General Information of DTT (ID: TTFQEO5)

DTT Name Squalene synthetase (FDFT1) DTT Info
Gene Name FDFT1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Investigative Drug(s)
7 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lapaquistat acetate DMJY9CW Hyperlipidaemia 5C80 Discontinued in Phase 3 [1]
BMS-187745 DMP8SIV Hyperlipidaemia 5C80 Discontinued in Phase 2 [2]
SQ-32709 DMSQRXW Arteriosclerosis BD40 Discontinued in Phase 2 [3]
A-87049 DMUID46 N. A. N. A. Terminated [4]
RPR-101821 DM21Y75 Arteriosclerosis BD40 Terminated [5]
SQ-34919 DMT7O9V N. A. N. A. Terminated [6]
Squalestatin 1 DM4JZPT Arteriosclerosis BD40 Terminated [7]
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⏷ Show the Full List of 7 Discontinued Drug(s)
67 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(Z)-3-[2-(9H-fluoren-2-yloxy)ethylidene]-quinuclidine hydrochloride 31 DMIQ14F Discovery agent N.A. Investigative [8]
1-allyl-2-[3-(isopropylamino)propoxy]-9H-carbazole DMQJ9RZ Discovery agent N.A. Investigative [9]
1-allyl-2-[3-(isopropylamino)propoxy]-9H-xanthen-9-one DMNDW4J Discovery agent N.A. Investigative [9]
2-[4-(2-Thienyl)phenyl]-4-methylmorpholin-2-ol DM6R1XH Discovery agent N.A. Investigative [10]
3-[1'-{4'-(Benzyloxy)-phenyl}]-quinuclidine-2-ene DMIHWAJ Discovery agent N.A. Investigative [11]
3-[7'-(Methoxy)-napht-2'-yl]-quinuclidine-2-ene DM7IHUK Discovery agent N.A. Investigative [11]
BPH-652 DMX4WI7 Hypercholesterolaemia 5C80.0 Investigative [12]
BPH-830 DM15L2J Discovery agent N.A. Investigative [13]
CP-294838 DM6BRLA Discovery agent N.A. Investigative [14]
E5700 DM8LPBF Discovery agent N.A. Investigative [15]
ER-119884 DMIQ801 Discovery agent N.A. Investigative [15]
J-104118 DMQ8J3M Discovery agent N.A. Investigative [12]
J-104123 DMWF7RO Discovery agent N.A. Investigative [12]
L-731120 DM8WCUY Discovery agent N.A. Investigative [12]
L-731128 DMTHLUN Discovery agent N.A. Investigative [12]
L-735021 DM8BVJQ Discovery agent N.A. Investigative [16]
PMID12238936C3a DMQZXMF Discovery agent N.A. Investigative [17]
PMID12238936C3f DMO5J8N Discovery agent N.A. Investigative [17]
PMID17709461C4g DMMB6NU Discovery agent N.A. Investigative [11]
PMID18754614C10 DM1JRGI Discovery agent N.A. Investigative [10]
PMID18754614C17 DMSVB9D Discovery agent N.A. Investigative [10]
PMID18754614C18 DMF7VZO Discovery agent N.A. Investigative [10]
PMID18754614C19 DMHSE96 Discovery agent N.A. Investigative [10]
PMID18754614C4 DMQFYM4 Discovery agent N.A. Investigative [10]
PMID18754614C7 DMVTLO0 Discovery agent N.A. Investigative [10]
PMID18754614C8 DM7SCM3 Discovery agent N.A. Investigative [10]
PMID18754614C9 DMPH7A6 Discovery agent N.A. Investigative [10]
PMID19191557C14 DMG7D3I Discovery agent N.A. Investigative [2]
PMID19191557C19 DMXLVEC Discovery agent N.A. Investigative [2]
PMID19191557C21 DM5RIB0 Discovery agent N.A. Investigative [2]
PMID19191557C3 DM1MEY3 Discovery agent N.A. Investigative [2]
PMID19191557C32 DMH8QRI Discovery agent N.A. Investigative [2]
PMID19191557C35 DM09IEK Discovery agent N.A. Investigative [2]
PMID19191557C8 DMUWYA2 Discovery agent N.A. Investigative [2]
PMID19456099C13 DMBU9E4 Discovery agent N.A. Investigative [13]
PMID19456099C15 DMPZMS0 Discovery agent N.A. Investigative [13]
PMID20299227C12 DMKAZ1O Discovery agent N.A. Investigative [18]
PMID20299227C20 DM9H6LZ Discovery agent N.A. Investigative [18]
PMID22464687C15a DMCDOHA Discovery agent N.A. Investigative [19]
PMID7473541C11 DMB2MQW Discovery agent N.A. Investigative [20]
PMID7473541C19 DM2CP5J Discovery agent N.A. Investigative [20]
PMID7473541C20 DMMZ1LR Discovery agent N.A. Investigative [20]
PMID7473541C21 DMMRSZB Discovery agent N.A. Investigative [20]
PMID7629799C2d DMOJ57D Discovery agent N.A. Investigative [21]
PMID7629799C2e DMBRH0Q Discovery agent N.A. Investigative [21]
PMID7629799C6 DMXMF39 Discovery agent N.A. Investigative [2]
PMID7650673C4q DM5SU6N Discovery agent N.A. Investigative [22]
PMID7966163C3f DMJF7OC Discovery agent N.A. Investigative [16]
PMID7966163C4e DMD524S Discovery agent N.A. Investigative [16]
PMID7966163C6c DMUEG8O Discovery agent N.A. Investigative [16]
PMID7966163C6d DM0XU3C Discovery agent N.A. Investigative [16]
PMID7966163C6g DM8T41N Discovery agent N.A. Investigative [16]
PMID8496919C7 DM8PBKQ Discovery agent N.A. Investigative [23]
PMID8576905C4 DMUJEA4 Discovery agent N.A. Investigative [24]
PMID8709131C15 DMWBPOJ Discovery agent N.A. Investigative [25]
PMID8709131C17 DM10IQP Discovery agent N.A. Investigative [25]
PMID8709131C23 DMSKJ53 Discovery agent N.A. Investigative [25]
PMID8709131C2a (+) DM1OS6M Discovery agent N.A. Investigative [25]
PMID8709131C4 DMETC8A Discovery agent N.A. Investigative [25]
PMID9216829C5j DM2F81A Discovery agent N.A. Investigative [4]
PMID9216829C5m DM3ARWX Discovery agent N.A. Investigative [4]
PMID9871507C14 DMY28QM Discovery agent N.A. Investigative [26]
YM-75440 DMMCXWQ Discovery agent N.A. Investigative [9]
ZARAGOZIC ACID B DMYRLA0 Discovery agent N.A. Investigative [27]
Zaragozic Acid C DMUQWP1 Discovery agent N.A. Investigative [27]
Zaragozic Acid D DMMTJE3 Discovery agent N.A. Investigative [27]
Zaragozic Acid D2 DML4WQJ Discovery agent N.A. Investigative [27]
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⏷ Show the Full List of 67 Investigative Drug(s)
Molecule Interaction Atlas

References

1 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.
2 Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in Staphylococcus aureus. J Med Chem. 2009 Feb 26;52(4):976-88.
3 Clinical pharmacokinetics and pharmacodynamics of a new squalene synthase inhibitor, BMS-188494, in healthy volunteers. J Clin Pharmacol. 1998 Dec;38(12):1116-21.
4 (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.
5 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.
6 Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine, Bioorg. Med. Chem. Lett. 6(12):1291-1296 (1996).
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 Syntheses and biological evaluation of novel quinuclidine derivatives as squalene synthase inhibitors. Bioorg Med Chem. 2003 May 29;11(11):2403-14.
9 Synthesis and biological evaluation of novel propylamine derivatives as orally active squalene synthase inhibitors. Bioorg Med Chem. 2004 Nov 15;12(22):5899-908.
10 Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity. J Med Chem. 2008 Sep 25;51(18):5861-5.
11 Quinuclidine derivatives as potential antiparasitics. Antimicrob Agents Chemother. 2007 Nov;51(11):4049-61.
12 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. (Target id: 645).
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.
14 Truncation of human squalene synthase yields active, crystallizable protein. Arch Biochem Biophys. 1998 Feb 15;350(2):283-90.
15 Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives. Antimicrob Agents Chemother. 2007 Jun;51(6):2123-9.
16 Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives. J Med Chem. 1994 Nov 11;37(23):4031-51.
17 Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis. J Med Chem. 2002 Sep 26;45(20):4571-80.
18 Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs). Bioorg Med Chem. 2010 Apr 1;18(7):2428-38.
19 Discovery of novel tricyclic compounds as squalene synthase inhibitors. Bioorg Med Chem. 2012 May 1;20(9):3072-93.
20 Phenoxypropylamines: a new series of squalene synthase inhibitors. J Med Chem. 1995 Oct 13;38(21):4157-60.
21 1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate. J Med Chem. 1995 Jul 7;38(14):2596-605.
22 (Aryloxy)methylsilane derivatives as new cholesterol biosynthesis inhibitors: synthesis and hypocholesterolemic activity of a new class of squalene epoxidase inhibitors. J Med Chem. 1995 Aug 18;38(17):3207-16.
23 N-(arylalkyl)farnesylamines: new potent squalene synthetase inhibitors. J Med Chem. 1993 May 14;36(10):1501-4.
24 Alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase. J Med Chem. 1996 Feb 2;39(3):657-60.
25 Synthesis and activity of a novel series of 3-biarylquinuclidine squalene synthase inhibitors. J Med Chem. 1996 Jul 19;39(15):2971-9.
26 Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation. Bioorg Med Chem Lett. 1998 Apr 21;8(8):891-6.
27 Zaragozic acids D and D2: potent inhibitors of squalene synthase and of Ras farnesyl-protein transferase. J Nat Prod. 1993 Nov;56(11):1923-9.