Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DEG3S8C)

DME Name Cathepsin K (CTSK)
Synonyms Cathepsin O; Cathepsin O2; Cathepsin X; CTSK; CTSO; CTSO2
Gene Name CTSK
UniProt ID
CATK_HUMAN
INTEDE ID
DME0573
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
1513
EC Number EC: 3.4.22.38
Hydrolases
Peptidase
Cysteine protease
EC: 3.4.22.38
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MWGLKVLLLPVVSFALYPEEILDTHWELWKKTHRKQYNNKVDEISRRLIWEKNLKYISIH
NLEASLGVHTYELAMNHLGDMTSEEVVQKMTGLKVPLSHSRSNDTLYIPEWEGRAPDSVD
YRKKGYVTPVKNQGQCGSCWAFSSVGALEGQLKKKTGKLLNLSPQNLVDCVSENDGCGGG
YMTNAFQYVQKNRGIDSEDAYPYVGQEESCMYNPTGKAAKCRGYREIPEGNEKALKRAVA
RVGPVSVAIDASLTSFQFYSKGVYYDESCNSDNLNHAVLAVGYGIQKGNKHWIIKNSWGE
NWGNKGYILMARNKNNACGIANLASFPKM
Function This enzyme displays potent endoprotease activity against fibrinogen at acid pH and may play an important role in extracellular matrix degradation.
KEGG Pathway
Apoptosis (hsa04210 )
Lysosome (hsa04142 )
Osteoclast differentiation (hsa04380 )
Rheumatoid arthritis (hsa05323 )
Toll-like receptor signaling pathway (hsa04620 )
Reactome Pathway
Collagen degradation (R-HSA-1442490 )
Degradation of the extracellular matrix (R-HSA-1474228 )
MHC class II antigen presentation (R-HSA-2132295 )
RUNX1 regulates transcription of genes involved in differentiation of keratinocytes (R-HSA-8939242 )
Trafficking and processing of endosomal TLR (R-HSA-1679131 )
Activation of Matrix Metalloproteinases (R-HSA-1592389 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
1 Clinical Trial Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
BRADYKININ DM4R6UV N. A. N. A. Phase 1 [24]

Molecular Expression Atlas (MEA) of This DME

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DME
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 1.72E-04 -2.36E-01 -4.87E-01
Alopecia ED70 Skin from scalp 3.60E-04 1.83E-01 6.33E-01
Alzheimer's disease 8A20 Entorhinal cortex 2.91E-01 4.76E-02 1.34E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 5.61E-01 8.07E-01 8.05E-01
Aortic stenosis BB70 Calcified aortic valve 7.83E-01 3.29E-01 2.36E-01
Apnea 7A40 Hyperplastic tonsil 9.47E-01 -4.59E-01 -1.23E+00
Arthropathy FA00-FA5Z Peripheral blood 6.30E-01 7.13E-02 3.26E-01
Asthma CA23 Nasal and bronchial airway 4.07E-03 8.39E-02 7.20E-02
Atopic dermatitis EA80 Skin 2.74E-12 -1.29E+00 -4.68E+00
Autism 6A02 Whole blood 2.24E-01 1.33E-01 2.83E-01
Autoimmune uveitis 9A96 Peripheral monocyte 3.98E-01 4.84E-01 1.21E+00
Autosomal dominant monocytopenia 4B04 Whole blood 1.63E-01 2.33E-01 7.18E-01
Bacterial infection of gingival 1C1H Gingival tissue 1.46E-07 4.17E-01 6.43E-01
Batten disease 5C56.1 Whole blood 9.16E-02 2.75E-01 6.41E-01
Behcet's disease 4A62 Peripheral blood 5.69E-01 1.78E-01 4.71E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 5.01E-01 -2.93E-02 -1.05E-01
Bladder cancer 2C94 Bladder tissue 1.67E-06 -1.26E+00 -3.94E+00
Breast cancer 2C60-2C6Z Breast tissue 1.29E-11 -5.77E-01 -5.19E-01
Cardioembolic stroke 8B11.20 Whole blood 1.97E-10 7.90E-01 2.26E+00
Cervical cancer 2C77 Cervical tissue 6.08E-02 4.40E-01 6.21E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 3.72E-01 -1.13E-01 -3.60E-01
Chronic hepatitis C 1E51.1 Whole blood 2.37E-01 -9.57E-02 -4.85E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 2.97E-01 1.45E-01 1.91E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 9.22E-02 -1.77E-01 -4.40E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 7.95E-01 -1.04E-01 -7.54E-02
Colon cancer 2B90 Colon tissue 9.70E-58 1.43E+00 2.09E+00
Coronary artery disease BA80-BA8Z Peripheral blood 2.26E-01 1.91E-01 4.14E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 3.81E-01 8.20E-02 1.28E-01
Endometriosis GA10 Endometrium tissue 2.70E-01 1.38E-01 1.10E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 8.45E-01 -9.97E-02 -3.33E-01
Familial hypercholesterolemia 5C80.00 Whole blood 2.44E-06 5.94E-01 1.48E+00
Gastric cancer 2B72 Gastric tissue 2.36E-01 1.08E+00 1.04E+00
Glioblastopma 2A00.00 Nervous tissue 3.42E-104 1.01E+00 1.64E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 3.93E-01 8.10E-01 7.95E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 1.64E-02 4.06E-01 5.02E-01
Head and neck cancer 2D42 Head and neck tissue 1.70E-32 1.96E+00 1.46E+00
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 1.18E-02 -1.59E-01 -7.74E-01
Huntington's disease 8A01.10 Whole blood 1.29E-01 3.58E-01 1.16E+00
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 4.28E-05 1.96E+00 4.26E+00
Immunodeficiency 4A00-4A20 Peripheral blood 1.36E-01 -6.11E-02 -2.61E-01
Influenza 1E30 Whole blood 9.70E-01 -1.56E-01 -5.70E-01
Interstitial cystitis GC00.3 Bladder tissue 1.28E-02 8.37E-01 2.61E+00
Intracranial aneurysm 8B01.0 Intracranial artery 1.70E-01 7.39E-01 1.45E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 8.37E-03 -2.84E-01 -5.71E-01
Ischemic stroke 8B11 Peripheral blood 3.72E-01 2.23E-01 6.25E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 3.47E-02 -1.20E-01 -3.24E-01
Lateral sclerosis 8B60.4 Skin 3.95E-01 2.67E-01 3.61E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 1.88E-01 -2.55E-01 -2.77E-01
Liver cancer 2C12.0 Liver tissue 5.14E-03 1.10E-01 2.02E-01
Liver failure DB99.7-DB99.8 Liver tissue 1.09E-03 1.15E+00 1.95E+00
Lung cancer 2C25 Lung tissue 1.34E-17 7.09E-01 8.69E-01
Lupus erythematosus 4A40 Whole blood 1.60E-03 2.80E-01 5.27E-01
Major depressive disorder 6A70-6A7Z Hippocampus 4.91E-01 -2.24E-02 -7.68E-02
Major depressive disorder 6A70-6A7Z Whole blood 9.81E-01 -4.31E-02 -7.60E-02
Melanoma 2C30 Skin 2.88E-02 6.01E-01 6.80E-01
Multiple myeloma 2A83.1 Peripheral blood 9.37E-02 2.34E-01 7.25E-01
Multiple myeloma 2A83.1 Bone marrow 1.53E-01 1.21E-01 4.88E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 4.34E-01 -1.34E-02 -3.11E-02
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 9.31E-02 -2.15E-01 -3.14E-01
Myelofibrosis 2A20.2 Whole blood 1.19E-04 2.52E-01 2.43E+00
Myocardial infarction BA41-BA50 Peripheral blood 4.56E-01 9.82E-02 1.17E-01
Myopathy 8C70.6 Muscle tissue 3.14E-04 1.34E+00 2.00E+00
Neonatal sepsis KA60 Whole blood 3.60E-10 4.11E-01 1.08E+00
Neuroectodermal tumour 2A00.11 Brain stem tissue 2.17E-03 3.47E-01 8.71E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 9.16E-01 -1.30E-01 -4.23E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 5.03E-01 1.67E-02 4.21E-02
Olive pollen allergy CA08.00 Peripheral blood 2.01E-01 4.92E-01 9.06E-01
Oral cancer 2B6E Oral tissue 5.70E-07 1.71E+00 1.54E+00
Osteoarthritis FA00-FA0Z Synovial tissue 5.32E-01 7.03E-01 6.35E-01
Osteoporosis FB83.1 Bone marrow 2.85E-01 -1.14E+00 -2.61E+00
Ovarian cancer 2C73 Ovarian tissue 5.31E-07 -1.50E+00 -4.64E+00
Pancreatic cancer 2C10 Pancreas 2.09E-03 1.63E+00 1.17E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 5.05E-01 1.32E-02 5.54E-02
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 2.52E-01 3.84E-01 7.10E-01
Pituitary cancer 2D12 Pituitary tissue 6.17E-01 -6.41E-02 -1.09E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 8.11E-01 6.83E-02 1.11E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 5.00E-01 -1.29E-01 -5.26E-01
Polycythemia vera 2A20.4 Whole blood 2.98E-01 7.45E-02 5.88E-01
Pompe disease 5C51.3 Biceps muscle 1.80E-02 6.01E-01 1.27E+00
Preterm birth KA21.4Z Myometrium 2.70E-01 -1.80E-01 -2.14E-01
Prostate cancer 2C82 Prostate 8.38E-03 -6.87E-01 -6.91E-01
Psoriasis EA90 Skin 8.88E-14 -7.07E-01 -1.15E+00
Rectal cancer 2B92 Rectal colon tissue 3.39E-02 5.72E-01 1.11E+00
Renal cancer 2C90-2C91 Kidney 2.86E-04 5.04E-01 1.08E+00
Retinoblastoma 2D02.2 Uvea 3.76E-08 3.11E+00 1.22E+01
Rheumatoid arthritis FA20 Synovial tissue 6.91E-04 1.59E+00 1.81E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 7.70E-01 -1.35E-02 -6.52E-02
Schizophrenia 6A20 Prefrontal cortex 3.77E-02 1.14E-01 3.21E-01
Schizophrenia 6A20 Superior temporal cortex 4.36E-01 -6.26E-02 -4.64E-01
Scleroderma 4A42.Z Whole blood 1.57E-01 1.40E-01 4.60E-01
Seizure 8A60-8A6Z Whole blood 3.83E-01 -5.03E-02 -1.29E-01
Sensitive skin EK0Z Skin 1.72E-01 -1.72E-01 -9.96E-01
Sepsis with septic shock 1G41 Whole blood 3.62E-16 2.67E-01 8.11E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.24E-01 -8.86E-02 -3.03E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 3.19E-01 8.17E-03 2.17E-02
Simpson golabi behmel syndrome LD2C Adipose tissue 8.12E-01 -1.25E-01 -1.50E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 1.40E-01 4.74E-01 1.91E+00
Skin cancer 2C30-2C3Z Skin 1.38E-20 -9.27E-01 -1.15E+00
Thrombocythemia 3B63 Whole blood 3.67E-01 2.35E-03 2.50E-02
Thrombocytopenia 3B64 Whole blood 4.67E-01 3.36E-01 6.13E-01
Thyroid cancer 2D10 Thyroid 3.81E-04 1.85E-01 3.60E-01
Tibial muscular dystrophy 8C75 Muscle tissue 2.12E-08 2.62E+00 3.28E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 1.50E-01 3.99E-01 1.76E+00
Type 2 diabetes 5A11 Liver tissue 6.37E-01 1.04E-01 3.47E-01
Ureter cancer 2C92 Urothelium 1.70E-01 -1.97E-01 -5.47E-01
Uterine cancer 2C78 Endometrium tissue 1.10E-13 -1.03E+00 -1.01E+00
Vitiligo ED63.0 Skin 5.42E-01 1.39E-02 2.81E-02
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⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Cathepsin K (CTSK) DTT Info
DME DTT Type Clinical trial
3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Odanacatib DM1EO3G Osteoporosis FB83.0 Phase 3 [1]
SAR-114137 DMZ1XR5 Pain MG30-MG3Z Phase 1 [2]
VEL-0230 DMDSC63 Rheumatoid arthritis FA20 Phase 1 [3]
8 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Oxotetrahydro-2-H-furo[3.2-b]pyrrol-4(5-H)-yl derivative 1 DM1SH5R Pain MG30-MG3Z Patented [4]
PMID25399719-Compound-17 DMRXKJZ N. A. N. A. Patented [5]
PMID27998201-Compound-10 DMVXTIL Osteoporosis FB83.0 Patented [4]
PMID27998201-Compound-12 DM8QZNC Bone cancer 2B5Z Patented [4]
PMID27998201-Compound-15 DMOB8LU Pain MG30-MG3Z Patented [4]
PMID27998201-Compound-5 DMVZ0ND Chronic obstructive pulmonary disease CA22 Patented [4]
PMID27998201-Compound-8 DMZK0SY N. A. N. A. Patented [4]
PMID27998201-Compound-9 DM1JOZN Rheumatoid arthritis FA20 Patented [4]
⏷ Show the Full List of 8 Patented Agent(s)
4 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Balicatib DM06JTL Osteoporosis FB83.0 Discontinued in Phase 2 [6]
ONO-5334 DMWS7C2 Osteoporosis FB83.0 Discontinued in Phase 2 [7]
Relacatib DMLJEFH Bone metastases 2D50 Discontinued in Phase 2 [8]
MIV-701 DM23KBM Osteoporosis FB83.0 Discontinued in Phase 1 [9]
2 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GW-2592X DMNAT5V Osteoporosis FB83.0 Preclinical [10]
L-006235-1 DMMEH12 Osteoarthritis FA00-FA05 Preclinical [11]
48 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate DMICUQK Discovery agent N.A. Investigative [12]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate DMAQX4K Discovery agent N.A. Investigative [12]
(S)-tert-butyl 4-methyl-1-oxopentan-2-ylcarbamate DMR1HQ3 Discovery agent N.A. Investigative [12]
2-cyclohexylamino-pyridine-2-carbonitrile DMFMZRB Discovery agent N.A. Investigative [13]
2-cyclohexylamino-pyrimidine-4-carbonitrile DMMIGXO Discovery agent N.A. Investigative [13]
3-Amino-5-Phenylpentane DMHDFZE Discovery agent N.A. Investigative [14]
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile DMNT5BF Discovery agent N.A. Investigative [15]
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile DM10U6S Discovery agent N.A. Investigative [15]
4-cyclohexylamino-pyrimidine-2-carbonitrile DMGVIXW Discovery agent N.A. Investigative [13]
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile DMS42TN Discovery agent N.A. Investigative [15]
4-phenyl-6-propylpyrimidine-2-carbonitrile DMMIB0R Discovery agent N.A. Investigative [16]
4-propyl-6-m-tolylpyrimidine-2-carbonitrile DMNM4GE Discovery agent N.A. Investigative [16]
AM-3701 DMZVLJH Bone metastases 2D50 Investigative [10]
BF/PC-21 DMCWB1V Inflammation 1A00-CA43.1 Investigative [10]
Boc-Agly-Val-Agly-OEt DMDX8M3 Discovery agent N.A. Investigative [17]
GNF-PF-5434 DMP9AIH Discovery agent N.A. Investigative [18]
L-873724 DMUP516 Asthma CA23 Investigative [8]
MIV-710 DM13TUY Bone metastases 2D50 Investigative [10]
N-(1-((cyanomethyl)carbamoyl)cyclohexyl)benzamide DMBQ5NS Discovery agent N.A. Investigative [19]
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile DMUJS4Y Discovery agent N.A. Investigative [20]
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile DMR18YI Discovery agent N.A. Investigative [20]
N-(cyanomethyl)cyclohex-1-ene-1-carboxamide DMTKREZ Discovery agent N.A. Investigative [19]
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile DMJ0S5C Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile DMXYQWG Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile DM3I0WZ Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile DMGF4XC Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-norvalyl-glycine-nitrile DMOP5N7 Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile DMUQBOP Discovery agent N.A. Investigative [20]
N-acetyl-phenylalanyl-glycine-nitrile DME8O69 Discovery agent N.A. Investigative [20]
N-benzoyl-phenylalanyl-glycine-nitrile DMRJ4B1 Discovery agent N.A. Investigative [20]
P2,P3 Ketoamide derivative DMETL3Z Discovery agent N.A. Investigative [21]
PMID16290936C1b DMOP8YM Discovery agent N.A. Investigative [12]
Pyrrolidine-1-carbonitrile DM906JK Discovery agent N.A. Investigative [22]
Tert-butyl (2S)-1-cyanopyrrolidine-2-carboxylate DM8LI1K Discovery agent N.A. Investigative [22]
TERT-BUTYL 2-CYANO-2-METHYLHYDRAZINECARBOXYLATE DMZG5I7 Discovery agent N.A. Investigative [23]
Tert-Butyl(1s)-1-Cyclohexyl-2-Oxoethylcarbamate DM42WFH Discovery agent N.A. Investigative [23]
Z-Ala-Leu-His-Agly-Ile-Val-OMe DMMP0DT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl DM7IGRT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-lle-Agly-Ile-Val-OMe DMVEUOL Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe DM3209T Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe DML16BT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe DMIB5O3 Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 DM69FKN Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 DMZDGJO Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ileu-Val-OMe DMT0UZ1 Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 DMM5O2V Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 DMTWNH7 Discovery agent N.A. Investigative [17]
Z-leu-Val-Agly-Val-OBzl DM6OGR9 Discovery agent N.A. Investigative [17]
⏷ Show the Full List of 48 Investigative Drug(s)

References

1 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
2 From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor. Eur J Pharm Biopharm. 2013 Apr;83(3):436-48.
3 Discovery and parallel synthesis of a new class of cathepsin K inhibitors. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2951-4.
4 Cathepsin B and L inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2017 Jun;27(6):643-656.
5 An updated patent review of calpain inhibitors (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):17-31.
6 Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
7 New approach for osteoporosis treatment: cathepsin K inhibitor, ONO-5334. Clin Calcium. 2011 Jan;21(1):64-9.
8 The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.
9 Medivir designates MIV-710 a Candidate Drug (CD) for Osteoporosis and Osteoarthritis, 2009
10 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2350).
11 Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional se... J Med Chem. 2005 Dec 1;48(24):7535-43.
12 Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83.
13 2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. J Med Chem. 2007 Feb 22;50(4):591-4.
14 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
15 Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7.
16 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50.
17 Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. J Med Chem. 2002 Sep 12;45(19):4202-11.
18 Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70.
19 Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K. J Med Chem. 2006 Feb 9;49(3):1066-79.
20 Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. J Med Chem. 2005 Dec 1;48(24):7688-707.
21 Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4897-902.
22 Acyclic cyanamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.
23 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
24 A cysteine-type carboxypeptidase, cathepsin X, generates peptide receptor agonists. Int Immunopharmacol. 2010 Jan;10(1):134-9.