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

General Information of DTT (ID: TTUF2HO)

• DTT Name: NAD-dependent deacetylase sirtuin-1 (SIRT1) DTT Info
• UniProt ID: SIR1_HUMAN
• Gene Name: SIRT1

Molecule-Related Drug & Molecule List

6 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Resveratrol	DM3RWXL	Giant cell arteritis	4A44.2	Phase 3	[1]
GSK2245840	DMG7YQL	Chronic obstructive pulmonary disease	CA22	Phase 2	[2], [3]
MB-12066	DMRSN2C	Obesity	5B81	Phase 2	[4]
SEN-196	DMLDBQ5	Huntington disease	8A01.10	Phase 2	[5], [1]
SRT2379	DM7DAKX	Type-2 diabetes	5A11	Phase 1	[6]
SRT3025	DMRAXFH	Type-2 diabetes	5A11	Phase 1	[7]

4 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CAMBINOL	DMW46GY	Discovery agent	N.A.	Patented	[8], [1]
PMID25435179-Compound-WO2012106509CAY10602	DM2F1T0	N. A.	N. A.	Patented	[1]
PMID25435179-Compound-WO2012106509Salermide	DMLAH39	N. A.	N. A.	Patented	[1]
PMID25435179-Compound-WO2012106509Tenovin-6	DMBSOED	N. A.	N. A.	Patented	[1]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GSK184072	DMMIR1K	Colon cancer	2B90.Z	Discontinued in Phase 2	[9]

11 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-sirtinol	DMV1IS8	Discovery agent	N.A.	Investigative	[10]
(S)-sirtinol	DMS8WG3	Discovery agent	N.A.	Investigative	[10]
2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide	DMXAS25	Discovery agent	N.A.	Investigative	[11]
2H-chromeno[2,3-d]pyrimidine-2,4(3H)-dione	DMET6FO	Discovery agent	N.A.	Investigative	[12]
Meta-sirtinol	DMSK0QX	Discovery agent	N.A.	Investigative	[10]
Para-sirtinol	DM83C9N	Discovery agent	N.A.	Investigative	[10]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[13]
Ro31-8220	DMDJLF0	Discovery agent	N.A.	Investigative	[13]
splitomicin	DMCLHZ5	Discovery agent	N.A.	Investigative	[12]
SRT1720	DMUKVHQ	Discovery agent	N.A.	Investigative	[14]
YK-3237	DMU0NHX	Solid tumour/cancer	2A00-2F9Z	Investigative	[15]

References

• [1] Sirtuin modulators: an updated patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):5-15.
• [2] Sirtuin 1 activator SRT2104 protects Huntington's disease mice. Ann Clin Transl Neurol. 2014 Dec;1(12):1047-52.
• [3] Anti-inflammatory agents to treat or prevent type 2 diabetes, metabolic syndrome and cardiovascular disease. Expert Opin Investig Drugs. 2015 Mar;24(3):283-307.
• [4] Pharmacological activation of Sirt1 ameliorates polyglutamine-induced toxicity through the regulation of autophagy.PLoS One.2013 Jun 10;8(6):e64953.
• [5] Sirtuin 1 (SIRT1): the misunderstood HDAC. J Biomol Screen. 2011 Dec;16(10):1153-69.
• [6] SRT2379, a small-molecule SIRT1 activator, fails to reduce cytokine release in a human endotoxemia model. Critical Care 2013, 17(Suppl 4):P8.
• [7] The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391.
• [8] Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity. J Med Chem. 2009 May 14;52(9):2673-82.
• [9] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [10] Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors. J Med Chem. 2005 Dec 1;48(24):7789-95.
• [11] Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54.
• [12] Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specif... J Med Chem. 2010 Feb 11;53(3):1407-11.
• [13] Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. J Med Chem. 2006 Dec 14;49(25):7307-16.
• [14] Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29;450(7170):712-6.
• [15] 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: 2707).