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Gaining ground with GPCRs
April 2013
by Kelsey Kaustinen  |  Email the author


BRUSSELS, BelgiumóUCB and ConfometRx, a structural biology company based in Santa Clara, Calif., announced in late February the launch of a research agreement for the discovery of novel medicines to address unmet medical needs in the field of neuroscience. No specific financial terms were disclosed, but the agreement will include an upfront payment, as well as research funding and success- based milestone payments.  
The agreement will run two years and focus on multiple targets, and the two partners will use structural biology to examine G-protein coupled receptor (GPCR) modulation for the design of differentiated drugs. UCB, for its part, brings to the partnership its expertise in the field of central nervous system diseases, which is one of the company's two primary focuses, as well as experience with both "large, antibody-based molecules and small, chemically derived molecules."  
ConfometRx, in turn, drives its drug discovery approach with a platform of "structure-based drug discovery technologies to facilitate lead identification and lead optimization" for GPCRs, including the generation of GPCR-specific functional antibodies.  
GPCRs represent the largest family of signaling proteins in the human genome, and are linked to nearly every physiological process in the body, making them the largest target class for drug discovery today. ConfometRx notes on its website that "clinical indications for GPCRs include cardiovascular, pulmonary, metabolic and psychiatric disorders, as well as inflammation, cancer and HIV infection."
"GPCR crystallization remains a challenge and requires state-of-the-art technologies as well as expertise. Prof. Brian Kobilka is the first to have succeeded in crystallizing a GPCR target in the active state and was awarded the chemistry Nobel prize for his work in the field of GPCR structural biology," Ismail Kola, executive vice president and president of NewMedicines at UCB, said in a press release. "We look forward to working with ConfometRx as part of our continued strategy to innovate in drug discovery, transforming knowledge and insight into health-changing invention. We strive to fulfill our mission of discovering new medicines that aim to improve the lives of people living with severe diseases. The collaboration with ConfometRx is another example of UCB's strategies at work, where we are continuing to build supernetworks of innovation that are aimed at creating superior and sustainable value for patients."  
ConfometRx notes on its website that developing antibodies for GPCRs is a difficult task due to factors such as tolerance and the fact that many GPCRs have only a small amount of available hydrophilic surface area. ConfometRx, however, notes it "has developed a method of preparing antigenic proteoliposomes containing a high density of purified, native GPCRs. This approach has been used to generate conformationally sensitive antibodies that recognize more than just a single linear epitope. This affords the antibodies higher affinity and greater selectivity."  
"We are delighted to be working with UCB's world-class central nervous system research group to enhance their drug development activities," Tong Sun Kobilka, CEO of ConfometRx, commented in a statement. "With over 20 years of experience working in the coupled receptor field and our unique technological approach, we believe that we can bring significant value to UCB's novel drug development process. We look forward to working closely with UCB's R&D teams."  
Neither company could be reached for additional comments on the deal.  
The agreement is the second central nervous system-focused partnership for UCB in recent months, as UCB also announced in mid-March a strategic discovery collaboration with FivePrime Therapeutics Inc. to discover biologics targets and therapeutics in the fields of fibrosis-related inflammatory diseases and central nervous system disorders. Per the agreement, the partners will collaborate on the design of assays to screen FivePrime's proprietary library of roughly 5,600 secreted proteins and transmembrane receptor proteins (ligand traps), and FivePrime will leverage its technology platforms to identify potential drug targets and candidates for the chosen fields.
Code: E041320



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