Owning to the complexity of the human immune system, it has proven challenging to discern its role in the causality of a broad spectrum of diseases such as oncology, neurology, and immunology. Thus, a scientific and medical need remains to develop drugs that can selectively target specific immune cells to deconvolute the mechanisms leading to disease progression. Our focus has been on identifying selective high potency kinase inhibitors to address this unmet medical need for over a decade. This work led to the discovery of drug candidates that have advanced to clinical studies to treat diseases such as CLL, SLE, and MS. The presentation will provide a synopsis of the challenges encountered and highlight the successful strategies employed during the medicinal chemistry campaign. Starting from novel chemical matter identified from a fragment-based screen, prioritizing molecules with improved drug-like properties was a contributing factor in evading the typical pitfalls of hit identification and lead optimization stages. In parallel, Structure-Based Drug Design (SBDD) was employed to guide the optimization of potency and selectivity for preclinical validation of novel autoimmune mechanisms in a range of clinically relevant diseases.

The development of selective kinase inhibitors to treat autoimmune disease “ finding a cure for Dr. Jekyll and Mr. Hyde”

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.