Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM8BVJQ)

• Drug Name: L-735021 Drug Info
• Synonyms: L 735021

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 9853075
  TTD Drug ID: DM8BVJQ

Molecule-Related Drug Atlas

Drug(s) Targeting Squalene synthetase (FDFT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lapaquistat acetate	DMJY9CW	Hyperlipidaemia	5C80	Discontinued in Phase 3	[3]
SQ-32709	DMSQRXW	Arteriosclerosis	BD40	Discontinued in Phase 2	[4]
BMS-187745	DMP8SIV	Hyperlipidaemia	5C80	Discontinued in Phase 2	[5]
Squalestatin 1	DM4JZPT	Arteriosclerosis	BD40	Terminated	[6]
A-87049	DMUID46	N. A.	N. A.	Terminated	[7]
RPR-101821	DM21Y75	Arteriosclerosis	BD40	Terminated	[8]
SQ-34919	DMT7O9V	N. A.	N. A.	Terminated	[9]
PMID19191557C32	DMH8QRI	Discovery agent	N.A.	Investigative	[5]
PMID9871507C14	DMY28QM	Discovery agent	N.A.	Investigative	[10]
PMID19456099C13	DMBU9E4	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Squalene synthetase (FDFT1)	TTFQEO5	FDFT_HUMAN	Inhibitor	[2]

References

• [1] 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: 3117).
• [2] Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives. J Med Chem. 1994 Nov 11;37(23):4031-51.
• [3] Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous le... Br J Pharmacol. 2008 Jul;154(5):949-57.
• [4] Clinical pharmacokinetics and pharmacodynamics of a new squalene synthase inhibitor, BMS-188494, in healthy volunteers. J Clin Pharmacol. 1998 Dec;38(12):1116-21.
• [5] Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in Staphylococcus aureus. J Med Chem. 2009 Feb 26;52(4):976-88.
• [6] Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo. J Biol Chem. 1992 Jun 15;267(17):11705-8.
• [7] (1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent ... J Med Chem. 1997 Jul 4;40(14):2123-5.
• [8] RPR 101821, a new potent cholesterol-lowering agent: inhibition of squalene synthase and 7-dehydrocholesterol reductase. Naunyn Schmiedebergs Arch Pharmacol. 1996 Jan;353(2):233-40.
• [9] Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine, Bioorg. Med. Chem. Lett. 6(12):1291-1296 (1996).
• [10] Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation. Bioorg Med Chem Lett. 1998 Apr 21;8(8):891-6.
• [11] Inhibition of staphyloxanthin virulence factor biosynthesis in Staphylococcus aureus: in vitro, in vivo, and crystallographic results. J Med Chem. 2009 Jul 9;52(13):3869-80.