Navigation Links
Emerald BioStructures announces discovery of small molecule modulators of PDE4
Date:12/27/2009

Bainbridge Island, WA. December 28, 2009. Emerald BioStructures (formerly deCODE biostructures) announced today a publication in the December 27, 2009 advance online issue of Nature Biotechnology, detailing the application of structure-based drug design (SBDD) to engineer new allosteric small molecule modulators of the enzyme phosphodiesterase-4 (PDE4), with reduced side effects. According to the paper, the researchers established the structural basis of PDE4 regulation through crystal structures of the PDE4 regulatory domain in contact with small molecules.

"This paper demonstrates Emerald's ability to address key challenges in drug discovery through our world-class X-ray crystallography and structure-based design capabilities," said Lance Stewart, Chief Executive Officer of Emerald BioStructures. "Our approach allows us to deliver valuable, 'game-changing' information in active areas of drug discovery and development, including intracellular protein-protein interactions, as shown in this case. I believe this expertise establishes Emerald BioStructures as a valuable partner to companies that need help solving their important problems in drug discovery, such as reaching historically undruggable targets."

PDE4 is an important therapeutic target, due to its involvement in an array of inflammatory diseases including asthma, psoriasis and COPD, and central nervous system disorders including schizophrenia, Alzheimer's disease, and other cognitive impairments. However, previously developed PDE4 inhibitors have been associated with side effects that have severely limited their potential as potential therapies, and no PDE4 inhibitor has been FDA-approved.

Dr. Alex Burgin, Chief Operating Officer of the Company and one of the corresponding authors on the paper, said, "Establishing novel PDE4 regulatory domain crystal structures enabled our research team to develop small molecules that interact with those regulatory domains and only partially inhibit enzyme activity. As a result, these newly reported modulators do not have the side effects of traditional PDE4 inhibitors, but have maintained therapeutic activity and efficacy in preclinical models of cognition. This is a strong demonstration of Emerald's ability to use its structural-based insights to rationally design enhanced and selective drug candidates."


'/>"/>

Contact: Jennifer Conrad
jconrad@macbiocom.com
781-235-3060
MacDougall Biomedical Communications, Inc.
Source:Eurekalert

Related biology news :

1. Selexis Announces Advanced Approach to Maximize Power of Genetic Elements for Rapid Development of High Performance Cell Lines
2. LaserCard Corporation Announces Expansion of Middle East Project
3. BIO-key(R) Announces Contracts for New Criminal Justice Data Sharing Solution
4. Balzan Foundation announces 2007 winners
5. The American Society of Plant Biologists announces 2007 awards
6. ASPB announces Summer Undergraduate Research Fellowship 2007 recipients
7. NIST announces 56 new awards for innovative technology research and development
8. Titanium Group Announces Contract With Haitong Securities
9. Measurement Specialties, Inc. Announces Impact of German Business Tax Reform 2008 Resulting in Lower Combined German Tax Rate - Impacts 2Q08 Reported Financial Results
10. FIJI Water announces sustainable growth initiative with commitment to help mitigate climate change
11. HGS announces positive Phase 2 LymphoStat-B at ACR meeting
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:5/20/2016)... May 20, 2016  VoiceIt is excited to ... VoicePass. By working together, VoiceIt and ... VoiceIt and VoicePass take slightly different approaches to ... both security and usability. ... this new partnership. "This marketing and ...
(Date:5/9/2016)... 2016 Elevay is currently known ... freedom for high net worth professionals seeking travel for ... connected world, there is still no substitute for a ... sealing your deal with a firm handshake. This is ... advantage of citizenship via investment programs like those offered ...
(Date:4/28/2016)... , April 28, 2016 First quarter ... (139.9), up 966% compared with the first quarter of 2015 ... totaled SEK 589.1 M (loss: 18.8) and the operating margin was ... (loss: 0.32) Cash flow from operations was SEK 249.9 ... 2016 revenue guidance is unchanged, SEK 7,000-8,500 M. The ...
Breaking Biology News(10 mins):
(Date:6/23/2016)... /PRNewswire/ - FACIT has announced the creation of ... company, Propellon Therapeutics Inc. ("Propellon" or "the Company"), ... portfolio of first-in-class WDR5 inhibitors for the treatment ... represent an exciting class of therapies, possessing the ... cancer patients. Substantial advances have been achieved with ...
(Date:6/23/2016)... , June, 23, 2016  The Biodesign Challenge (BDC), ... new ways to harness living systems and biotechnology, announced ... (MoMA) in New York City . ... participating students, showcased projects at MoMA,s Celeste Bartos Theater ... Antonelli , MoMA,s senior curator of architecture and design, ...
(Date:6/23/2016)... June 23, 2016 Apellis Pharmaceuticals, Inc. ... clinical trials of its complement C3 inhibitor, APL-2. ... multiple ascending dose studies designed to assess the ... subcutaneous injection in healthy adult volunteers. ... as a single dose (ranging from 45 to ...
(Date:6/23/2016)... Prairie, WI (PRWEB) , ... June 23, 2016 ... ... consultancy focused on quality, regulatory and technical consulting, provides a free webinar ... is presented on July 13, 2016 at 12pm CT at no charge. , ...
Breaking Biology Technology: