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

General Information of DTT (ID: TTIKWV4)

• DTT Name: Geranyltranstransferase (FDPS) DTT Info
• Gene Name: FDPS

Molecule-Related Drug & Molecule List

8 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alendronate	DMY2KX9	Bone Paget disease		Approved	[1]
Ibandronate	DM0QZBN	Hypercalcaemia	5B91.0	Approved	[1]
Incadronate	DM3DSVJ	Hypercalcaemia	5B91.0	Approved	[2]
Minodronate	DM50PMY	Osteoporosis	FB83.0	Approved	[3]
NERIDRONIC ACID	DMMPG5V	Bone disease	FC0Z	Approved	[4]
Pamidronate	DMB4AVP	Bone Paget disease		Approved	[5]
Risedronate	DM5FLTY	Bone Paget disease		Approved	[6]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[1]

1 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zarnestra	DMF30HL	Acute myeloid leukaemia	2A60	Phase 3	[7]

57 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(1-hydroxy-1-phosphono-heptyl)-phosphonic acid	DM5L8WX	Discovery agent	N.A.	Investigative	[8]
(2E, 6E)-farnesylbisphosphonate	DM3ST2Y	Discovery agent	N.A.	Investigative	[9]
(biphenyl-3-ylamino)methylenediphosphonic acid	DMGB97I	Discovery agent	N.A.	Investigative	[10]
1-(but-2-ylamino)ethyl 1,I-bisphosphonic acid	DMTMZAJ	Discovery agent	N.A.	Investigative	[8]
1-[(cyclohexylamino)ethyl]-1,1-bisphosphonicacid	DM1JQPW	Discovery agent	N.A.	Investigative	[8]
1-[(n-but-1-ylamino)ethyl]-1,1-bisphosphonic acid	DM8VNYA	Discovery agent	N.A.	Investigative	[8]
1-[(n-hex-1-ylamino)ethyl]-1,1-bisphosphonic acid	DM4ABTN	Discovery agent	N.A.	Investigative	[8]
1-[(n-oct-1-ylamino)ethyl]-1,1-bisphosphonic acid	DM9ZK0D	Discovery agent	N.A.	Investigative	[8]
1-[(prop-1-ylamino)ethyl]-1,1-bisphosphonic acid	DMCRHVI	Discovery agent	N.A.	Investigative	[8]
1-[(prop-2-ylamino)ethyl]-1,1-bisphosphonicacid	DMSCN8J	Discovery agent	N.A.	Investigative	[8]
1-[(tert-butylamino)ethyl]-1,1-bisphosphonicacid	DMLDY3H	Discovery agent	N.A.	Investigative	[8]
3-azageranylgeranyl diphosphate	DM6KNMB	Discovery agent	N.A.	Investigative	[11]
BPH-252	DMUOS3G	Discovery agent	N.A.	Investigative	[12]
BPH-608	DM0NQLI	Discovery agent	N.A.	Investigative	[13]
BPH-628	DM0TJ6R	Discovery agent	N.A.	Investigative	[12]
BPH-629	DM49BFM	Discovery agent	N.A.	Investigative	[13]
BPH-675	DM3IPYV	Discovery agent	N.A.	Investigative	[13]
BPH-676	DMPKAEW	Discovery agent	N.A.	Investigative	[13]
BPH-715	DMTHW3F	Discovery agent	N.A.	Investigative	[12]
BPH-742	DMD0XEO	Discovery agent	N.A.	Investigative	[12]
CT-10	DMIVNMJ	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
digeranyl bisphosphonate	DMXK8BH	Discovery agent	N.A.	Investigative	[12]
Dimethylallyl Diphosphate	DMP5I47	Discovery agent	N.A.	Investigative	[15]
diphosphoric acid	DMYWL89	Discovery agent	N.A.	Investigative	[4]
Geranyl Diphosphate	DMB9LE1	Discovery agent	N.A.	Investigative	[16]
GERANYLGERANYL DIPHOSPHATE	DMJZ0AM	Discovery agent	N.A.	Investigative	[15]
Homorisedronate	DMX8DC2	Discovery agent	N.A.	Investigative	[17]
ISOPENTENYL PYROPHOSPHATE	DMTU05Y	Discovery agent	N.A.	Investigative	[15]
Isopentyl Pyrophosphate	DM9J5IS	Discovery agent	N.A.	Investigative	[16]
NE-10575	DMGSNU4	Discovery agent	N.A.	Investigative	[4]
NE10790	DMVESO2	Discovery agent	N.A.	Investigative	[4]
NE11808	DMR92HV	Discovery agent	N.A.	Investigative	[4]
NE21650	DM58O3I	Discovery agent	N.A.	Investigative	[18]
NE58018	DM28ZPT	Discovery agent	N.A.	Investigative	[4]
NE58027	DMU4I8R	Discovery agent	N.A.	Investigative	[4]
NE58043	DMS7UNR	Discovery agent	N.A.	Investigative	[4]
NE58062	DMHIM6N	Discovery agent	N.A.	Investigative	[4]
NE97220	DMDWESP	Discovery agent	N.A.	Investigative	[4]
OLPADRONIC ACID SODIUM SALT	DM1XJBE	Bone resorption	FC0Z	Investigative	[19]
PG-1014491	DMH4AKG	Bone disease	FC0Z	Investigative	[14]
Piridronic acid	DMRDF8Z	Discovery agent	N.A.	Investigative	[4]
PMID12014956C12	DMFO7UC	Discovery agent	N.A.	Investigative	[11]
PMID17963374C31	DMTP5OY	Discovery agent	N.A.	Investigative	[20]
PMID17975902C5e	DMS1QM8	Discovery agent	N.A.	Investigative	[21]
PMID18295483C2	DM3GYNM	Discovery agent	N.A.	Investigative	[22]
PMID18800762C11	DM4UWKR	Discovery agent	N.A.	Investigative	[12]
PMID18800762C14	DM5T2FR	Discovery agent	N.A.	Investigative	[12]
PMID18800762C16	DM70SEQ	Discovery agent	N.A.	Investigative	[12]
PMID18800762C19	DM1QXFI	Discovery agent	N.A.	Investigative	[12]
PMID18800762C47	DMZDC14	Discovery agent	N.A.	Investigative	[12]
PMID18800762C51	DMWFGY4	Discovery agent	N.A.	Investigative	[12]
[2-(6-Chloro-purin-9-yl)ethyl]-bisphosphonic acid	DM5LVIR	Discovery agent	N.A.	Investigative	[23]
[2-(Benzoimidazol-1-yl)ethyl]-bisphosphonic acid	DM98MXT	Discovery agent	N.A.	Investigative	[23]
[2-(Imidazol-1-yl)ethyl]-bisphosphonic acid	DMQZUD9	Discovery agent	N.A.	Investigative	[23]
[2-(Imidazol-2-yl-thio)ethyl]-bisphosphonic acid	DMBVDY5	Discovery agent	N.A.	Investigative	[23]
[2-(Purin-9-yl)ethyl]-bisphosphonic acid	DM3VT8M	Discovery agent	N.A.	Investigative	[23]
[2-(Pyrazol-1-yl)ethyl]-bisphosphonic acid	DMJN8XK	Discovery agent	N.A.	Investigative	[23]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [2] Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42.
• [3] Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid. J Med Chem. 2010 May 13;53(9):3454-64.
• [4] Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of hu... J Med Chem. 2008 Apr 10;51(7):2187-95.
• [5] Detection of nonsterol isoprenoids by HPLC-MS/MS. Anal Biochem. 2008 Dec 1;383(1):18-24.
• [6] Activity of bisphosphonates against Trypanosoma brucei rhodesiense. J Med Chem. 2002 Jul 4;45(14):2904-14.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl... Bioorg Med Chem. 2008 Mar 15;16(6):3283-90.
• [9] Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors. Bioorg Med Chem. 2008 Jan 1;16(1):390-9.
• [10] Bisphosphonate inhibitors of ATP-mediated HIV-1 reverse transcriptase catalyzed excision of chain-terminating 3'-azido, 3'-deoxythymidine: a QSAR i... Bioorg Med Chem. 2008 Oct 1;16(19):8959-67.
• [11] Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents. J Med Chem. 2002 May 23;45(11):2185-96.
• [12] Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation. J Med Chem. 2008 Sep 25;51(18):5594-607.
• [13] Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7.
• [14] 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: 643).
• [15] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [16] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [17] Bisphosphonates are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase. J Biol Chem. 2001 Sep 7;276(36):33930-7.
• [18] Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase. Biochem Biophys Res Commun. 2002 Jan 18;290(2):869-73.
• [19] Nitrogen-containing bisphosphonates inhibit isopentenyl pyrophosphate isomerase/farnesyl pyrophosphate synthase activity with relative potencies corresponding to their antiresorptive potencies in vitro and in vivo. Biochem Biophys Res Commun. 1999 Feb 16;255(2):491-4.
• [20] Activity of sulfonium bisphosphonates on tumor cell lines. J Med Chem. 2007 Nov 29;50(24):6067-79.
• [21] Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate. J Med Chem. 2007 Nov 29;50(24):5967-75.
• [22] Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones. Bioorg Med Chem Lett.2008 Mar 15;18(6):1840-4.
• [23] Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocy... J Med Chem. 2008 Nov 13;51(21):6800-7.