From Protein Structures to Drug Discovery: Novel therapeutic opportunities.

DATE: November 19, 2020

TIME: 9:00am PT, 12am ET

Knowledge of the three-dimensional structure of therapeutically relevant targets has become an essential step in the pipeline of drug discovery. The X-ray crystallography has been the primary biophysical method for elucidating the 3D- structure of macromolecules and structural information has paved the way for novel pharmaceutical strategies (such as structure-based drug design (SBDD) method). Moreover, protein structures can be exploited by modeling methods to screen for novel ligands or to rationally design ligands. In this webinar, therapeutically relevant proteins will be presented. First, adhesion G protein- coupled receptors (aGPCRs), known for their exceptionally long ectodomains, which extend several hundreds to thousands of amino acids, and they contain important cell adhesion-related domains, including the GPCR autoproteolysis- inducing (GAIN) domain. this domain is conserved among the aGPCR family and is characterized by playing crucial roles in the receptor activation by undergoing an autoproteolysis process. However, the molecular mechanism of this process and the downstream signal transduction mediated by aGPCRs are poorly understood at the structural level. Many researchers have highlighted the critical role of these receptors in promoting or preventing cancer development. Thus, structural and functional studies would trigger future characterization of aGPCRs to explore their potential as therapeutic targets in cancer.

Learning Objectives:

• Discuss membrane proteins, protein complexes, and structural biology
• Discuss X-ray Crystallography, and Cryo-EM
• Discuss Nanobody, GPCRs, and Adhesion GPCRs

LabRoots is approved as a provider of continuing education programs in the clinical laboratory sciences by the ASCLS P.A.C.E. ® Program. By attending this webinar, you can earn 1 Continuing Education credit once you have viewed the webinar in its entirety.