Target Information

Target General Infomation
Target ID
T46628
Former ID
TTDC00123
Target Name
Microsomal triglyceride transfer protein, large subunit
Gene Name
MTTP
Synonyms
Microsomal triglyceride transfer protein large subunit; MTTP
Target Type
Successful
Disease Arteriosclerosis [ICD9: 440; ICD10: I70]
Diabetes; Dyslipidaemias; Hyperlipidaemia [ICD9:253.5, 588.1, 272, 272.0-272.4; ICD10: E23.2, N25.1, E78]
Familial hypercholesterolemia [ICD9: 272; ICD10: E78.0]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Kidney disorders [ICD10: N00-N39]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Catalyzes the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces. Required for the secretion of plasma lipoproteins that contain apolipoprotein B.
BioChemical Class
Vitellogenin lipid transport
Target Validation
T46628
UniProt ID
P55157
Sequence
MILLAVLFLCFISSYSASVKGHTTGLSLNNDRLYKLTYSTEVLLDRGKGKLQDSVGYRIS
SNVDVALLWRNPDGDDDQLIQITMKDVNVENVNQQRGEKSIFKGKSPSKIMGKENLEALQ
RPTLLHLIHGKVKEFYSYQNEAVAIENIKRGLASLFQTQLSSGTTNEVDISGNCKVTYQA
HQDKVIKIKALDSCKIARSGFTTPNQVLGVSSKATSVTTYKIEDSFVIAVLAEETHNFGL
NFLQTIKGKIVSKQKLELKTTEAGPRLMSGKQAAAIIKAVDSKYTAIPIVGQVFQSHCKG
CPSLSELWRSTRKYLQPDNLSKAEAVRNFLAFIQHLRTAKKEEILQILKMENKEVLPQLV
DAVTSAQTSDSLEAILDFLDFKSDSSIILQERFLYACGFASHPNEELLRALISKFKGSIG
SSDIRETVMIITGTLVRKLCQNEGCKLKAVVEAKKLILGGLEKAEKKEDTRMYLLALKNA
LLPEGIPSLLKYAEAGEGPISHLATTALQRYDLPFITDEVKKTLNRIYHQNRKVHEKTVR
TAAAAIILNNNPSYMDVKNILLSIGELPQEMNKYMLAIVQDILRFEMPASKIVRRVLKEM
VAHNYDRFSRSGSSSAYTGYIERSPRSASTYSLDILYSGSGILRRSNLNIFQYIGKAGLH
GSQVVIEAQGLEALIAATPDEGEENLDSYAGMSAILFDVQLRPVTFFNGYSDLMSKMLSA
SGDPISVVKGLILLIDHSQELQLQSGLKANIEVQGGLAIDISGAMEFSLWYRESKTRVKN
RVTVVITTDITVDSSFVKAGLETSTETEAGLEFISTVQFSQYPFLVCMQMDKDEAPFRQF
EKKYERLSTGRGYVSQKRKESVLAGCEFPLHQENSEMCKVVFAPQPDSTSSGWF
Drugs and Mode of Action
Drug(s) BMS-201038 Drug Info Approved Familial hypercholesterolemia [532210], [542462]
Granotapide Drug Info Phase 2 Hyperlipidaemia [522707]
Implitapide Drug Info Phase 2 Hyperlipidaemia [521593]
JNJ-16269110 Drug Info Phase 2 Type 2 diabetes [522314]
SLx-4090 Drug Info Phase 2 Diabetes; Dyslipidaemias; Hyperlipidaemia [524039]
KD020 Drug Info Phase 1/2 Kidney disorders [547974]
GR-328713 Drug Info Discontinued in Phase 1 Arteriosclerosis [546541]
Inhibitor BMS-201038 Drug Info [536426], [537143]
DIRLOTAPIDE Drug Info [528651]
Granotapide Drug Info [531286]
Implitapide Drug Info [536042], [536210], [536980]
JNJ-16269110 Drug Info [522314]
Modulator GR-328713 Drug Info [550856]
KD020 Drug Info [549956]
SLx-4090 Drug Info [531392]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Fat digestion and absorption
Reactome Chylomicron-mediated lipid transport
WikiPathways Statin Pathway
Lipid digestion, mobilization, and transport
References
Ref 521593ClinicalTrials.gov (NCT00080132) Implitapide in Patients With Hypertriglyceridemia (HTG) on Maximal, Concurrent Triglyceride-Lowering Therapy. U.S. National Institutes of Health.
Ref 522314ClinicalTrials.gov (NCT00672386) A Study of the Safety and Effectiveness of a R256918 in Patients With Type 2 Diabetes. U.S. National Institutes of Health.
Ref 522707ClinicalTrials.gov (NCT00929539) Safety and Efficacy Study of JTT-130 in Obese Type 2 Diabetic Patients. U.S. National Institutes of Health.
Ref 524039ClinicalTrials.gov (NCT01675154) Phase 2 Study of Orlistat and SLx-4090 for the Treatment of Type 1 Hyperlipoproteinemia. U.S. National Institutes of Health.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 542462(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: 7439).
Ref 546541Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008868)
Ref 547974Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020855)
Ref 522314ClinicalTrials.gov (NCT00672386) A Study of the Safety and Effectiveness of a R256918 in Patients With Type 2 Diabetes. U.S. National Institutes of Health.
Ref 528651Bioorg Med Chem Lett. 2007 Apr 1;17(7):1996-9. Epub 2007 Jan 17.In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
Ref 531286JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, suppresses food intake and gastric emptying with the elevation of plasma peptide YY and glucagon-like peptide-1 in a dietary fat-dependent manner. J Pharmacol Exp Ther. 2011 Mar;336(3):850-6.
Ref 531392A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85.
Ref 536042Implitapide, a microsomal triglyceride transfer protein inhibitor, reduces progression of atherosclerosis in apolipoprotein E knockout mice fed a Western-type diet: involvement of the inhibition of postprandial triglyceride elevation. Biol Pharm Bull. 2005 Feb;28(2):247-52.
Ref 536210Lipid-lowering drugs. Cell Mol Life Sci. 2006 May;63(10):1165-78.
Ref 536426Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Apr;29(3):231-45.
Ref 536980Novel nonstatin strategies to lower low-density lipoprotein cholesterol. Curr Atheroscler Rep. 2009 Jan;11(1):67-70.
Ref 537143Dyslipidemia and cardiovascular diseases. Curr Opin Lipidol. 2009 Apr;20(2):157-8.
Ref 549956Clinical pipeline report, company report or official report of Kadmon Pharmaceuticals.
Ref 550856Patent CN101237870 B.

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