General Information of Drug Therapeutic Target (DTT) (ID: TT0GV3R)

DTT Name DGAT1 messenger RNA (DGAT1 mRNA)
Synonyms
Retinol O-fatty-acyltransferase (mRNA); Diglyceride acyltransferase (mRNA); Diacylglycerol O-acyltransferase 1 (mRNA); DGAT (mRNA); Acyl-CoA retinol O-fatty-acyltransferase (mRNA); ARAT (mRNA); AGRP1 (mRNA); ACAT-related gene product 1 (mRNA)
Gene Name DGAT1
DTT Type
Literature-reported target
[1]
BioChemical Class
mRNA target
UniProt ID
DGAT1_HUMAN
TTD ID
T75386
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.3.1.20
Sequence
MGDRGSSRRRRTGSRPSSHGGGGPAAAEEEVRDAAAGPDVGAAGDAPAPAPNKDGDAGVG
SGHWELRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQV
VSLFLKDPYSWPAPCLVIAANVFAVAAFQVEKRLAVGALTEQAGLLLHVANLATILCFPA
AVVLLVESITPVGSLLALMAHTILFLKLFSYRDVNSWCRRARAKAASAGKKASSAAAPHT
VSYPDNLTYRDLYYFLFAPTLCYELNFPRSPRIRKRFLLRRILEMLFFTQLQVGLIQQWM
VPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWLFHSCLNAVAELMQFGDREF
YRDWWNSESVTYFWQNWNIPVHKWCIRHFYKPMLRRGSSKWMARTGVFLASAFFHEYLVS
VPLRMFRLWAFTGMMAQIPLAWFVGRFFQGNYGNAAVWLSLIIGQPIAVLMYVHDYYVLN
YEAPAAEA
Function
In contrast to DGAT2 it is not essential for survival. May be involved in VLDL (very low density lipoprotein) assembly. In liver, plays a role in esterifying exogenous fatty acids to glycerol. Functions as the major acyl-CoA retinol acyltransferase (ARAT) in the skin, where it acts to maintain retinoid homeostasis and prevent retinoid toxicity leading to skin and hair disorders. Catalyzes the terminal and only committed step in triacylglycerol synthesis by using diacylglycerol and fatty acyl CoA as substrates.
KEGG Pathway
Glycerolipid metabolism (hsa00561 )
Retinol metabolism (hsa00830 )
Metabolic pathways (hsa01100 )
Fat digestion and absorption (hsa04975 )
Reactome Pathway
Triglyceride Biosynthesis (R-HSA-75109 )
Acyl chain remodeling of DAG and TAG (R-HSA-1482883 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ISIS 191729 DMOQ27M Discovery agent N.A. Investigative [2]
ISIS 191731 DM52ZWB Discovery agent N.A. Investigative [2]
ISIS 191755 DMHWMFP Discovery agent N.A. Investigative [2]
ISIS 191756 DMQRZX8 Discovery agent N.A. Investigative [2]
ISIS 191759 DMHPENR Discovery agent N.A. Investigative [2]
ISIS 191761 DM0VAUR Discovery agent N.A. Investigative [2]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1 Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem. 2009 Mar 26;52(6):1558-68.
2 US patent application no. 7,414,033, Modulation of diacylglycerol acyltransferase 1 expression.