Our group is involved in the discovery and development of new molecules targeting 5-lipoxygenase-activating protein (FLAP) and microsomal prostaglandin E2 synthase (mPGES-1), which are important targets for treatment of chronic inflammatory and cardiovascular diseases as well as cancer. An important aspect of our research activities includes the combined use of chemical, computational and pharmacological tools in order to eventually provide new chemotypes for novel therapies of inflammation-related disorders. Our efforts led to the discovery of selective and multi-target inhibitors of both FLAP and mPGES-1, such as BRP-7 and BRP-187. We think that BRP-7 and BRP-187 can be valuable chemical probes to study the LT and PG mediated pathways in the AA cascade. We work closely with Prof. Oliver Werz (University of Jena, Germany) for the study of the mechanistic properties of our newly developed molecules in our ongoing studies.
Our group in collaboration with Prof. Özgür Şahin (University of South Carolina, United States) also focuses on the development of new Transforming acidic coiled-coil-containing protein 3 (TACC3) inhibitors as drug candidates for treatment of various cancers. TACC3, a transforming acidic coiled-coil family member, is frequently upregulated in a broad spectrum of cancers. It plays critical roles in protecting microtubule stability and centrosome integrity that is often dysregulated in cancers; therefore, making TACC3 a highly attractive therapeutic target. Our recently developed molecule BO-264 is one of the most potent TACC3 inhibitors known in the literature so far. We work closely with Prof. Şahin for further development of BO-264 into a drug-like candidate, which can be of value for treatment of different types of cancers including breast and colon.
More to follow very soon. Watch this space!