Carmona,A.K., de Castro,A.A., Ramalho,T.C., da Silva Junior,E.N. and de Freitas,R.P.
    Cathepsin K inhibitors based on 2-amino-1,3,4-oxadiazole derivatives
    Bioorg Chem (2021) 109, 104662-104662. PubMed  Europe PubMed DOI  I
  7. Pomeislova,A., Otmar,M., Rubesova,P., Benysek,J., Matousova,M., Mertlikova-Kaiserova,H., Pohl,R., Postova Slavetinska,L., Pomeisl,K. and Krecmerova,M.
    1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3beta
    Bioorg Med Chem (2021) 32, 115998-115998. PubMed  Europe PubMed DOI  I
  8. Soundararajan,A., Ghag,S.A., Vuda,S.S., Wang,T. and Pattabiraman,P.P.
    Cathepsin K Regulates Intraocular Pressure by Modulating Extracellular Matrix Remodeling and Actin-Bundling in the Trabecular Meshwork Outflow Pathway
    Cells (2021) 10 PubMed  Europe PubMed DOI  PMC  EPMC  I
  9. Vashum,Y., Premsingh,R., Kottaiswamy,A., Soma,M., Padmanaban,A., Kalaiselvan,P. and Samuel,S.
    Inhibitory effect of cathepsin K inhibitor (ODN-MK-0822) on invasion, migration and adhesion of human breast cancer cells in vitro
    Mol Biol Rep (2021) 48, 105-116. PubMed  Europe PubMed DOI  I
  10. Vashum,Y., Kottaiswamy,A., Bupesh,G., Singh,R.P., Kalaiselvan,P., Thiagarajan,K. and Samuel,S.
    Inhibitory Effects of Cathepsin K Inhibitor (ODN-MK-0822) on the Paracrine Pro-Osteoclast Factors of Breast Cancer Cells
    Curr Mol Pharmacol (2021) PubMed  Europe PubMed DOI  I
    11. 2020
  11. Bennacef,I., Rubins,D., Riffel,K., Williams,M., Posavec,D.J., Holahan,M.A., Purcell,M.L., Haley,H.D., Wolf,M., Stachel,S.J., Lubbers,L.S., Wesolowski,G.A., Duong,L.T., Hamill,T.G., Evelhoch,J.L. and Hostetler,E.D.
    Preclinical evaluation of [(11) C]L-235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone
    J Labelled Comp Radiopharm (2020) PubMed  Europe PubMed DOI  I
  12. 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
  13. Conaghan,P.G., Bowes,M.A., Kingsbury,S.R., Brett,A., Guillard,G., Rizoska,B., Sjogren,N., Graham,P., Jansson,A., Wadell,C., Bethell,R. and Ohd,J.
    Disease-modifying effects of a novel cathepsin K inhibitor in osteoarthritis: a randomized, placebo-controlled study
    Ann Intern Med (2020) 172, 86-95. PubMed  Europe PubMed DOI  I
  14. Jastaniah,A., Gaisina,I.N., Knopp,R.C. and Thatcher,G.R.J.
    Synthesis of alpha-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents
    ChemMedChem (2020) PubMed  Europe PubMed DOI  I
  15. Oso,B.J., Adeoye,A.O. and Olaoye,I.F.
    Pharmacoinformatics and hypothetical studies on allicin, curcumin, and gingerol as potential candidates against COVID-19-associated proteases
    J Biomol Struct Dyn (2020) , 1-12. PubMed  Europe PubMed DOI  I
  16. Reithmeier,A., Norgard,M., Ek-Rylander,B., Nareoja,T. and Andersson,G.
    Cathepsin K regulates localization and secretion of tartrate-resistant acid phosphatase (TRAP) in TRAP-overexpressing MDA-MB-231 breast cancer cells
    BMC Mol Cell Biol (2020) 21, 15-15. PubMed  Europe PubMed DOI  PMC  EPMC  I
  17. Seo,S.U., Woo,S.M., Kim,M.W., Lee,H.S., Kim,S.H., Kang,S.C., Lee,E.W., Min,K.J. and Kwon,T.K.
    Cathepsin K inhibition-induced mitochondrial ROS enhances sensitivity of cancer cells to anti-cancer drugs through USP27x-mediated Bim protein stabilization
    Redox Biol (2020) 30, 101422-101422. PubMed  Europe PubMed DOI  PMC  EPMC  I
  18. Silva,T.L., Dos Santos,D.A., de Jesus,H.C.R., Bromme,D., Fernandes,J.B., Paixao,M.W., Correa,A.G. and Vieira,P.C.
    Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors
    Bioorg Med Chem (2020) 28, 115597-115597. PubMed  Europe PubMed DOI  I
  19. Zajic,S., Stoch,S.A., McCrea,J.B., Witter,R., Fayad,G.N., Martinho,M. and Stone,J.A.
    A phase 1 pooled PK/PD analysis of bone resorption biomarkers for odanacatib, a Cathepsin K inhibitor
    J Pharmacokinet Pharmacodyn (2020) 47, 473-484. PubMed  Europe PubMed DOI  I
    20. 2019
  20. Law,S., Du,X., Panwar,P., Honson,N.S., Pfeifer,T., Roberge,M. and Bromme,D.
    Identification of substrate-specific inhibitors of cathepsin K through high-throughput screening
    Biochem J (2019) 476, 499-512. PubMed  Europe PubMed DOI  I
  21. Ma,B., Wesolowski,G., Luo,B., Lifsted,T., Wessner,K., Adamson,G., Glantschnig,H. and Lubbers,L.S.
    Suppression of cathepsin K biomarker in synovial fluid as a free-drug-driven process
    J Circ Biomark (2019) 8, 1849454418821819-1849454418821819. PubMed  Europe PubMed DOI  PMC  EPMC  I
  22. Mons,E., Jansen,I.D.C., Loboda,J., van Doodewaerd,B.R., Hermans,J., Verdoes,M., van Boeckel,C.A.A., van Veelen,P.A., Turk,B., Turk,D. and Ovaa,H.
    The alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of cathepsin K
    J Am Chem Soc (2019) 141, 3507-3514. PubMed  Europe PubMed DOI  I
  23. Petek,N., Stefane,B., Novinec,M. and Svete,J.
    Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors
    Bioorg Chem (2019) 84, 226-238. PubMed  Europe PubMed DOI  I
  24. Pirapaharan,D.C., Soe,K., Panwar,P., Madsen,J.S., Bergmann,M.L., Overgaard,M., Bromme,D. and Delaisse,J.M.
    A mild inhibition of cathepsin K paradoxically stimulates the resorptive activity of osteoclasts in culture
    Calcif Tissue Int (2019) 104, 92-101. PubMed  Europe PubMed DOI  I
  25. Visetvichaporn,V., Kim,K.H., Jung,K., Cho,Y.S. and Kim,D.D.
    Formulation of self-microemulsifying drug delivery system (SMEDDS) by D-optimal mixture design to enhance the oral bioavailability of a new cathepsin K inhibitor (HL235)
    Int J Pharm (2019) , 118772-118772. PubMed  Europe PubMed DOI  I
  26. Yuan,X.Y., Ren,Z., Wu,Y., Bougault,C., Brizuela,L., Magne,D., Buchet,R. and Mebarek,S.
    Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes
    Bioorg Med Chem (2019) 27, 1034-1042. PubMed  Europe PubMed DOI  I
    27. 2018
  27. Colon-Bernal,I.D., Duong,L.T., Pennypacker,B., Henderson,J., Kozloff,K.M. and Banaszak Holl,M.M.
    Cathepsin K inhibition preserves compressive load in lumbar vertebrae of osteoporotic monkeys
    Bone Rep (2018) 9, 159-164. PubMed  Europe PubMed DOI  PMC  EPMC  I
  28. Lindstrom,E., Rizoska,B., Tunblad,K., Edenius,C., Bendele,A.M., Maul,D., Larson,M., Shah,N., Yoder Otto,V., Jerome,C. and Grabowska,U.
    The selective cathepsin K inhibitor MIV-711 attenuates joint pathology in experimental animal models of osteoarthritis
    J Transl Med (2018) 16, 56-56. PubMed  Europe PubMed DOI  PMC  EPMC  I
  29. Lu,J., Wang,M., Wang,Z., Fu,Z., Lu,A. and Zhang,G.
    Advances in the discovery of cathepsin K inhibitors on bone resorption
    J Enzyme Inhib Med Chem (2018) 33, 890-904. PubMed  Europe PubMed DOI  V  I
    30. 2017
  30. Drake,M.T., Clarke,B.L., Oursler,M.J. and Khosla,S.
    Cathepsin K inhibitors for osteoporosis: biology, potential clinical utility, and lessons learned
    Endocr Rev (2017) 38, 325-350. PubMed  Europe PubMed DOI  I
  31. 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
  32. Kruglyak,N., Williams,D.E., Chen,H., Law,S., Kaleta,J., Villanueva,I., Davies,J.E., Andersen,R.J. and Bromme,D.
    Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K
    Bioorg Med Chem Lett (2017) 27, 1397-1400. PubMed  Europe PubMed DOI  I
  33. Law,S., Andrault,P.M., Aguda,A.H., Nguyen,N.T., Kruglyak,N., Brayer,G.D. and Bromme,D.
    Identification of mouse cathepsin K structural elements that regulate the potency of odanacatib
    Biochem J (2017) 474, 851-864. PubMed  Europe PubMed DOI  S  I
  34. Law,S., Panwar,P., Li,J., Aguda,A.H., Jamroz,A., Guido,R.V.C. and Bromme,D.
    A composite docking approach for the identification and characterization of ectosteric inhibitors of cathepsin K
    PLoS ONE (2017) 12, e0186869-e0186869. PubMed  Europe PubMed DOI  PMC  EPMC  I
  35. Ma,B., Luo,B., Euler,D.H., Cusick,T.E., Wesolowski,G., Glantschnig,H., Duong,L.T., Ou,Y., Carroll,S.S. and Lubbers,L.S.
    Applicability of in vitro-in vivo translation of cathepsin K inhibition from animal species to human with the use of free-drug hypothesis
    Naunyn Schmiedebergs Arch Pharmacol (2017) 390, 435-441. PubMed  Europe PubMed DOI  I
  36. Panwar,P., Xue,L., Soe,K., Srivastava,K., Law,S., Delaisse,J.M. and Bromme,D.
    An ectosteric inhibitor of cathepsin K inhibits bone resorption in ovariectomized mice
    J Bone Miner Res (2017) 32, 2415-2430. PubMed  Europe PubMed DOI  I
  37. Yamashita,K., Iwatake,M., Okamoto,K., Yamada,S.I., Umeda,M. and Tsukuba,T.
    Cathepsin K modulates invasion, migration, and adhesion of oral squamous cell carcinomas in vitro
    Oral Dis (2017) 23, 518-525. PubMed  Europe PubMed DOI  I
    38. 2016
  38. Bromme,D., Panwar,P. and Turan,S.
    Cathepsin K osteoporosis trials, pycnodysostosis and mouse deficiency models: commonalities and differences
    Expert Opin Drug Discov (2016) 11, 457-472. PubMed  Europe PubMed DOI  I
  39. Duong,l.T., Leung,A.T. and Langdahl,B.
    Cathepsin K inhibition: a new mechanism for the treatment of osteoporosis
    Calcif Tissue Int (2016) 98, 381-397. PubMed  Europe PubMed DOI  I
  40. Herroon,M.K., Sharma,R., Rajagurubandara,E., Turro,C., Kodanko,J.J. and Podgorski,I.
    Photoactivated inhibition of cathepsin K in a 3D tumor model
    Biol Chem (2016) 397, 571-582. PubMed  Europe PubMed DOI  I
  41. 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
  42. Jiang,Y.-T., Ma,Z.-G., Jiao,J.-B., Guo,Z., Qian,L.-G., Chen,T.-P., Li,Q.-G., Wang,Y.-F. and Xue,J.-W.
    Cathepsin K inhibitor, icariin, increases the healing potential and biomechanical properties of femoral neck in a mice fractured model
    Int J Clin Exp Med (2016) 9, 15788-15795.  I
  43. Mukherjee,K. and Chattopadhyay,N.
    Pharmacological inhibition of cathepsin K: a promising novel approach for postmenopausal osteoporosis therapy
    Biochem Pharmacol (2016) 117, 10-19. PubMed  Europe PubMed DOI  I
  44. Ochi,Y., Yamada,H., Mori,H., Kawada,N., Tanaka,M., Imagawa,A., Ohmoto,K. and Kawabata,K.
    Combination therapy with ONO-KK1-300-01, a cathepsin K inhibitor, and parathyroid hormone results in additive beneficial effect on bone mineral density in ovariectomized rats
    J Bone Miner Metab (2016) 34, 33-40. PubMed  Europe PubMed DOI  I
  45. Panwar,P., Soe,K., Guido,R.V., Bueno,R.V., Delaisse,J.M. and Bromme,D.
    A novel approach to inhibit bone resorption: exosite inhibitors against cathepsin K
    Br J Pharmacol (2016) 173, 396-410. PubMed  Europe PubMed DOI  I
  46. 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
  47. Qiu,Z.C., Dong,X.L., Dai,Y., Xiao,G.K., Wang,X.L., Wong,K.C., Wong,M.S. and Yao,X.S.
    Discovery of a new class of cathepsin K inhibitors in Rhizoma drynariae as potential candidates for the treatment of osteoporosis
    Int J Mol Sci (2016) 17 PubMed  Europe PubMed DOI  I
  48. Wang,Y., Li,R., Zheng,Z., Yi,H. and Li,Z.
    Identification of novel cathepsin K inhibitors using ligand-based virtual screening and structure-based docking
    RSC Adv (2016) 6, 82961-82968. DOI  I
    49. 2015
  49. Abdel-Magid,A.F.
    Inhibition of cathepsin K: a novel and promising treatment for osteoporosis
    ACS Med Chem Lett (2015) 6, 628-629. PubMed  Europe PubMed DOI  PMC  EPMC  I
  50. Borisek,J., Vizovisek,M., Sosnowski,P., Turk,B., Turk,D., Mohar,B. and Novic,M.
    Development of N-(functionalized benzoyl)-homocycloleucyl-glycinonitriles as potent cathepsin K inhibitors
    J Med Chem (2015) 58, 6928-6937. PubMed  Europe PubMed DOI  I
  51. Fujii,T., Ishikawa,M., Kubo,A. and Tanaka,Y.
    Effect of SI-591, a new class of cathepsin K inhibitor with peptidomimetic structure, on bone metabolism in vitro and in vivo
    Bone (2015) 81, 427-434. PubMed  Europe PubMed DOI  I
  52. Gamsjager,M. and Resch,H.
    [Cathepsin K antagonists: preclinical and clinical data]
    Wien Med Wochenschr (2015) 165, 65-70. PubMed  Europe PubMed DOI  I
  53. Gruber,R.
    Molecular and cellular basis of bone resorption
    Wien Med Wochenschr (2015) 165, 48-53. PubMed  Europe PubMed DOI  I
  54. Pietschmann,P.
    Cathepsin K inhibitors: emerging treatment options for osteoporosis
    Wien Med Wochenschr (2015) 165, 47-47. PubMed  Europe PubMed DOI  I
  55. Suzuki,N., Takimoto,K. and Kawashima,N.
    Cathepsin K inhibitor regulates inflammation and bone destruction in experimentally induced rat periapical lesions
    J Endod (2015) 41, 1474-1479. PubMed  Europe PubMed DOI  I
  56. Yuan,X., Liu,Y., Hua,X., Deng,X., Sun,P., Yu,C., Chen,L., Yu,S., Liu,S. and Pang,H.
    Myricetin ameliorates the symptoms of collagen-induced arthritis in mice by inhibiting cathepsin K activity
    Immunopharmacol Immunotoxicol (2015) 37, 513-519. PubMed  Europe PubMed DOI  I
    57. 2014
  57. Borisek,J., Drgan,V., Minovski,N. and Novic,M.
    Mechanistic interpretation of artificial neural network-based QSAR model for prediction of cathepsin K inhibition potency
    J Chemometr (2014) 28, 272-281. DOI  I
  58. Hussein,H., Ishihara,A., Menendez,M. and Bertone,A.
    Pharmacokinetics and bone resorption evaluation of a novel cathepsin K inhibitor (VEL-0230) in healthy adult horses
    J Vet Pharmacol Ther (2014) 37, 556-564. PubMed  Europe PubMed DOI  I
  59. Novinec,M., Korenc,M., Caflisch,A., Ranganathan,R., Lenarcic,B. and Baici,A.
    A novel allosteric mechanism in the cysteine peptidase cathepsin K discovered by computational methods
    Nat Commun (2014) 5, 3287-3287. PubMed  Europe PubMed DOI  S  I
  60. Pennypacker,B.L., Chen,C.M., Zheng,H., Shih,M.S., Belfast,M., Samadfam,R. and Duong,l.T.
    Inhibition of cathepsin K increases modeling-based bone formation, and improves cortical dimension and strength in adult ovariectomized monkeys
    J Bone Miner Res (2014) 29, 1847-1858. PubMed  Europe PubMed DOI  I
  61. Respondek,T., Sharma,R., Herroon,M.K., Garner,R.N., Knoll,J.D., Cueny,E., Turro,C., Podgorski,I. and Kodanko,J.J.
    Inhibition of cathepsin activity in a cell-based assay by a light-activated ruthenium compound
    ChemMedChem (2014) 9, 1306-1315. PubMed  Europe PubMed DOI  I
  62. Rodnick,M.E., Shao,X., Kozloff,K.M., Scott,P.J. and Kilbourn,M.R.
    Carbon-11 labeled cathepsin K inhibitors: syntheses and preliminary in vivo evaluation
    Nucl Med Biol (2014) 41, 384-389. PubMed  Europe PubMed DOI  I
  63. Zhuo,Y., Gauthier,J.Y., Black,W.C., Percival,M.D. and Duong,L.T.
    Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible
    Bone (2014) 67, 269-280. PubMed  Europe PubMed DOI  I
    64. 2013
  64. 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
  65. Helali,A.M., Iti,F.M. and Mohamed,I.N.
    Cathepsin K inhibitors: a novel target but promising approach in the treatment of osteoporosis
    Curr Drug Targets (2013) 14, 1591-1600. PubMed  Europe PubMed DOI  V  I
  66. Ren,X.F., Li,H.W., Fang,X., Wu,Y., Wang,L. and Zou,S.
    Highly selective azadipeptide nitrile inhibitors for cathepsin K: design, synthesis and activity assays
    Org Biomol Chem (2013) 11, 1143-1148. PubMed  Europe PubMed DOI  I
  67. Stoch,S.A., Zajic,S., Stone,J.A., Miller,D.L., van Bortel,L., Lasseter,K.C., Pramanik,B., Cilissen,C., Liu,Q., Liu,L., Scott,B.B., Panebianco,D., Ding,Y., Gottesdiener,K. and Wagner,J.A.
    Odanacatib, a selective cathepsin K inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics - results from single oral dose studies in healthy volunteers
    Br J Clin Pharmacol (2013) 75, 1240-1254. PubMed  Europe PubMed DOI  I
  68. Sun,P., Liu,Y., Deng,X., Yu,C., Dai,N., Yuan,X., Chen,L., Yu,S., Si,W., Wang,X., Wu,D., Liu,S. and Pang,H.
    An inhibitor of cathepsin K, icariin suppresses cartilage and bone degradation in mice of collagen-induced arthritis
    Phytomedicine (2013) 20, 975-979. PubMed  Europe PubMed DOI  I
  69. Yu,Y.Y., Sun,W., Dong,L., Liu,H.D., Jiang,D., Xiao,J.H., Yang,X.H. and Li,S.
    Design, synthesis, and screen of cathepsin K inhibitors
    Chin Chem Lett (2013) 24, 715-718. DOI  I
  70. Yuan,X.Y., Fu,D.Y., Ren,X.F., Fang,X., Wang,L., Zou,S. and Wu,Y.
    Highly selective aza-nitrile inhibitors for cathepsin K, structural optimization and molecular modeling
    Org Biomol Chem (2013) 11, 5847-5852. PubMed  Europe PubMed DOI  S  I
    71. 2012
  71. Boonen,S., Rosenberg,E., Claessens,F., Vanderschueren,D. and Papapoulos,S.
    Inhibition of cathepsin K for treatment of osteoporosis
    Curr Osteoporos Rep (2012) 10, 73-79. PubMed  Europe PubMed DOI  I
  72. Crawford,J.J., Kenny,P.W., Bowyer,J., Cook,C.R., Finlayson,J.E., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Krapp,S., Martin,S., Macfaul,P.A., McDermott,B.P., McGuire,T.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S., Smith,C. and Dossetter,A.G.
    Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors
    J Med Chem (2012) 55, 8827-8837. PubMed  Europe PubMed DOI  I
  73. Dossetter,A.G., Beeley,H., Bowyer,J., Cook,C.R., Crawford,J.J., Finlayson,J.E., Heron,N.M., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Kenny,P.W., Krapp,S., Martin,S., Macfaul,P.A., McGuire,T.M., Gutierrez,P.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S., Smith,C. and Vickers,M.
    (1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A potent and highly selective Cathepsin K inhibitor for the treatment of osteoarthritis
    J Med Chem (2012) 55, 6363-6374. PubMed  Europe PubMed DOI  I
  74. Dossetter,A.G., Bowyer,J., Cook,C.R., Crawford,J.J., Finlayson,J.E., Heron,N.M., Heyes,C., Highton,A.J., Hudson,J.A., Jestel,A., Krapp,S., Macfaul,P.A., McGuire,T.M., Morley,A.D., Morris,J.J., Page,K.M., Ribeiro,L.R., Sawney,H., Steinbacher,S. and Smith,C.
    Isosteric replacements for benzothiazoles and optimisation to potent cathepsin K inhibitors free from hERG channel inhibition
    Bioorg Med Chem Lett (2012) 22, 5563-5568. PubMed  Europe PubMed DOI  I
  75. Hayami,T., Zhuo,Y., Wesolowski,G.A., Pickarski,M. and Duong,L.T.
    Inhibition of cathepsin K reduces cartilage degeneration in the anterior cruciate ligament transection rabbit and murine models of osteoarthritis
    Bone (2012) 50, 1250-1259. PubMed  Europe PubMed DOI  I
  76. Jerome,C., Missbach,M. and Gamse,R.
    Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys
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