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

General Information of Drug (ID: DMSQRXW)

Drug Name

SQ-32709 Drug Info

Synonyms

farnesyl diphosphate; farnesyl pyrophosphate; (2E,6E)-Farnesyl diphosphate; trans,trans-Farnesyl diphosphate; all-trans-Farnesyl pyrophosphate; (all-E)-Farnesyl diphosphate; (E,E)-Farnesyl pyrophosphate; (2E,6E)-Farnesyl pyrophosphate; trans-Farnesyl pyrophosphate; 2-trans,6-trans-Farnesyl pyrophosphate; farnesyl-PP; (E,E)-Farnesyl diphosphate; 2-trans,6-trans-farnesyl diphosphate; trans-trans-farnesyl diphosphate; UNII-79W6B01D07; CHEBI:17407; trans,trans-Farnesyl pyrophosphate; Sq 32709; 13058-04-3; CHEMBL69330

Indication

Disease Entry	ICD 11	Status	REF
Arteriosclerosis	BD40	Discontinued in Phase 2	[1]

Cross-matching ID

PubChem CID: 445713
ChEBI ID: CHEMBL69330
CAS Number: CAS 372-97-4
TTD Drug ID: DMSQRXW
INTEDE Drug ID: DR1927

Molecule-Related Drug Atlas

Molecule Type:

DTT

DME

Drug Status:

Discontinued Drug(s)

Investigative Drug(s)

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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	[5]
BMS-187745	DMP8SIV	Hyperlipidaemia	5C80	Discontinued in Phase 2	[6]
Squalestatin 1	DM4JZPT	Arteriosclerosis	BD40	Terminated	[7]
A-87049	DMUID46	N. A.	N. A.	Terminated	[8]
RPR-101821	DM21Y75	Arteriosclerosis	BD40	Terminated	[9]
SQ-34919	DMT7O9V	N. A.	N. A.	Terminated	[10]
L-735021	DM8BVJQ	Discovery agent	N.A.	Investigative	[11]
PMID19191557C32	DMH8QRI	Discovery agent	N.A.	Investigative	[6]
PMID9871507C14	DMY28QM	Discovery agent	N.A.	Investigative	[12]
PMID19456099C13	DMBU9E4	Discovery agent	N.A.	Investigative	[13]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

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

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Ras proteins prenyltransferase alpha (FNTA)	DEFNVD7	FNTA_HUMAN	Substrate	[3]
Squalene synthase (FDFT1)	DEIDTHQ	FDFT_HUMAN	Substrate	[4]

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References

1	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005302)
2	Clinical pharmacokinetics and pharmacodynamics of a new squalene synthase inhibitor, BMS-188494, in healthy volunteers. J Clin Pharmacol. 1998 Dec;38(12):1116-21.
3	Site-selective enzymatic labeling of designed ankyrin repeat proteins using protein farnesyltransferase. Methods Mol Biol. 2019;2033:207-219.
4	Increased activity of the sterol branch of the mevalonate pathway elevates glycosylation of secretory proteins and improves antifungal properties of Trichoderma atroviride. Fungal Genet Biol. 2020 Jan 17;137:103334.
5	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.
6	Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in Staphylococcus aureus. J Med Chem. 2009 Feb 26;52(4):976-88.
7	Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo. J Biol Chem. 1992 Jun 15;267(17):11705-8.
8	(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.
9	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.
10	Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine, Bioorg. Med. Chem. Lett. 6(12):1291-1296 (1996).
11	Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives. J Med Chem. 1994 Nov 11;37(23):4031-51.
12	Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation. Bioorg Med Chem Lett. 1998 Apr 21;8(8):891-6.
13	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.