Leveraging ChemBridge Libraries in Cancer Research

More than 1,500 articles cite the use of ChemBridge^® small molecule screening libraries and compounds in a wide variety of research areas using high-throughput screening or focused screening following computer-aided screening. The list below highlights a small sampling of articles, from 2014 to present, that focus on work in cancer research and provides a sample of the different techniques employed and targets explored in hit finding and probe discovery using ChemBridge libraries and compounds.

Identification of a Selective G1- Phase Benzimidazolone Inhibitor by a Senescence-Targeted Virtual Screen Using Artificial Neural Networks
Bilsland AE, et al.; Neoplasia. 2015 Sep;17(9):704-15. doi: 10.1016/j.neo.2015.08.009 The authors identified CB-20903630 ChemBridge ID 20903630, as a senescence associated beta-galactosidase inhibitor using virtual screening as the primary screen.

Estrogen receptor alpha inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression
Andruska ND, et al.; Proc Natl Acad Sci U S A. 2015 Mar 30. pii: 201403685. [Epub ahead of print].
The authors identified BHPI (ChemBridge ID 6373538) as an estrogen receptor alpha biomodulator using a high-throughput screen as the primary screen.

A novel pyruvate kinase M2 activator compound that suppresses lung cancer cell viability under hypoxia
Kim DJ, et al.; Mol Cells. 2015 Apr;38(4):373-9. doi: 10.14348/molcells.2015.2314. Epub 2015 Mar 26.
The authors identified PA-12 (ChemBridge ID 7871820) as pyruvate kinase M2 activator using a virtual screen as the primary screen.

Anticancer/Antiviral Agent Akt Inhibitor-IV Massively Accumulates in Mitochondria and Potently Disrupts Cellular Bioenergetics
Meinig JM and Peterson BR.; ACS Chem Biol. 2015 Feb 20;10(2):570-6. doi: 10.1021/cb500856c. Epub 2014 Dec 1.
The authors had previously identified AKTIV (Akt Inhibitor-IV; ChemBridge ID 5233705) as an PI3-kinase/Akt (protein kinase B) inhibitor and focused on elucidation of the mechanism of action.

Targeted inhibition of cell-surface serine protease Hepsin blocks prostate cancer bone metastasis
Tang X, et al.; Oncotarget. 2014 Mar 15;5(5):1352-62
The authors had previously identified HepIN-13 (ChemBridge ID 5717483) as serine protease Hepsin inhibitor and focused on the development, analysis and animal trial of the inhibitor.

Structure-based discovery of a small non-peptidic Neuropilins antagonist exerting in vitro and in vivo anti-tumor activity on breast cancer model
Borriello L et al. ; Cancer Lett. 2014 Jul 28;349(2):120-7. doi: 10.1016/j.canlet.2014.04.004. Epub 2014 Apr 19.
The authors identified Compound 1 (ChemBridge ID 7967674) as a neuropilins (non-tyrosine kinase receptor) antagonist using a virtual screen as the primary screen.

Activation of the Proapoptotic Bcl-2 Protein Bax by a Small Molecule Induces Tumor Cell Apoptosis
Zhao G et al.; Mol Cell Biol. 2014 Apr;34(7):1198-207. doi: 10.1128/MCB.00
996-13. Epub 2014 Jan 13; The authors identified Compound 106 (ChemBridge ID 78872106) as a proapoptotic Bcl-2 protein Bax activator using a virtual screen as the primary screen.

Discovery of SIRT3 Inhibitors Using SAMDI Mass Spectrometry
Patel K et al.; J Biomol Screen. 2015 May 29. pii: 1087057115588512. [Epub ahead of print]
The authors identified SDX-437 (ChemBridge ID 7706915) as a sirtuin deacytelase 3 (SIRT3) inhibitor using a high-throughput screen.

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