Target Information
| Target General Information | Top | |||||
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| Target ID |
T45151
(Former ID: TTDI01754)
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| Target Name |
Plasminogen activator inhibitor (PAI)
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| Synonyms |
Serpin; PAI
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| Gene Name |
SERPINE1; SERPINB2; SERPINA5
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Alzheimer disease [ICD-11: 8A20] | |||||
| Function |
Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation offibrinolysis.
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| UniProt ID | ||||||
| Sequence |
MQMSPALTCLVLGLALVFGEGSAVHHPPSYVAHLASDFGVRVFQQVAQASKDRNVVFSPY
GVASVLAMLQLTTGGETQQQIQAAMGFKIDDKGMAPALRHLYKELMGPWNKDEISTTDAI FVQRDLKLVQGFMPHFFRLFRSTVKQVDFSEVERARFIINDWVKTHTKGMISNLLGKGAV DQLTRLVLVNALYFNGQWKTPFPDSSTHRRLFHKSDGSTVSVPMMAQTNKFNYTEFTTPD GHYYDILELPYHGDTLSMFIAAPYEKEVPLSALTNILSAQLISHWKGNMTRLPRLLVLPK FSLETEVDLRKPLENLGMTDMFRQFQADFTSLSDQEPLHVAQALQKVKIEVNESGTVASS STAVIVSARMAPEEIIMDRPFLFVVRHNPTGTVLFMGQVMEP Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Aleplasinin | Drug Info | Phase 1 | Alzheimer disease | [2] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | BX-044 | Drug Info | Terminated | Thrombosis | [3] | |
| 2 | T-686 | Drug Info | Terminated | Arteriosclerosis | [4] | |
| 3 | XR-1853 | Drug Info | Terminated | Thrombosis | [5] | |
| 4 | XR-5082 | Drug Info | Terminated | Thrombosis | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 4 Inhibitor drugs | + | ||||
| 1 | Aleplasinin | Drug Info | [1] | |||
| 2 | BX-044 | Drug Info | [7] | |||
| 3 | T-686 | Drug Info | [8] | |||
| 4 | XR-5082 | Drug Info | [10] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | XR-1853 | Drug Info | [9] | |||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | HIF-1 signaling pathway | |||||
| 2 | p53 signaling pathway | |||||
| 3 | Hippo signaling pathway | |||||
| 4 | Complement and coagulation cascades | |||||
| 5 | Chagas disease (American trypanosomiasis) | |||||
| References | Top | |||||
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| REF 1 | CN patent application no. 102046168, Pai-1 expression and activity inhibitors for the treatment of ocular disorders. | |||||
| REF 2 | ClinicalTrials.gov (NCT00739037) Study Evaluating PAZ-417 in Cerebrospinal Fluid in Subjects With Alzheimer's Disease. U.S. National Institutes of Health. | |||||
| REF 3 | Inhibition of PAI-1: a new anti-thrombotic approach. Curr Drug Targets Cardiovasc Haematol Disord. 2002 Jun;2(1):27-42. | |||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008057) | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006899) | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006901) | |||||
| REF 7 | Characterization of a small molecule PAI-1 inhibitor, ZK4044. Thromb Res. 2005;115(4):341-50. | |||||
| REF 8 | T-686, a novel inhibitor of plasminogen activator inhibitor-1, inhibits thrombosis without impairment of hemostasis in rats. Eur J Pharmacol. 1997 Jul 9;330(2-3):151-6. | |||||
| REF 9 | Characterization and comparative evaluation of a novel PAI-1 inhibitor. Thromb Haemost. 2002 Jul;88(1):137-43. | |||||
| REF 10 | Evaluation of a low molecular weight modulator of human plasminogen activator inhibitor-1 activity. Thromb Haemost. 1996 May;75(5):808-15. | |||||
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