scholarly journals Structure-Based Design of Flavonoid Compounds As a New Class of Small-Molecule Inhibitors of the Anti-apoptotic Bcl-2 Proteins

2007 ◽  
Vol 50 (14) ◽  
pp. 3163-3166 ◽  
Author(s):  
Guozhi Tang ◽  
Ke Ding ◽  
Zaneta Nikolovska-Coleska ◽  
Chao-Yie Yang ◽  
Su Qiu ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
New Class ◽  
Flavonoid Compounds

scholarly journals Screening for Caspase-3 Inhibitors: A New Class of Potent Small-Molecule Inhibitors of Caspase-3

2006 ◽  
Vol 11 (3) ◽  
pp. 277-285 ◽  
Author(s):  
Ilya Okun ◽  
Sergei Malarchuk ◽  
Elena Dubrovskaya ◽  
Alexander Khvat ◽  
Sergey Tkachenko ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput Screening ◽  
Caspase 3 ◽  
Small Molecule Inhibitors ◽  
High Potency ◽  
New Class ◽  
Mechanistic Analysis ◽  
Compound Collection ◽  
Induced Apoptosis

From the authors'650,000 compound collection, they have selected approximately 15,000 potential small-molecule protease inhibitors, which were subjected to high-throughput screening against caspase-3. The screening yielded a series of hits that belong to 11 different scaffolds. Based on the structure of one of the hits, a new class of the small-molecule inhibitors with a double electrophilicwarhead, 8-sulfonyl-pyrrolo[3,4-c]quinoline-1,3-diones (SPQ), was synthesized and tested in follow-up mechanistic and antiapoptosis assays. Mechanistic analysis of a representative compound of this class, CD-001-0011, showed that the compound exhibited a high potency (IC 50 = 130 nM), was reversible though noncompetitive, and had a broad selectivity profile to other caspases belonging to groups I to III. The compound was effective in preventing staurosporineinduced apoptosis in a few cell lines and retinoic acid–induced apoptosis in zebrafish.

scholarly journals Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics

2018 ◽  
Vol 4 (7) ◽  
pp. 1130-1145 ◽  
Author(s):  
Rahul Tyagi ◽  
Amarendar Reddy Maddirala ◽  
Mostafa Elfawal ◽  
Chelsea Fischer ◽  
Christina A. Bulman ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Metabolic Enzymes ◽  
New Class

scholarly journals The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity

2012 ◽  
Vol 3 (5) ◽  
pp. 352-356 ◽  
Author(s):  
Mark J. Robertson ◽  
Gordana Hadzic ◽  
Joseph Ambrus ◽  
D. Yuri Pomè ◽  
Emily Hyde ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Gtpase Activity ◽  
New Class
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