Target Information
Target General Infomation | |||||
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Target ID |
T86161
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Former ID |
TTDR00015
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Target Name |
Prolyl endopeptidase
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Gene Name |
PREP
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Synonyms |
PE; Post-proline cleaving enzyme; PREP
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Target Type |
Clinical Trial
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Disease | Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3] | ||||
Celiac disease [ICD9: 579; ICD10: K90.0] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Function |
Cleaves peptide bonds on the C-terminal side of prolyl residues within peptides that are up to approximately 30 amino acids long.
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BioChemical Class |
Peptidase
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Target Validation |
T86161
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UniProt ID | |||||
EC Number |
EC 3.4.21.26
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Sequence |
MLSLQYPDVYRDETAVQDYHGHKICDPYAWLEDPDSEQTKAFVEAQNKITVPFLEQCPIR
GLYKERMTELYDYPKYSCHFKKGKRYFYFYNTGLQNQRVLYVQDSLEGEARVFLDPNILS DDGTVALRGYAFSEDGEYFAYGLSASGSDWVTIKFMKVDGAKELPDVLERVKFSCMAWTH DGKGMFYNSYPQQDGKSDGTETSTNLHQKLYYHVLGTDQSEDILCAEFPDEPKWMGGAEL SDDGRYVLLSIREGCDPVNRLWYCDLQQESSGIAGILKWVKLIDNFEGEYDYVTNEGTVF TFKTNRQSPNYRVINIDFRDPEESKWKVLVPEHEKDVLEWIACVRSNFLVLCYLHDVKNI LQLHDLTTGALLKTFPLDVGSIVGYSGQKKDTEIFYQFTSFLSPGIIYHCDLTKEELEPR VFREVTVKGIDASDYQTVQIFYPSKDGTKIPMFIVHKKGIKLDGSHPAFLYGYGGFNISI TPNYSVSRLIFVRHMGGILAVANIRGGGEYGETWHKGGILANKQNCFDDFQCAAEYLIKE GYTSPKRLTINGGSNGGLLVAACANQRPDLFGCVIAQVGVMDMLKFHKYTIGHAWTTDYG CSDSKQHFEWLVKYSPLHNVKLPEADDIQYPSMLLLTADHDDRVVPLHSLKFIATLQYIV GRSRKQSNPLLIHVDTKAGHGAGKPTAKVIEEVSDMFAFIARCLNVDWIP |
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Drugs and Mode of Action | |||||
Drug(s) | ALV-003 | Drug Info | Phase 2 | Celiac disease | [522758] |
ONO-1603 | Drug Info | Phase 2 | Cognitive disorders | [545099] | |
S-17092-1 | Drug Info | Phase 1 | Cognitive disorders | [546918] | |
S 17092 | Drug Info | Clinical trial | Non-small cell lung cancer | [541690] | |
JTP-4819 | Drug Info | Discontinued in Phase 2 | Cognitive disorders | [546065] | |
Z-321 | Drug Info | Discontinued in Phase 1 | Parkinson's disease | [545389] | |
BAICALIN | Drug Info | Terminated | Human immunodeficiency virus infection | [546402] | |
Y-29794 | Drug Info | Terminated | Discovery agent | [544947] | |
Inhibitor | 1-Hydroxy-1-Thio-Glycerol | Drug Info | [551393] | ||
ARI-3531 | Drug Info | [532317] | |||
BAICALEIN | Drug Info | [529614] | |||
BAICALIN | Drug Info | [530628] | |||
Double Oxidized Cysteine | Drug Info | [551393] | |||
Monothioglycerol | Drug Info | [551393] | |||
S 17092 | Drug Info | [530628] | |||
S-17092-1 | Drug Info | [526549] | |||
S-Oxy Cysteine | Drug Info | [551391] | |||
Y-29794 | Drug Info | [530628] | |||
Z-Pro-Prolinal | Drug Info | [551374] | |||
Modulator | ALV-003 | Drug Info | [530542] | ||
JTP-4819 | Drug Info | [534339] | |||
ONO-1603 | Drug Info | [534253] | |||
Z-321 | Drug Info | [534340] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Renin-angiotensin system | ||||
PANTHER Pathway | Vasopressin synthesis | ||||
References | |||||
Ref 522758 | ClinicalTrials.gov (NCT00959114) Safety and Efficacy of ALV003 for the Treatment of Celiac Disease. U.S. National Institutes of Health. | ||||
Ref 541690 | (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. (Ligand id: 6565). | ||||
Ref 544947 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001631) | ||||
Ref 545099 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002119) | ||||
Ref 545389 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003089) | ||||
Ref 546065 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006163) | ||||
Ref 526549 | Effect of S 17092, a novel prolyl endopeptidase inhibitor, on substance P and alpha-melanocyte-stimulating hormone breakdown in the rat brain. J Neurochem. 2003 Mar;84(5):919-29. | ||||
Ref 529614 | Bioorg Med Chem. 2008 Aug 1;16(15):7516-24. Epub 2008 Apr 29.Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor. | ||||
Ref 530542 | The effects of ALV003 pre-digestion of gluten on immune response and symptoms in celiac disease in vivo. Clin Immunol. 2010 Mar;134(3):289-95. | ||||
Ref 530628 | J Med Chem. 2010 May 13;53(9):3423-38.Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors. | ||||
Ref 532317 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem. 2013 May 9;56(9):3467-77. | ||||
Ref 534253 | ONO-1603, a potential antidementia drug, shows neuroprotective effects and increases m3-muscarinic receptor mRNA levels in differentiating rat cerebellar granule neurons. Neurosci Lett. 1996 Aug 23;214(2-3):151-4. | ||||
Ref 534339 | A novel prolyl endopeptidase inhibitor, JTP-4819, with potential for treating Alzheimer's disease. Behav Brain Res. 1997 Feb;83(1-2):147-51. | ||||
Ref 534340 | Z-321, a prolyl endopeptidase inhibitor, augments the potentiation of synaptic transmission in rat hippocampal slices. Behav Brain Res. 1997 Feb;83(1-2):213-6. |
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