m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00120
 [1], [2], [3]
m6A modification ADAR1 ADAR1 METTL3 Methylation : m6A sites Direct Enhancement RNA modification CTSS CTSS ADAR Methylation : modification sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target Interferon-inducible protein 4 (ADAR1)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Adenosine-to-Inosine editing (A-to-I)
Epigenetic Regulator Interferon-inducible protein 4 (ADAR1) WRITER View Details
Regulated Target Cathepsin S (CTSS) View Details
Crosstalk Relationship m6A  →  A-to-I Enhancement
Crosstalk Mechanism m6A modification directly impacts RNA modification through modulating the expression level of RNA modification regulator
Crosstalk Summary METTL3 methylates Interferon-inducible protein 4 (ADAR1) mRNA, thereby enhancing its protein expression, which subsequently promotes ADAR mediated A-to-I RNA editing of the Cathepsin S (CTSS) transcript.
Responsed Drug RG7625
 Drug Info 
Pathway Response mRNA surveillance pathway hsa03015
RNA degradation hsa03018
Cell Process RNA stability
In-vitro Model
 MGG8 Glioblastoma Homo sapiens CVCL_D1H4
U-87MG ATCC Glioblastoma Homo sapiens CVCL_0022
U-118MG Astrocytoma Homo sapiens CVCL_0633
HUVEC-C Normal Homo sapiens CVCL_2959
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Cathepsin S (CTSS) 60 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name RG7625 Phase 2 [4]
Synonyms
Petesicatib; UNII-A26QO95U37; A26QO95U37; RG-7625; RO-5459072; Petesicatib [INN]; SCHEMBL700776; GTPL9855; KXAAIORSMACJSI-AEFFLSMTSA-N; RO5459072; 2-Pyrrolidinecarboxamide, N-(1-cyanocyclopropyl)-4-((4-(1-methyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)phenyl)sulfonyl)-1-((1-(trifluoromethyl)cyclopropyl)carbonyl)-, (2S,4R)-; 1252637-35-6; (2S,4R)-N-(1-cyanocyclopropyl)-4-[4-(1-methylpyrazol-4-yl)-2-(trifluoromethyl)phenyl]sulfonyl-1-[1-(trifluoromethyl)cyclopropanecarbonyl]pyrrolidine-2-carboxamide; (2s,4r)-4-[4-(1-me
    Click to Show/Hide
MOA Antagonist
External Link
CID: 59543597
TTD: D0DQ2D
DrugBank: DB15297
 Compound Name VBY- 891 Phase 1 [5]
Synonyms
VBY-891
    Click to Show/Hide
MOA Modulator
External Link
TTD: D01REJ
 Compound Name VBY- 036 Phase 1 [6]
Synonyms
VBY-036
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D07ODC
 Compound Name VBY-129 Phase 1 [7]
Synonyms
Cathepsin S inhibitor (oral, psoriasis), Virobay
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D07UKF
 Compound Name SAR-114137 Phase 1 [8]
MOA Inhibitor
External Link
CID: 9828551
TTD: D08KIB
 Compound Name Phenylalanine derivative 1 Patented [9]
Synonyms
PMID27998201-Compound-21
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D01MKD
 Compound Name PMID27998201-Compound-7 Patented [9]
MOA Inhibitor
Activity IC50 = 0.6 nM
External Link
CID: 73294953
TTD: D0JD5W
 Compound Name PMID27998201-Compound-15 Patented [9]
MOA Inhibitor
Activity Ki = 12 nM
External Link
TTD: D0MR9V
 Compound Name Oxotetrahydro-2-H-furo[3.2-b]pyrrol-4(5-H)-yl derivative 1 Patented [9]
Synonyms
PMID27998201-Compound-14
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 38 nM
External Link
CID: 44229370
TTD: D0QM0D
 Compound Name PMID27998201-Compound-6 Patented [9]
MOA Inhibitor
Activity IC50 = 0.29 nM
External Link
TTD: D0X1AF
 Compound Name PMID27998201-Compound-17 Patented [9]
MOA Inhibitor
Activity IC50 = 56 nM
External Link
TTD: D06XTA
 Compound Name PMID27998201-Compound-9 Patented [9]
MOA Inhibitor
Activity Ki = 0.0031 nM
External Link
CID: 78108715
TTD: D04VGR
 Compound Name PMID25399719-Compound-17 Patented [10]
MOA Inhibitor
Activity Ki = 21000 nM
External Link
TTD: D06LLT
 Compound Name PMID27998201-Compound-5 Patented [9]
MOA Inhibitor
Activity Ki < 100 nM
External Link
CID: 46202117
TTD: D05OIU
 Compound Name PMID27998201-Compound-12 Patented [9]
MOA Inhibitor
Activity IC50 = 0.009 nM
External Link
TTD: D06XCD
 Compound Name RG-7236 Discontinued in Phase 1 [5]
Synonyms
RG7236
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0D3KG
 Compound Name RO5461111 Preclinical [11]
MOA Inhibitor
External Link
TTD: DC9J1Y
 Compound Name L-006235-1 Preclinical [12]
Synonyms
294623-49-7; L 006235; CHEMBL426819; N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(2-(4-methylpiperazin-1-yl)thiazol-4-yl)benzamide; L006235; N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide; SCHEMBL6183485; CTK8E9371; BDBM19854; DTXSID90432735; MolPort-023-276-653; BCP28510; ZINC3993799; AKOS024457410; basic piperazine-containing compound, 1; NCGC00371088-01; RT-013466; CRA-013783/L-006235; J-017526; L-006235; L-006,235
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 47000 nM
External Link
CID: 9912381
TTD: D0Z0PR
 Compound Name CRA-028129 Terminated [13]
MOA Inhibitor
External Link
TTD: D0K0IW
 Compound Name 6-(3-(trifluoromethyl)phenyl)picolinonitrile Investigative [14]
Synonyms
CHEMBL1210691; 833457-45-7; SCHEMBL9954071; CTK3D2833; DTXSID80678807; BDBM50322920; 6-[3-(Trifluoromethyl)phenyl]pyridine-2-carbonitrile; 2-Pyridinecarbonitrile, 6-[3-(trifluoromethyl)phenyl]-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2884 nM
External Link
CID: 49863205
TTD: D01IFO
 Compound Name Cbz-Ile-Phe-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL207284
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9000 nM
External Link
CID: 11534772
TTD: D01NCW
 Compound Name N-(1-oxobutan-2-yl)-3-(trifluoromethyl)benzamide Investigative [16]
Synonyms
CHEMBL1288588
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1070 nM
External Link
CID: 52945617
TTD: D02FPU
 Compound Name Cbz-Ile-Pro-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL207670
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 13000 nM
External Link
CID: 11505372
TTD: D05MDE
 Compound Name N-(2-naphthylsulfonyl)-glycyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 38; CHEMBL200338; BDBM20117
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2500 nM
External Link
CID: 11652399
TTD: D07SOQ
 Compound Name AM-3840 Investigative [5]
Synonyms
Cathepsin S inihibitors (oral, autoimmune disease/pain), Amura
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D08WDP
 Compound Name Ac-hPhe-Leu-Gly-LeuVSMe Investigative [15]
Synonyms
CHEMBL209243
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MOA Inhibitor
Activity IC50 = 12000 nM
External Link
CID: 11713852
TTD: D09GZQ
 Compound Name Cbz-Ile-t-ButylGln-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL438612
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MOA Inhibitor
Activity IC50 = 3300 nM
External Link
CID: 11621748
TTD: D09IMK
 Compound Name Cbz-Ile-MetO2-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL383730
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MOA Inhibitor
Activity IC50 = 13000 nM
External Link
CID: 11585523
TTD: D0B3US
 Compound Name Fsn-0503 Investigative [5]
Synonyms
Cathepsin S mAb (cancer), Fusion
    Click to Show/Hide
External Link
TTD: D0G3PK
 Compound Name VBY- 285 Investigative [5]
Synonyms
VBY-285; Cathepsin S inhibitor (neuropathic pain, oral), Virobay
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0J0HV
 Compound Name Cbz-Glu(OtBu)-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL208015
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3000 nM
External Link
CID: 11621207
TTD: D0K0KT
 Compound Name 2-[(2',3',4'-TRIFLUOROBIPHENYL-2-YL)OXY]ETHANOL Investigative [18]
Synonyms
TF5
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MOA Inhibitor
External Link
CID: 46937163
TTD: D0M8WX
DrugBank: DB08611
 Compound Name BF/PC-18 Investigative [5]
Synonyms
PC18-BF; Cathepsin S inhibitor (inflammation), Biofrontera
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0P5RJ
 Compound Name Cbz-Ile-hPhe-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL446443
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10000 nM
External Link
CID: 11714476
TTD: D0RL4S
 Compound Name JNJ-10329670 Investigative [5]
Synonyms
Cathepsin S inhibitors (autoimmune disease); Cathepsin S inhibitors (autoimmune disease), J&J PRD; Cathepsin S inhibitors (autoimmune disease), Johnson & Johnson
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 100 nM
External Link
CID: 10168449
TTD: D0V5LJ
 Compound Name Clik60 Investigative [19]
MOA Inhibitor
External Link
TTD: D0Y8LO
 Compound Name 4-cyclooctyl-6-propylpyrimidine-2-carbonitrile Investigative [20]
Synonyms
CHEMBL1077194
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MOA Inhibitor
Activity IC50 = 2239 nM
External Link
CID: 46881498
TTD: D01JGB
 Compound Name 4-propyl-6-m-tolylpyrimidine-2-carbonitrile Investigative [21]
Synonyms
CHEMBL1082859; SCHEMBL4453859
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MOA Inhibitor
Activity IC50 = 950 nM
External Link
CID: 46881451
TTD: D04BGT
 Compound Name Ac-hPhe-Leu-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL207579
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MOA Inhibitor
Activity IC50 = 6900 nM
External Link
CID: 11556056
TTD: D05VEV
 Compound Name P2,P3 Ketoamide derivative Investigative [22]
Synonyms
CHEMBL186650; SCHEMBL14260244; AAYZJXOZLLKNGZ-DEOSSOPVSA-N; BDBM50152530
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MOA Inhibitor
Activity IC50 = 130 nM
External Link
CID: 10129151
TTD: D05WZF
 Compound Name Ac-hPhe-Leu-Phe-LeuVSMe Investigative [15]
Synonyms
CHEMBL379669; BDBM50186702
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MOA Inhibitor
Activity IC50 = 150 nM
External Link
CID: 11693148
TTD: D06NEB
 Compound Name PMID22686657C(R)-26 Investigative [23]
Synonyms
GTPL6535; BDBM50392215
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MOA Inhibitor
Activity Ki = 0.55 nM
External Link
CID: 60148519
TTD: D06WQP
 Compound Name N-(tert-butoxycarbonyl)-norvalyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 6; CHEMBL383816; BDBM20086; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]butyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 900 nM
External Link
CID: 11514386
TTD: D0A7ER
 Compound Name Cbz-Ile-Leu-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL207403
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 700 nM
External Link
CID: 11534625
TTD: D0I0MU
 Compound Name N-(tert-butoxycarbonyl)-tyrosyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 23; CHEMBL371893; BDBM20102; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]-2-(4-hydroxyphenyl)ethyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 970 nM
External Link
CID: 11551481
TTD: D0JF8D
 Compound Name Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe Investigative [15]
Synonyms
CHEMBL207196
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MOA Inhibitor
Activity IC50 = 7100 nM
External Link
CID: 11513217
TTD: D0QY3R
 Compound Name 4-cycloheptyl-6-propylpyrimidine-2-carbonitrile Investigative [20]
Synonyms
CHEMBL1085423; SCHEMBL5796281
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
CID: 11694425
TTD: D0U4TY
 Compound Name N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 9; CHEMBL197113; BDBM20088; tert-butyl N-[(1S,2R)-1-[(cyanomethyl)carbamoyl]-2-methylbutyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 4100 nM
External Link
CID: 23648531
TTD: D01YNC
 Compound Name N-(tert-butoxycarbonyl)-valyl-glycine-nitrile Investigative [17]
Synonyms
N-(tert-butoxycarbonyl)-L-valyl-glycine-nitrile; 191033-03-1; dipeptide-derived nitrile, 5; CHEMBL200004; BDBM20085; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]-2-methylpropyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 6200 nM
External Link
CID: 14774521
TTD: D06VIP
 Compound Name N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 13; CHEMBL383584; BDBM20092; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]pentyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 550 nM
External Link
CID: 11637576
TTD: D07FLB
 Compound Name N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile Investigative [17]
Synonyms
phenylalanine derivative, 44; CHEMBL200235; BDBM20120
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MOA Inhibitor
Activity Ki = 240 nM
External Link
CID: 11696652
TTD: D07RSA
 Compound Name N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 7; CHEMBL200160; SCHEMBL6257676; BDBM20087; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]-3-methylbutyl]carbamate
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MOA Inhibitor
Activity Ki = 130 nM
External Link
CID: 11492732
TTD: D09AHN
 Compound Name N-acetyl-phenylalanyl-glycine-nitrile Investigative [17]
Synonyms
phenylalanine derivative, 42; CHEMBL197181; SCHEMBL15634553; BDBM20118; ITHLBMBCVIAAIX-LBPRGKRZSA-N; ZINC13676602; (N-acetyl-l-phenylalanyl)aminoacetonitrile; SR-03000002938; SR-03000002938-1; (S)-2-Acetamido-N-(cyanomethyl)-3-phenylpropanamide
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MOA Inhibitor
Activity Ki = 1400 nM
External Link
CID: 11086036
TTD: D0A8OV
 Compound Name N-(benzyloxycarbonyl)-leucyl-glycine-nitrile Investigative [17]
Synonyms
dipeptidyl nitrile, 1; Cbz-Leu-NH-CH2-CN; JMC487688 Compound 8; CHEMBL200161; SCHEMBL6183068; BDBM19768; UFXQLUZNMRVTPU-AWEZNQCLSA-N; 2-[(Z-L-Leu-)Amino]ethanenitrile; benzyl (S)-1-cyanomethylcarbamoyl-3-methylbutylcarbamate; benzyl N-[(1S)-1-[(cyanomethyl)carbamoyl]-3-methylbutyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 130 nM
External Link
CID: 11702208
TTD: D0G8OD
 Compound Name N-benzoyl-phenylalanyl-glycine-nitrile Investigative [17]
Synonyms
phenylalanine derivative, 43; SCHEMBL5517755; CHEMBL371466; BDBM20119
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MOA Inhibitor
Activity Ki = 77 nM
External Link
CID: 11702265
TTD: D0JN8Q
 Compound Name N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile Investigative [17]
Synonyms
dipeptide-derived nitrile, 12; CHEMBL381847; BDBM20091; tert-butyl N-[(1S)-1-[(cyanomethyl)carbamoyl]-3-(methylsulfanyl)propyl]carbamate
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 660 nM
External Link
CID: 11709032
TTD: D0U0XG
 Compound Name E-64 Investigative [24]
Synonyms
66701-25-5; CHEMBL189382; AC1NEEQI; SCHEMBL13283063; HMS3369L13; trans-Epoxysuccinyl-leucylamido-[4-guanidino]butane; [L-3-trans-carboxy-oxiran-2-carbonyl]-Leu-agmatin; trans-Epoxysuccinyl-leucylamido- [4-guanidino]butane; [L -3-trans-carboxy- oxiran-2-carbonyl]-Leu-agmatin; 3-({1-[(4-carbamimidamidobutyl)carbamoyl]-3-methylbutyl}carbamoyl)oxirane-2-carboxylic acid; 3-[[1-[4-(diaminomethylideneamino)butylamino]-4-methyl-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7 nM
External Link
CID: 123985
TTD: D09FGQ
 Compound Name L-873724 Investigative [25]
Synonyms
UNII-29250PP3ON; 603139-12-4; CHEMBL437501; 29250PP3ON; (2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]Pentanamide; (2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide; VYFDSJLOCIGIKP-SFTDATJTSA-N; GTPL7860; SCHEMBL2157182; BDBM19489; (+)-L-873724; ZINC34802820; CS-6814; HY-50887; Pentanamide, N-(cyanomethyl)-4-methyl-2-(((1S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)(1,1'-biphenyl)-4-yl)eth
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 95 nM
External Link
CID: 9913088
TTD: D0D0LD
 Compound Name GNF-PF-5434 Investigative [26]
Synonyms
CHEMBL486232; N~2~-(MORPHOLIN-4-YLCARBONYL)-N~1~-[(1S,2E)-1-(2-PHENYLETHYL)-3-(PHENYLSULFONYL)PROP-2-ENYL]-D-LEUCINAMIDE; MORPHOLINE-4-CARBOXYLIC ACID (1-(3-BENZENESULFONYL-1-PHENETHYLALLYLCARBAMOYL)-3-METHYLBUTYL)-AMIDE; N-[(1S)-1-[[(E,1S)-3-(benzenesulfonyl)-1-phenethyl-allyl]carbamoyl]-3-methyl-butyl]morpholine-4-carboxamide; AC1NRAGB; SCHEMBL7352997; BDBM50243232; K-11017; 4-Morpholinecarboxamide, N-[(1S)-3-methyl-1-[[[(1S,2E)-1-(2-phenylethyl)-3-(phenylsulfonyl)-2-propenyl]amino]carbonyl]butyl]-
    Click to Show/Hide
MOA Inhibitor
Activity Ki < 0.1 nM
External Link
CID: 5287864
TTD: D0L9VP
 Compound Name Fucose Investigative [27]
Synonyms
L-galactomethylose; 6-Desoxygalactose; SCHEMBL13092958; AKOS030212707
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MOA Inhibitor
External Link
CID: 17106
TTD: D0G6XS
References
Ref 1 N?-Methyladenosine Landscape of Glioma Stem-Like Cells: METTL3 Is Essential for the Expression of Actively Transcribed Genes and Sustenance of the Oncogenic Signaling. Genes (Basel). 2019 Feb 13;10(2):141. doi: 10.3390/genes10020141.
Ref 2 ADAR1 is a new target of METTL3 and plays a pro-oncogenic role in glioblastoma by an editing-independent mechanism. Genome Biol. 2021 Jan 28;22(1):51. doi: 10.1186/s13059-021-02271-9.
Ref 3 Adenosine-to-inosine RNA editing controls cathepsin S expression in atherosclerosis by enabling HuR-mediated post-transcriptional regulation. Nat Med. 2016 Oct;22(10):1140-1150. doi: 10.1038/nm.4172. Epub 2016 Sep 5.
Ref 4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 5 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: 2353).
Ref 6 Clinical pipeline report, company report or official report of ViroBay.
Ref 7 Clinical pipeline report, company report or official report of ViroBay.
Ref 8 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.
Ref 9 Cathepsin B and L inhibitors: a patent review (2010 - present). Expert Opin Ther Pat. 2017 Jun;27(6):643-656. doi: 10.1080/13543776.2017.1272572. Epub 2016 Dec 23.
Ref 10 An updated patent review of calpain inhibitors (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):17-31.
Ref 11 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 Feb;74(2):452-63.
Ref 12 Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43. doi: 10.1021/jm0504961.
Ref 13 Phase I clinical trial for cathepsin S inhibitor for psoriasis begins. Celera Genomics. 2005.
Ref 14 4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4507-10.
Ref 15 Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors. J Med Chem. 2006 May 18;49(10):2953-68. doi: 10.1021/jm058289o.
Ref 16 Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4.
Ref 17 Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. J Med Chem. 2005 Dec 1;48(24):7688-707.
Ref 18 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 19 Cathepsin S inhibitor prevents autoantigen presentation and autoimmunity. J Clin Invest. 2002 Aug;110(3):361-9.
Ref 20 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.
Ref 21 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50.
Ref 22 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.
Ref 23 Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F. J Med Chem. 2012 Jun 28;55(12):5982-6.
Ref 24 Baculoviral expression and characterization of rodent cathepsin S. Protein Expr Purif. 2001 Oct;23(1):45-54.
Ref 25 The identification of potent, selective, and bioavailable cathepsin S inhibitors. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. doi: 10.1016/j.bmcl.2007.06.023. Epub 2007 Jun 10.
Ref 26 Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. doi: 10.1016/j.bmc.2008.02.002. Epub 2008 Feb 7.
Ref 27 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.