Gaining ground with GPCRs

UCB, ConfometRx partner on novel neuroscience medicines

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BRUSSELS, Belgium—UCB and ConfometRx, a structural biologycompany based in Santa Clara, Calif., announced in late February the launch ofa research agreement for the discovery of novel medicines to address unmetmedical needs in the field of neuroscience. No specific financial terms weredisclosed, but the agreement will include an upfront payment, as well asresearch funding and success-based milestone payments.
The agreement will run two years and focus on multipletargets, and the two partners will use structural biology to examine G-proteincoupled receptor (GPCR) modulation for the design of differentiated drugs. UCB,for its part, brings to the partnership its expertise in the field of centralnervous system diseases, which is one of the company's two primary focuses, aswell as experience with both "large, antibody-based molecules and small,chemically derived molecules."
ConfometRx, in turn, drives its drug discovery approach witha platform of "structure-based drug discovery technologies to facilitate leadidentification and lead optimization" for GPCRs, including the generation ofGPCR-specific functional antibodies.
GPCRs represent the largest family of signaling proteins inthe human genome, and are linked to nearly every physiological process in thebody, making them the largest target class for drug discovery today. ConfometRxnotes on its website that "clinical indications for GPCRs includecardiovascular, pulmonary, metabolic and psychiatric disorders, as well asinflammation, cancer and HIV infection."
"GPCR crystallization remains a challenge and requiresstate-of-the-art technologies as well as expertise. Prof. Brian Kobilka is thefirst to have succeeded in crystallizing a GPCR target in the active state andwas awarded the chemistry Nobel prize for his work in the field of GPCRstructural biology," Ismail Kola, executive vice president and president ofNewMedicines at UCB, said in a press release. "We look forward to working withConfometRx as part of our continued strategy to innovate in drug discovery,transforming knowledge and insight into health-changing invention. We strive tofulfill our mission of discovering new medicines that aim to improve the livesof people living with severe diseases. The collaboration with ConfometRx isanother example of UCB's strategies at work, where we are continuing to buildsupernetworks of innovation that are aimed at creating superior and sustainablevalue for patients."
ConfometRx notes on its website that developing antibodiesfor GPCRs is a difficult task due to factors such as tolerance and the factthat many GPCRs have only a small amount of available hydrophilic surface area.ConfometRx, however, notes it "has developed a method of preparing antigenicproteoliposomes containing a high density of purified, native GPCRs. Thisapproach has been used to generate conformationally sensitive antibodies thatrecognize more than just a single linear epitope. This affords the antibodieshigher affinity and greater selectivity."
"We are delighted to be working with UCB's world-classcentral nervous system research group to enhance their drug developmentactivities," Tong Sun Kobilka, CEO of ConfometRx, commented in a statement."With over 20 years of experience working in the coupled receptor field and ourunique technological approach, we believe that we can bring significant valueto UCB's novel drug development process. We look forward to working closelywith UCB's R&D teams."
Neither company could be reached for additional comments onthe deal.
The agreement is the second central nervous system-focusedpartnership for UCB in recent months, as UCB also announced in mid-March astrategic discovery collaboration with FivePrime Therapeutics Inc. to discoverbiologics targets and therapeutics in the fields of fibrosis-relatedinflammatory diseases and central nervous system disorders. Per the agreement,the partners will collaborate on the design of assays to screen FivePrime'sproprietary library of roughly 5,600 secreted proteins and transmembranereceptor proteins (ligand traps), and FivePrime will leverage its technologyplatforms to identify potential drug targets and candidates for the chosenfields.

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