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Literature summary for 2.3.1.B43 extracted from

  • Yang, L.; He, Y.; Chen, Q.; Qian, S.; Wang, Z.
    Design and synthesis of new 9-substituted norharmane derivatives as potential Sirt5 inhibitors (2017), J. Heterocycl. Chem., 54, 1457-1466 .
No PubMed abstract available
Search for more literature for 2.3.1.B43

Application

Application Comment Organism
drug development Sirt5 is a potential drug target for the treatment of cancer, Alzheimer's disease, and Parkinson's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)-3-phenylurea 10% inhibition at 0.1 mM Homo sapiens
3-(((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)amino)methyl)benzoic acid 32% inhibition at 0.1 mM Homo sapiens
3-((2-(9H-pyrido[3,4-b]indol-9-yl)acetamido)methyl)benzoic acid 21% inhibition at 0.1 mM Homo sapiens
3-((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)carbamoyl)benzoicacid 15% inhibition at 0.1 mM Homo sapiens
3-(3-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)ureido)benzoic acid 36% inhibition at 0.1 mM Homo sapiens
4-(((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)amino)methyl)benzoic acid 22% inhibition at 0.1 mM Homo sapiens
4-((2-(9H-pyrido[3,4-b]indol-9-yl)acetamido)methyl)benzoic acid 25% inhibition at 0.1 mM Homo sapiens
4-((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)carbamoyl)benzoic acid 25% inhibition at 0.1 mM Homo sapiens
4-(3-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)ureido)benzoic acid 52% inhibition at 0.1 mM Homo sapiens
5-[[4-(benzyloxy)phenyl]methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione
-
 Homo sapiens
cambinol
-
 Homo sapiens
ethyl 4-[[2-(9H-pyrido[3,4-b]indol-9-yl)acetamido]methyl]benzoate 12% inhibition at 0.1 mM Homo sapiens
GW5074 85% inhibition at 0.1 mM Homo sapiens
additional information design and synthesis of 9-substituted norharmane derivatives as potential Sirt5 inhibitors, molceular docking, overview Homo sapiens
N-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)benzamide 7% inhibition at 0.1 mM Homo sapiens
N-(4-chlorobenzyl)-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 18% inhibition at 0.1 mM Homo sapiens
N-(pyridin-3-ylmethyl)-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 24% inhibition at 0.1 mM Homo sapiens
N-benzyl-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 8% inhibition at 0.1 mM Homo sapiens
N-benzyl-2-(9H-pyrido[3,4-b]indol-9-yl)ethan-1-amine 10% inhibition at 0.1 mM Homo sapiens
nicotinamide
-
 Homo sapiens
sirtinol
-
 Homo sapiens
suramin
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
 Homo sapiens 5739
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NXA8
-
-

Synonyms

Synonyms Comment Organism
SIRT5
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0126
-
 pH and temperature not specified in the publication Homo sapiens 5-[[4-(benzyloxy)phenyl]methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione
0.0425
-
 pH and temperature not specified in the publication Homo sapiens cambinol
0.0466
-
 pH and temperature not specified in the publication Homo sapiens nicotinamide
0.0466
-
 pH and temperature not specified in the publication Homo sapiens suramin
0.0489
-
 pH and temperature not specified in the publication Homo sapiens sirtinol

General Information

General Information Comment Organism
malfunction because these modifications by Sirt5 cover a broad range of pivotal protein substrates involved in cellular metabolism and metabolic energy homeostasis, aberrant activity of Sirt5 is considered to be a very critical factor for many human diseases, for example, cancer, Alzheimer's disease, and Parkinson's disease Homo sapiens
physiological function Sirt5 has only weak deacetylation, but has robust desuccinylation, demalonylation, and deglutarylation activities in vitro and in vivo. Modifications by Sirt5 cover a broad range of pivotal protein substrates involved in cellular metabolism and metabolic energy homeostasis Homo sapiens