Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTMX39J)

• DTT Name: Matrix metalloproteinase-1 (MMP-1)
• Synonyms: Interstitial collagenase; Fibroblast collagenase; CLG
• Gene Name: MMP1
• DTT Type: Successful target; [1]
• BioChemical Class: Peptidase
• UniProt ID: MMP1_HUMAN
• TTD ID: T52450
• EC Number: EC 3.4.24.7
• Sequence:
  MHSFPPLLLLLFWGVVSHSFPATLETQEQDVDLVQKYLEKYYNLKNDGRQVEKRRNSGPV
  VEKLKQMQEFFGLKVTGKPDAETLKVMKQPRCGVPDVAQFVLTEGNPRWEQTHLTYRIEN
  YTPDLPRADVDHAIEKAFQLWSNVTPLTFTKVSEGQADIMISFVRGDHRDNSPFDGPGGN
  LAHAFQPGPGIGGDAHFDEDERWTNNFREYNLHRVAAHELGHSLGLSHSTDIGALMYPSY
  TFSGDVQLAQDDIDGIQAIYGRSQNPVQPIGPQTPKACDSKLTFDAITTIRGEVMFFKDR
  FYMRTNPFYPEVELNFISVFWPQLPNGLEAAYEFADRDEVRFFKGNKYWAVQGQNVLHGY
  PKDIYSSFGFPRTVKHIDAALSEENTGKTYFFVANKYWRYDEYKRSMDPGYPKMIAHDFP
  GIGHKVDAVFMKDGFFYFFHGTRQYKFDPKTKRILTLQKANSWFNCRKN
• Function: Cleaves collagens of types VII and X. In case of HIV infection, interacts and cleaves the secreted viral Tat protein, leading to a decrease in neuronal Tat's mediated neurotoxicity. Cleaves collagens of types I, II, and III at one site in the helical domain.
• KEGG Pathway:
  PPAR signaling pathway (hsa03320)
  Pathways in cancer (hsa05200)
  Bladder cancer (hsa05219)
  Rheumatoid arthritis (hsa05323)
• Reactome Pathway:
  Degradation of the extracellular matrix (R-HSA-1474228)
  Activation of Matrix Metalloproteinases (R-HSA-1592389)
  Basigin interactions (R-HSA-210991)
  Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) (R-HSA-381426)
  Collagen degradation (R-HSA-1442490)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Prinomastat	DM9HOKG	Lung cancer	2C25.0	Approved	[1]

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CIPEMASTAT	DM803GL	Rheumatoid arthritis	FA20	Phase 3	[2]
Marimastat	DM6V34C	Pancreatic cancer	2C10	Phase 3	[3]
Apratastat	DM8W4N9	Rheumatoid arthritis	FA20	Phase 2	[4]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID29130358-Compound-Figure10(2a)	DMFWXPS	N. A.	N. A.	Patented	[5]
PMID29130358-Compound-Figure18(14a)	DMHIBTZ	N. A.	N. A.	Patented	[5]

10 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS 275291	DMKSFPE	Kaposi sarcoma	2B57	Discontinued in Phase 3	[6]
GM6001	DM7V9CT	Corneal ulcer	9A76	Discontinued in Phase 2	[7]
RS-130830	DMOTANY	Hepatitis C virus infection	1E51.1	Discontinued in Phase 2	[8]
XL784	DMICR39	Diabetic nephropathy	GB61.Z	Discontinued in Phase 2	[9]
BB-1101	DM7GH5Z	Multiple sclerosis	8A40	Terminated	[10]
BB-3644	DM7YRFE	Solid tumour/cancer	2A00-2F9Z	Terminated	[11]
L-696418	DMV785R	N. A.	N. A.	Terminated	[12]
Ro-31-4724	DM8B9YT	Arthritis	FA20	Terminated	[13]
RO-319790	DML3NEU	Rheumatoid arthritis	FA20	Terminated	[14]
SC-44463	DMBPNKT	N. A.	N. A.	Terminated	[15]

22 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol	DM206M1	Discovery agent	N.A.	Investigative	[16]
3-(4-Methoxy-benzenesulfonyl)-hexane-1-thiol	DMRLAX8	Discovery agent	N.A.	Investigative	[17]
3-(4-Methoxy-benzenesulfonyl)-pentane-1-thiol	DM854IG	Discovery agent	N.A.	Investigative	[17]
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol	DMBKDZ3	Discovery agent	N.A.	Investigative	[16]
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol	DM2HBGL	Discovery agent	N.A.	Investigative	[17]
3-Benzenesulfinyl-heptanoic acid hydroxyamide	DMQXD0N	Discovery agent	N.A.	Investigative	[18]
3-Benzenesulfonyl-heptanoic acid hydroxyamide	DM7XDCF	Discovery agent	N.A.	Investigative	[18]
3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide	DMJSOTE	Discovery agent	N.A.	Investigative	[18]
4-(4-Butoxy-phenyl)-N-hydroxy-4-oxo-butyramide	DMNGDOM	Discovery agent	N.A.	Investigative	[19]
4-(4-Methoxy-benzenesulfonyl)-butane-2-thiol	DM5PTB9	Discovery agent	N.A.	Investigative	[17]
4-Butoxy-N-hydroxycarbamoylmethyl-benzamide	DMMGK2B	Discovery agent	N.A.	Investigative	[19]
METHYLAMINO-PHENYLALANYL-LEUCYL-HYDROXAMIC ACID	DM9JECY	Discovery agent	N.A.	Investigative	[20]
MMI270	DM38N2K	Discovery agent	N.A.	Investigative	[21]
N-(Ethylphosphoryl)-L-isoleucyl-L-Trp-NHCH3	DMJ6U4H	Discovery agent	N.A.	Investigative	[22]
N-Hydroxy-4-(4-methoxy-phenyl)-4-oxo-butyramide	DMQN6CL	Discovery agent	N.A.	Investigative	[19]
N-Hydroxy-4-oxo-4-(4-phenoxy-phenyl)-butyramide	DMQSWO8	Discovery agent	N.A.	Investigative	[19]
N-Hydroxycarbamoylmethyl-4-methoxy-benzamide	DM41JIB	Discovery agent	N.A.	Investigative	[19]
N-Hydroxycarbamoylmethyl-4-phenoxy-benzamide	DMDTX4L	Discovery agent	N.A.	Investigative	[19]
PKF-242-484	DMNDLAS	Discovery agent	N.A.	Investigative	[23]
Ro-37-9790	DM83QMZ	Discovery agent	N.A.	Investigative	[24]
RS-39066	DM2SCM7	Discovery agent	N.A.	Investigative	[25]
SR-973	DMU48OD	Discovery agent	N.A.	Investigative	[26]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Sarcoma	2C82	Muscle tissue	7.25E-65	0.99	3.23
Rheumatoid arthritis	FA20	Synovial tissue	2.10E-02	5.07	1.67
Prostate cancer	2C82	Prostate	7.68E-01	0.32	0.19
Lung cancer	2C82	Lung tissue	2.68E-70	4.53	2.57

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