San Diego, CA, September 07, 2013 --(PR.com
)-- Lixin Qiao, Principal Scientist at Celgene will give a presentation on “Discovery of an Irreversible PI3Ka-specific Inhibitor” at the 2nd Protein Kinases & Drug Design Conference to be held in San Diego, CA on October 24-25, 2013 by GTC.
The PI3K pathway, which regulates cell growth, proliferation and survival, is activated in many types of human tumors by mutational activation of PI3Ka, PTEN inactivation, or activation of upstream receptor tyrosine kinases. Several PI3K inhibitors are currently in clinical development, but most are pan-PI3K inhibitors. Tumor biology data suggests that targeting PI3Ka specifically should be efficacious, and there may be advantages to not disrupting other members of the complex PI3K signaling cascade. Using structure-based drug design (SBDD), Celgene has discovered a series of small molecules that selectively inhibit PI3Ka via the formation of an irreversible covalent bond. In addition to the enhanced pharmacodynamics achieved through permanent silencing of targets, covalent inhibitors also exhibit key advantages in terms of selectivity and retained activity against drug-resistant mutant targets. CNX-1351 is introduced as an example to demonstrate PI3Ka-specific inhibition, prolonged PD inhibiting p-AKTSer473, and in vivo efficacy inhibiting SKOV3 tumor growth.
Kinases, key drivers of malignant transformation and major contributors to a variety of other human pathologies, have emerged as some of the most exciting targets in drug discovery. However, with initial well documented success stories came realization that many hurdles lie in the path of successful development of new drugs, targeting kinase signaling. GTC’s 2nd Protein Kinases & Drug Design Conference will bring together speakers representing world leading academic centers and pharmaceutical companies to discuss how to overcome the many hurdles and answer exciting key questions.
This conference is part of our Protein Discovery Summit 2013, which includes three additional parallel conferences shown below:
Protein Kinases & Drug Design
Antibody & Protein Therapeutics
Protein Expression, Purification & Characterization
For more information, please visit www.gtcbio.com