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

General Information of Drug (ID: DMJ63GW)

• Drug Name: RPR-113829 Drug Info
• Synonyms: RPR-113829; CHEMBL48866; SCHEMBL8750304; BDBM50058204; (S)-2-{[6-((R)-2-Amino-3-mercapto-propylamino)-naphthalene-1-carbonyl]-amino}-4-methylsulfanyl-butyric acid
• Cross-matching ID:
  PubChem CID: 9953221
  TTD Drug ID: DMJ63GW

Molecule-Related Drug Atlas

Drug(s) Targeting Farnesyl protein transferase (Ftase)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lonafarnib	DMGM2Z6	Hutchinson-Gilford progeria syndrome	LD2B	Approved	[2]
Zarnestra	DMF30HL	Acute myeloid leukaemia	2A60	Phase 3	[3]
L-778123	DMWSC5L	Lymphoma	2A80-2A86	Phase 1	[4]
GGTI-2418	DM8U23L	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
BMS214662	DM5M48F	Non-small-cell lung cancer	2C25.Y	Phase 1	[6]
L-745631	DM4UP7R	Solid tumour/cancer	2A00-2F9Z	Terminated	[7]
ABT-839	DM4UN9A	Non-small-cell lung cancer	2C25.Y	Terminated	[8]
MANUMYCIN A	DM1SWOY	N. A.	N. A.	Terminated	[9]
SCH-44342	DMUL4VX	N. A.	N. A.	Terminated	[10]
RPR-114334	DMAIJT6	N. A.	N. A.	Terminated	[1]

Drug(s) Targeting CAAX farnesyltransferase beta (FNTB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
L-745631	DM4UP7R	Solid tumour/cancer	2A00-2F9Z	Terminated	[7]
ABT-839	DM4UN9A	Non-small-cell lung cancer	2C25.Y	Terminated	[11]
MANUMYCIN A	DM1SWOY	N. A.	N. A.	Terminated	[9]
SCH-44342	DMUL4VX	N. A.	N. A.	Terminated	[7]
RPR-114334	DMAIJT6	N. A.	N. A.	Terminated	[1]
L-731735	DM1XBKC	Solid tumour/cancer	2A00-2F9Z	Terminated	[7]
FUSIDIENOL	DMI1Y92	N. A.	N. A.	Terminated	[12]
ABT-100	DMPFLS5	Solid tumour/cancer	2A00-2F9Z	Terminated	[13]
B-956	DM1IO9X	Solid tumour/cancer	2A00-2F9Z	Terminated	[14]
L-739749	DMAUG0L	Solid tumour/cancer	2A00-2F9Z	Terminated	[7]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
CAAX farnesyltransferase beta (FNTB)	TT7WZIJ	FNTB_HUMAN	Inhibitor	[1]
Farnesyl protein transferase (Ftase)	TTXQKM3	FNTA_HUMAN; FNTB_HUMAN	Inhibitor	[1]

References

• [1] Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. J Med Chem. 1997 Jun 6;40(12):1763-7.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [3] Tipifarnib in the treatment of newly diagnosed acute myelogenous leukemia. Biologics. 2008 Sep;2(3):491-500.
• [4] Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein trans... Mol Cancer Ther. 2002 Jul;1(9):747-58.
• [5] Company report (Prescient)
• [6] Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells. Leukemia. 2004 Oct;18(10):1599-604.
• [7] Ras farnesyltransferase: a new therapeutic target. J Med Chem. 1997 Sep 12;40(19):2971-90.
• [8] Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.
• [9] A novel metal-chelating inhibitor of protein farnesyltransferase. Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.
• [10] Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. J Med Chem. 1999 Jun 17;42(12):2125-35.
• [11] Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.
• [12] Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking. J Med Chem. 2002 Mar 28;45(7):1460-5.
• [13] Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. J Heart Lung Transplant. 2005 Sep;24(9):1403-9.
• [14] Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. 1995 Nov 15;55(22):5310-4.