Drug Discovery

March 2015

News Highlight

PARPs as cancer drug targets - first EC-approved drug

Recently, the European commission approved the first drug directed against a member of the PARP family (Poly ADP-Ribose Polymerases): Olaparib, a drug against ovarian cancer. This product blocks PARP1, an enzyme involved in cell repair, and is designed for ovarian cancer patients with certain hereditary gene mutations. It also has promise in treating other cancers, including breast and gastric tumors, opening up a substantial market opportunity.

Product Focus

PARP inhibitors involved in Cancer and Parkinson research

Poly (ADP-ribose) polymerase (PARP) is a family of proteins which†catalyze the NAD-dependent addition of Poly ADP-ribose (PAR) chains to nuclear proteins. PARPs play key signaling roles in apoptosis, DNA excision and repair, telomere stability, and chromatin structure. PARPs are also involved in transcriptional regulation of several signaling pathways, including genes involved in cancer and inflammation...


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Current News

Immunotherapy Screening - IDO pathway

The indoleamine 2,3-dioxygenase (IDO) pathway is the next hot target behind the PD-1 and CTLA pathways for developing a new class of immunotherapeutic anticancer agents.
In this post, Dr el Bay‚ takes a look at the IDO1 Inhibitor Screening Assay Kit designed to measure IDO1 enzyme inhibition in the IDO pathway...

Microtubule destabilization by Suprafenacine: template for novel anti-cancer drugs

Recently, B.-H. Choi et al. characterized a novel anti-mitotic molecule termed Suprafenacine which destabilizes microtubules, resulting in cell cycle arrest in the G2/M phase and apoptotic cell death. This cell-permeable compound can serve as a template for designing and synthesizing future anti-cancer drugs. Learn more

Technical Corner

Ali gives you some advice on easily detecting luciferase activity in cell based assays...

"Luciferase is the general term given to a class of oxidative enzymes which†catalyze reactions that give off light, a process known as bioluminescence.
In biology, researchers take advantage of this reaction to†use it as a readout for various biological processes. This has perhaps been exploited most in luciferase reporter cell lines where a promoter region from a gene of interest is placed immediately upstream of the coding sequence for luciferase. In this system, transcriptional activation of the gene of interest leads to a level of luciferase expression that is proportional to the level of gene activation..." Read more...

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