Target General Infomation
Target ID
T75888 (Former ID: TTDS00433)
Target Name
Carnitine O-palmitoyltransferase I (CPT1B)
Synonyms
KIAA1670; Carnitine palmitoyltransferase I-like protein; Carnitine palmitoyltransferase I; Carnitine palmitoyltransferase 1B; Carnitine palmitoyl-transferase I; Carnitine o-palmitoyltransferase-1; Carnitine O-palmitoyltransferase I, muscle isoform; Carnitine O-palmitoyltransferase 1, muscle isoform; CPTI-M; CPTI-L; CPT1-M; CPT-1; CPT I; CPT
Gene Name
CPT1B
Target Type
Successful target
[1]
Disease [+] 3 Target-related Diseases +
1 Angina pectoris [ICD-11: BA40]
2 Mild neurocognitive disorder [ICD-11: 6D71]
3 Nutritional deficiency [ICD-11: 5B50-5B71]
Function
mitochondrial outer membrane, mitochondrion, carnitine O-palmitoyltransferase activity, carnitine metabolic process, carnitine shuttle, fatty acid beta-oxidation, long-chain fatty acid transport.
BioChemical Class
Acyltransferase
UniProt ID
CPT1B_HUMAN
EC Number
EC 2.3.1.21
Sequence
MAEAHQAVAFQFTVTPDGVDFRLSREALKHVYLSGINSWKKRLIRIKNGILRGVYPGSPT
SWLVVIMATVGSSFCNVDISLGLVSCIQRCLPQGCGPYQTPQTRALLSMAIFSTGVWVTG
IFFFRQTLKLLLCYHGWMFEMHGKTSNLTRIWAMCIRLLSSRHPMLYSFQTSLPKLPVPR
VSATIQRYLESVRPLLDDEEYYRMELLAKEFQDKTAPRLQKYLVLKSWWASNYVSDWWEE
YIYLRGRSPLMVNSNYYVMDLVLIKNTDVQAARLGNIIHAMIMYRRKLDREEIKPVMALG
IVPMCSYQMERMFNTTRIPGKDTDVLQHLSDSRHVAVYHKGRFFKLWLYEGARLLKPQDL
EMQFQRILDDPSPPQPGEEKLAALTAGGRVEWAQARQAFFSSGKNKAALEAIERAAFFVA
LDEESYSYDPEDEASLSLYGKALLHGNCYNRWFDKSFTLISFKNGQLGLNAEHAWADAPI
IGHLWEFVLGTDSFHLGYTETGHCLGKPNPALAPPTRLQWDIPKQCQAVIESSYQVAKAL
ADDVELYCFQFLPFGKGLIKKCRTSPDAFVQIALQLAHFRDRGKFCLTYEASMTRMFREG
RTETVRSCTSESTAFVQAMMEGSHTKADLRDLFQKAAKKHQNMYRLAMTGAGIDRHLFCL
YLVSKYLGVSSPFLAEVLSEPWRLSTSQIPQSQIRMFDPEQHPNHLGAGGGFGPVADDGY
GVSYMIAGENTIFFHISSKFSSSETNAQRFGNHIRKALLDIADLFQVPKAYS
Drugs and Modes of Action
Approved Drug(s) [+] 2 Approved Drugs +
1 Levacecarnine hci Drug Info Approved Nutritional deficiency [2], [3], [4]
2 Perhexiline Drug Info Approved Angina pectoris [1]
Discontinued Drug(s) [+] 3 Discontinued Drugs +
1 SDZ-CPI-975 Drug Info Discontinued in Phase 1 Diabetic complication [5]
2 DB-200 Drug Info Terminated Psoriasis vulgaris [6]
3 Etomoxir Drug Info Terminated Heart failure [7]
Mode of Action [+] 3 Modes of Action +
Activator [+] 2 Activator drugs +
1 Levacecarnine hci Drug Info [8]
2 C75 Drug Info [11]
Inhibitor [+] 3 Inhibitor drugs +
1 Perhexiline Drug Info [1]
2 SDZ-CPI-975 Drug Info [9]
3 DB-200 Drug Info [10]
Modulator [+] 1 Modulator drugs +
1 Etomoxir Drug Info [7]
Target Regulators
Target-regulating Transcription Factors
Target Affiliated Biological Pathways
KEGG Pathway [+] 6 KEGG Pathways +
1 Fatty acid degradation
2 Fatty acid metabolism
3 PPAR signaling pathway
4 AMPK signaling pathway
5 Adipocytokine signaling pathway
6 Glucagon signaling pathway
Pathwhiz Pathway [+] 1 Pathwhiz Pathways +
1 Fatty acid Metabolism
Reactome [+] 3 Reactome Pathways +
1 RORA activates gene expression
2 PPARA activates gene expression
3 Import of palmitoyl-CoA into the mitochondrial matrix
WikiPathways [+] 8 WikiPathways +
1 SIDS Susceptibility Pathways
2 Mitochondrial LC-Fatty Acid Beta-Oxidation
3 Nuclear Receptors Meta-Pathway
4 PPAR Alpha Pathway
5 Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
6 Circadian Clock
7 Fatty Acid Beta Oxidation
8 AMPK Signaling
Target-Related Models and Studies
Target Validation
References
REF 1 Perhexiline. Cardiovasc Drug Rev. 2007 Spring;25(1):76-97.
REF 2 URL: 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 3 Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
REF 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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 800005522)
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 800026687)
REF 7 Etomoxir, 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 8 Central ghrelin regulates peripheral lipid metabolism in a growth hormone-independent fashion. Endocrinology. 2009 Oct;150(10):4562-74.
REF 9 Hypoglycemic effects of a novel fatty acid oxidation inhibitor in rats and monkeys. Am J Physiol. 1998 Feb;274(2 Pt 2):R524-8.
REF 10 Comparison of the effects of carnitine palmitoyltransferase-1 and -2 inhibitors on rat heart hypertrophy. Cardioscience. 1994 Sep;5(3):193-7.
REF 11 C75 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.

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