News item posted on 2015-07-17

Research Spotlight - Stephen Fesik

CSB Researcher Stephen Fesik, Ph.D., was recently highlighted in ACS Chemical Research in Toxicology for his research involving the antiapoptotic protein myeloid cell leukemia-1 (Mcl-1).

Dr. Fesik led a team to identify small molecule inhibitors that bind Mcl-1, which is overexpressed and amplified in many human cancers. Mcl-1 is also associated with poor survival, as it allows cancer cells to evade apoptosis and is implicated in chemotherapy resistance.

The findings, published in the Journal of Medicinal Chemistry, report that C-ring modifications can enhance Mcl-1 interactions and improve binding affinity, as can substituting methyl groups at R1 or R2 positions.

Although there are currently no available therapies that selectively target Mcl-1, the compounds that successfully neutralize it can potentially restore successful regulation of apoptosis and enhance responses to cancer treatment.

Read the review in ACS Chemical Research in Toxicology.

Author: Karen D. Davis