Navigation Links
Receptos Scientists Publish Determination of a High Resolution Sphingosine 1-Phosphate Receptor 1 Structure in Science
Date:2/16/2012

SAN DIEGO, Feb. 16, 2012 /PRNewswire/ -- Receptos Inc. announced today the publication of key results relating to its expertise in S1P1 biology and structure-based drug discovery for high-value G-protein-coupled receptor (GPCR) targets in Science.

The article, entitled "Crystal Structure of a Lipid G Protein-Coupled Receptor," was co-authored by Receptos in collaboration with scientific founders Hugh Rosen, M.D., Ph.D., and Raymond Stevens, Ph.D. Drs. Rosen and Stevens are both professors at The Scripps Research Institute®, with expertise in immunology and lymphocyte trafficking and GPCR crystallography, respectively. Receptos is the exclusive licensee of the GPCR crystal structure determination technology platform, developed at The Scripps Research Institute®, which enabled the elucidation of the S1P1 receptor structure.

"Receptos and its founders have an unparalleled track record in the determination of high resolution GPCR structures to enable rational drug design," said Faheem Hasnain, President and Chief Executive Officer of Receptos. "The publication of the S1P1 structure in Science highlights the importance of this therapeutic target and Receptos's leading position in decoding receptor-ligand interactions for pharmaceutically relevant GPCR targets. Our expertise in the S1P1 field has resulted in the discovery of a best-in-class small molecule agonist, RPC1063, which is scheduled to initiate Phase 2 clinical studies in multiple sclerosis and inflammatory bowel disease later this year."

Receptos utilizes the GPCR crystal structure determination technology platform to assist in building a pipeline of high-value therapeutic candidates. In addition to RPC1063, the technology supports a small molecule glucagon-like peptide 1 (GLP1) research program, which has demonstrated proof of concept in in vivo models of type 2 diabetes. Receptos has also initiated technology collaborations to conduct novel drug screening assays and study dynamic conformational changes to receptor topography that allow rational drug design for high-value GPCR targets. These collaborators include Eli Lilly, Ono Pharmaceutical and Janssen Pharmaceuticals.

Advancements in the technology, as well as in proprietary drug discovery and development programs at Receptos, have resulted in a patent estate comprising twelve patent applications, seven of which are directed to small molecule composition of matter and four of which support the technology platform, including novel reagents to enable crystallography. The Receptos scientific management team has broad experience in the development and registration of therapeutics including rituximab, targretin, panretin, belatacept, abatacept, omalizumab, and others.

About the S1P1 Target and Utilization of the S1P1 Structure

The lyso-phospholipid sphingosine 1-phosphate modulates lymphocyte trafficking, endothelial development and integrity, heart rate, and vascular tone and maturation by activating G protein–coupled sphingosine 1-phosphate receptors. Activation of the S1P1 receptor through exogenous ligands, both physiological and pharmacological, results in significant inhibition of lymphocyte re-circulation. This physiological effect was leveraged in the development of the nonselective S1P receptor agonist prodrug fingolimod (GILENYA®), approved in 2010 for the clinical treatment of relapsing-remitting multiple sclerosis. The high resolution crystal structure of the sphingosine 1-phosphate receptor 1 has revealed the architecture of the ligand binding pocket and extracellular region providing insights into the molecular interactions associated with binding and signaling of diverse S1P ligands. In combination with mutagenesis and signaling studies, Receptos has pinpointed regions in the binding pocket responsible for driving interactions within S1P ligand classes, and prioritized drug candidates accordingly.

About GPCR Protein Crystal Structure Determination Technology

GPCR receptors are the largest single drug discovery protein family, yet many high-value targets have been intractable to traditional drug discovery techniques. Receptos offers a paradigm-shifting technology that enables, for the first time, structure-based drug design for this important target class. This unique offering delivers novel drug discovery tools along the path to structure determination, including the generation of purified GPCR protein (to allow biophysical ligand screening and therapeutic antibody candidate generation), the identification of novel receptor binding sites such as allosteric sites (to confer improved potency and selectivity profiles to drug candidates), and GPCR structure determination to transform drug discovery. Receptos's proprietary technology platform was exclusively licensed from The Scripps Research Institute® and has been further advanced by the company into the disciplines of drug discovery and development.

About Receptos

Receptos is a biopharmaceutical company developing autoimmune therapeutic candidates through information-driven drug discovery, including GPCR structure determination. The company's lead program is a best-in-class S1P1 small molecule agonist candidate for autoimmune indications, including multiple sclerosis and inflammatory bowel disease, which will complete a Phase 1 clinical study in the first quarter of 2012. The S1P1 program is supported by the company's proprietary high resolution protein crystal structure of the S1P1 receptor. Receptos has established partnerships for its GPCR structure determination technology platform with Eli Lilly, Ono Pharmaceutical and Janssen Pharmaceuticals, Inc. For more information visit www.receptos.com.

Media and Investor Contacts:

Russo Partners
Ian Stone or David Schull (media)
(619) 308-6541 or (212) 845-4271
Ian.stone@russopartnersllc.com 
David.schull@russopartnersllc.com

Cindy McGee (investors)
(619) 308-6538
Cindy.mcgee@russopartnersllc.com

 


'/>"/>
SOURCE Receptos
Copyright©2010 PR Newswire.
All rights reserved

Related biology technology :

1. Receptos and Ono Establish Collaboration with Focus on Bioactive Lipid Discovery Research
2. Scientists decode brain waves to eavesdrop on what we hear
3. Chinese Scientists Zhen-Yi Wang and Zhu Chen Awarded 7th Annual Szent-Gyorgyi Prize for Progress in Cancer Research
4. iBioSeminars and iBioMagazine: Free, Online Biology Seminars and Short Talks by Leading Scientists
5. Scientists solve mystery of colorful armchair nanotubes
6. Nanowiggles: Scientists discover graphene nanomaterials with tunable functionality in electronics
7. Sheffield scientists shine a light on the detection of bacterial infection
8. Singapore scientists lead human embryonic stem cell study
9. Scientists defuse the Vietnam time bomb
10. Scientists carve nanowires out of ultrananocrystalline diamond thin films
11. Berkeley Lab scientists develop new tool for the study of spatial patterns in living cells
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:6/27/2016)... , ... June 27, 2016 , ... ... bring innovative medical technologies, services and solutions to the healthcare market. The company's ... of various distribution, manufacturing, sales and marketing strategies that are necessary to help ...
(Date:6/27/2016)... 2016  Liquid Biotech USA ... a Sponsored Research Agreement with The University of ... from cancer patients.  The funding will be used ... with clinical outcomes in cancer patients undergoing a ... be employed to support the design of a ...
(Date:6/24/2016)... on a range of subjects including policies, debt and investment ... Speaking at a lecture to the Canadian Economics ... the country,s inflation target, which is set by both the ... "In certain areas there needs to be frequent ... not sit down and address strategy together?" He ...
(Date:6/24/2016)... ... June 24, 2016 , ... While the majority of commercial ... Cary 5000 and the 6000i models are higher end machines that use the more ... the spectrophotometer’s light beam from the bottom of the cuvette holder. , FireflySci ...
Breaking Biology Technology:
(Date:5/12/2016)... 2016 WearablesResearch.com , a brand of ... results from the Q1 wave of its quarterly wearables ... consumers, receptivity to a program where they would receive ... insurance company. "We were surprised to see ... Michael LaColla , CEO of Troubadour Research, "primarily because ...
(Date:4/28/2016)... , April 28, 2016 Infosys ... (NYSE: INFY ), and Samsung SDS, a global ... that will provide end customers with a more secure, fast ...      (Logo: http://photos.prnewswire.com/prnh/20130122/589162 ) , ... but it also plays a fundamental part in enabling and ...
(Date:4/26/2016)... -- Research and Markets has announced the ...  report to their offering.  , ,     (Logo: ... forecast the global multimodal biometrics market to grow ... 2016-2020.  Multimodal biometrics is being implemented ... healthcare, BFSI, transportation, automotive, and government for controlling ...
Breaking Biology News(10 mins):