Target Information

Target General Infomation
Target ID
T75888
Former ID
TTDS00433
Target Name
Carnitine O-palmitoyltransferase I
Gene Name
CPT1B
Synonyms
CPT; CPT I; CPT-1; CPTI-L; Carnitine o-palmitoyltransferase-1; Carnitine palmitoyl-transferase I; Carnitine palmitoyltransferase I; CPT1B
Target Type
Successful
Disease Angina pectoris [ICD9: 413; ICD10: I20]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Heart failure [ICD9: 428; ICD10: I50]
Nutritional deficiency [ICD9: 260-269; ICD10: E40-E64]
Obesity [ICD9: 278; ICD10: E66]
Psoriasis [ICD9: 696; ICD10: L40]
Function
Catalyzes the transfer of the acyl group of long-chain fatty acid-CoA conjugates onto carnitine, an essential step for the mitochondrial uptake of long-chain fatty acids and their subsequent beta-oxidationin the mitochondrion. Plays an important role in triglyceride metabolism.
BioChemical Class
Acyltransferase
Target Validation
T75888
UniProt ID
Q92523
EC Number
EC 2.3.1.21
Sequence
MAEAHQAVAFQFTVTPDGVDFRLSREALKHVYLSGINSWKKRLIRIKNGILRGVYPGSPT
SWLVVIMATVGSSFCNVDISLGLVSCIQRCLPQGCGPYQTPQTRALLSMAIFSTGVWVTG
IFFFRQTLKLLLCYHGWMFEMHGKTSNLTRIWAMCIRLLSSRHPMLYSFQTSLPKLPVPR
VSATIQRYLESVRPLLDDEEYYRMELLAKEFQDKTAPRLQKYLVLKSWWASNYVSDWWEE
YIYLRGRSPLMVNSNYYVMDLVLIKNTDVQAARLGNIIHAMIMYRRKLDREEIKPVMALG
IVPMCSYQMERMFNTTRIPGKDTDVLQHLSDSRHVAVYHKGRFFKLWLYEGARLLKPQDL
EMQFQRILDDPSPPQPGEEKLAALTAGGRVEWAQARQAFFSSGKNKAALEAIERAAFFVA
LDEESYSYDPEDEASLSLYGKALLHGNCYNRWFDKSFTLISFKNGQLGLNAEHAWADAPI
IGHLWEFVLGTDSFHLGYTETGHCLGKPNPALAPPTRLQWDIPKQCQAVIESSYQVAKAL
ADDVELYCFQFLPFGKGLIKKCRTSPDAFVQIALQLAHFRDRGKFCLTYEASMTRMFREG
RTETVRSCTSESTAFVQAMMEGSHTKADLRDLFQKAAKKHQNMYRLAMTGAGIDRHLFCL
YLVSKYLGVSSPFLAEVLSEPWRLSTSQIPQSQIRMFDPEQHPNHLGAGGGFGPVADDGY
GVSYMIAGENTIFFHISSKFSSSETNAQRFGNHIRKALLDIADLFQVPKAYS
Structure
2LE3
Drugs and Mode of Action
Drug(s) L-Carnitine Drug Info Approved Nutritional deficiency [468010], [536186]
Perhexiline Drug Info Approved Angina pectoris [536403]
SDZ-CPI-975 Drug Info Discontinued in Phase 1 Diabetes [545960]
DB-200 Drug Info Terminated Psoriasis [548567]
Etomoxir Drug Info Terminated Heart failure [533432]
Activator C75 Drug Info [535480]
L-Carnitine Drug Info [537609]
Inhibitor DB-200 Drug Info [533757]
Perhexiline Drug Info [536403]
SDZ-CPI-975 Drug Info [534566]
Modulator Etomoxir Drug Info [533432]
Pathways
KEGG Pathway Fatty acid degradation
Fatty acid metabolism
PPAR signaling pathway
AMPK signaling pathway
Adipocytokine signaling pathway
Glucagon signaling pathway
PathWhiz Pathway Fatty acid Metabolism
Reactome RORA activates gene expression
PPARA activates gene expression
Import of palmitoyl-CoA into the mitochondrial matrix
WikiPathways SIDS Susceptibility Pathways
Mitochondrial LC-Fatty Acid Beta-Oxidation
Nuclear Receptors Meta-Pathway
PPAR Alpha Pathway
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Circadian Clock
Fatty Acid Beta Oxidation
AMPK Signaling
References
Ref 468010(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: 4780).
Ref 533432Etomoxir, a carnitine palmitoyltransferase I inhibitor, protects hearts from fatty acid-induced ischemic injury independent of changes in long chain acylcarnitine. Circ Res. 1988 Dec;63(6):1036-43.
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 536403Perhexiline. Cardiovasc Drug Rev. 2007 Spring;25(1):76-97.
Ref 545960Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005522)
Ref 548567Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026687)
Ref 533432Etomoxir, a carnitine palmitoyltransferase I inhibitor, protects hearts from fatty acid-induced ischemic injury independent of changes in long chain acylcarnitine. Circ Res. 1988 Dec;63(6):1036-43.
Ref 533757Comparison of the effects of carnitine palmitoyltransferase-1 and -2 inhibitors on rat heart hypertrophy. Cardioscience. 1994 Sep;5(3):193-7.
Ref 534566Hypoglycemic effects of a novel fatty acid oxidation inhibitor in rats and monkeys. Am J Physiol. 1998 Feb;274(2 Pt 2):R524-8.
Ref 535480C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502. Epub 2002 Jun 11.
Ref 536403Perhexiline. Cardiovasc Drug Rev. 2007 Spring;25(1):76-97.
Ref 537609Central ghrelin regulates peripheral lipid metabolism in a growth hormone-independent fashion. Endocrinology. 2009 Jul 16.

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