Prof. Laura HEITMAN
Division of Drug Discovery and Safety 
Leiden Academic Centre for Drug Research (LACDR, Leiden University)
Website Prof. Heitman

Program

"Insurmountable antagonists for chemokine receptor CCR2 – from allosteric antagonists to PROTACs"

In early drug discovery pharmaceutical companies optimize the properties of drug candidates for a given therapeutic target, focusing on standard pharmacological parameters of affinity, potency and intrinsic activity. Despite these intensive efforts, the success rate of a candidate drug moving to the preclinical development phase is disappointingly low.

We have recently focused on the chemokine receptor CCR2, which is a G protein-coupled receptor – an important family of drug targets. This receptor is primarily activated by the endogenous chemokine CCL2. Several small molecule antagonists have been developed to inhibit this receptor, as it is involved in many diseases characterized by chronic inflammation. Unfortunately, all these antagonists lack clinical efficacy warranting a better understanding of their mechanism of action.

During this talk, I will show how our work on novel drug discovery concepts, that all result in insurmountable antagonism, contributes to this understanding. Ultimately, these efforts open new avenues for CCR2, and GPCR small molecule drug discovery.

Host: Sonja SUCIC

Contact for questions: Helmut KUBISTA