Target Information

Target General Infomation
Target ID
T86161
Former ID
TTDR00015
Target Name
Prolyl endopeptidase
Gene Name
PREP
Synonyms
PE; Post-proline cleaving enzyme; PREP
Target Type
Clinical Trial
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.
BioChemical Class
Peptidase
Target Validation
T86161
UniProt ID
P48147
EC Number
EC 3.4.21.26
Sequence
MLSLQYPDVYRDETAVQDYHGHKICDPYAWLEDPDSEQTKAFVEAQNKITVPFLEQCPIR
GLYKERMTELYDYPKYSCHFKKGKRYFYFYNTGLQNQRVLYVQDSLEGEARVFLDPNILS
DDGTVALRGYAFSEDGEYFAYGLSASGSDWVTIKFMKVDGAKELPDVLERVKFSCMAWTH
DGKGMFYNSYPQQDGKSDGTETSTNLHQKLYYHVLGTDQSEDILCAEFPDEPKWMGGAEL
SDDGRYVLLSIREGCDPVNRLWYCDLQQESSGIAGILKWVKLIDNFEGEYDYVTNEGTVF
TFKTNRQSPNYRVINIDFRDPEESKWKVLVPEHEKDVLEWIACVRSNFLVLCYLHDVKNI
LQLHDLTTGALLKTFPLDVGSIVGYSGQKKDTEIFYQFTSFLSPGIIYHCDLTKEELEPR
VFREVTVKGIDASDYQTVQIFYPSKDGTKIPMFIVHKKGIKLDGSHPAFLYGYGGFNISI
TPNYSVSRLIFVRHMGGILAVANIRGGGEYGETWHKGGILANKQNCFDDFQCAAEYLIKE
GYTSPKRLTINGGSNGGLLVAACANQRPDLFGCVIAQVGVMDMLKFHKYTIGHAWTTDYG
CSDSKQHFEWLVKYSPLHNVKLPEADDIQYPSMLLLTADHDDRVVPLHSLKFIATLQYIV
GRSRKQSNPLLIHVDTKAGHGAGKPTAKVIEEVSDMFAFIARCLNVDWIP
Drugs and Mode of Action
Drug(s) ALV-003 Drug Info Phase 2 Celiac disease [1]
ONO-1603 Drug Info Phase 2 Cognitive disorders [2]
S-17092-1 Drug Info Phase 1 Cognitive disorders [3]
S 17092 Drug Info Clinical trial Non-small cell lung cancer [4]
JTP-4819 Drug Info Discontinued in Phase 2 Cognitive disorders [5]
Z-321 Drug Info Discontinued in Phase 1 Parkinson's disease [6]
BAICALIN Drug Info Terminated Human immunodeficiency virus infection [7]
Y-29794 Drug Info Terminated Discovery agent [8]
Inhibitor 1-Hydroxy-1-Thio-Glycerol Drug Info [9]
ARI-3531 Drug Info [10]
BAICALEIN Drug Info [11]
BAICALIN Drug Info [12]
Double Oxidized Cysteine Drug Info [9]
Monothioglycerol Drug Info [9]
S 17092 Drug Info [12]
S-17092-1 Drug Info [13]
S-Oxy Cysteine Drug Info [14]
Y-29794 Drug Info [12]
Z-Pro-Prolinal Drug Info [15]
Modulator ALV-003 Drug Info [16]
JTP-4819 Drug Info [17]
ONO-1603 Drug Info [18]
Z-321 Drug Info [19]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Renin-angiotensin system
PANTHER Pathway Vasopressin synthesis
References
REF 1ClinicalTrials.gov (NCT00959114) Safety and Efficacy of ALV003 for the Treatment of Celiac Disease. U.S. National Institutes of Health.
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002119)
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011104)
REF 4(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 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006163)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003089)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007921)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001631)
REF 9How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 10Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem. 2013 May 9;56(9):3467-77.
REF 11Bioorg 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 12J Med Chem. 2010 May 13;53(9):3423-38.Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
REF 13Effect 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 14DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
REF 15The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 16The 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 17A novel prolyl endopeptidase inhibitor, JTP-4819, with potential for treating Alzheimer's disease. Behav Brain Res. 1997 Feb;83(1-2):147-51.
REF 18ONO-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 19Z-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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