Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTDL0NY)

• DTT 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
• DTT Type: Successful target; [1]
• BioChemical Class: Acyltransferase
• UniProt ID: CPT1B_HUMAN
• TTD ID: T75888
• EC Number: EC 2.3.1.21
• Sequence:
  MAEAHQAVAFQFTVTPDGVDFRLSREALKHVYLSGINSWKKRLIRIKNGILRGVYPGSPT
  SWLVVIMATVGSSFCNVDISLGLVSCIQRCLPQGCGPYQTPQTRALLSMAIFSTGVWVTG
  IFFFRQTLKLLLCYHGWMFEMHGKTSNLTRIWAMCIRLLSSRHPMLYSFQTSLPKLPVPR
  VSATIQRYLESVRPLLDDEEYYRMELLAKEFQDKTAPRLQKYLVLKSWWASNYVSDWWEE
  YIYLRGRSPLMVNSNYYVMDLVLIKNTDVQAARLGNIIHAMIMYRRKLDREEIKPVMALG
  IVPMCSYQMERMFNTTRIPGKDTDVLQHLSDSRHVAVYHKGRFFKLWLYEGARLLKPQDL
  EMQFQRILDDPSPPQPGEEKLAALTAGGRVEWAQARQAFFSSGKNKAALEAIERAAFFVA
  LDEESYSYDPEDEASLSLYGKALLHGNCYNRWFDKSFTLISFKNGQLGLNAEHAWADAPI
  IGHLWEFVLGTDSFHLGYTETGHCLGKPNPALAPPTRLQWDIPKQCQAVIESSYQVAKAL
  ADDVELYCFQFLPFGKGLIKKCRTSPDAFVQIALQLAHFRDRGKFCLTYEASMTRMFREG
  RTETVRSCTSESTAFVQAMMEGSHTKADLRDLFQKAAKKHQNMYRLAMTGAGIDRHLFCL
  YLVSKYLGVSSPFLAEVLSEPWRLSTSQIPQSQIRMFDPEQHPNHLGAGGGFGPVADDGY
  GVSYMIAGENTIFFHISSKFSSSETNAQRFGNHIRKALLDIADLFQVPKAYS
• Function: mitochondrial outer membrane, mitochondrion, carnitine O-palmitoyltransferase activity, carnitine metabolic process, carnitine shuttle, fatty acid beta-oxidation, long-chain fatty acid transport.
• KEGG Pathway:
  Fatty acid degradation (hsa00071)
  Fatty acid metabolism (hsa01212)
  PPAR signaling pathway (hsa03320)
  AMPK signaling pathway (hsa04152)
  Adipocytokine signaling pathway (hsa04920)
  Glucagon signaling pathway (hsa04922)
• Reactome Pathway:
  PPARA activates gene expression (R-HSA-1989781)
  Import of palmitoyl-CoA into the mitochondrial matrix (R-HSA-200425)
  RORA activates gene expression (R-HSA-1368082)
• BioCyc Pathway: MetaCyc:MON66-34409

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Levacecarnine hci	DMJBOCR	Cognitive impairment	6D71	Approved	[2]
Perhexiline	DMINO7Z	Angina pectoris	BA40	Approved	[1]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SDZ-CPI-975	DM70MJQ	Diabetic complication	5A2Y	Discontinued in Phase 1	[3]
DB-200	DMTXPSB	Psoriasis vulgaris	EA90	Terminated	[4]
Etomoxir	DM3BHN1	Heart failure	BD10-BD13	Terminated	[5]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
C75	DMHGX1N	Obesity	5B81	Investigative	[6]

References

• [1] Perhexiline. Cardiovasc Drug Rev. 2007 Spring;25(1):76-97.
• [2] Central ghrelin regulates peripheral lipid metabolism in a growth hormone-independent fashion. Endocrinology. 2009 Oct;150(10):4562-74.
• [3] Hypoglycemic effects of a novel fatty acid oxidation inhibitor in rats and monkeys. Am J Physiol. 1998 Feb;274(2 Pt 2):R524-8.
• [4] Comparison of the effects of carnitine palmitoyltransferase-1 and -2 inhibitors on rat heart hypertrophy. Cardioscience. 1994 Sep;5(3):193-7.
• [5] 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.
• [6] 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.