UCB Domainex Combinatorial Domain Hunting MEK kinase


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Domainex\'s CDH technology applied to cancer target, MEK kinase

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UCB Domainex Combinatorial Domain Hunting MEK kinase

  1. 1. This press release is for medical and trade journalists onlyUCB and Domainex collaboration providesvaluable information on cancer drug target• Combinatorial domain hunting technology aids identification of MEK protein suitable for structure-based drug discovery• New structural information allowed UCB scientists to design a novel class of molecules which inhibit MEKSlough/ Cambridge, UK, 12th March 2012: UCB and Domainex Ltd, a UK-based drugdiscovery company, have jointly published the results of a collaboration in the field of cancerdrug discovery. Working together, the two companies have developed an experimentalsystem to study the three-dimensional structure of Mitogen-activated protein kinase kinase(MAPKK, also known as MEK), a protein which is over-active in many human cancers. Usingthe high-resolution structural information, UCB scientists were able to design a novel class ofmolecules which inhibit MEK and which have the potential to combat cancer.The key step in this work, reported in the latest edition of the Journal of Structural Biology,used Domainex’s Combinatorial Domain Hunting (CDH) technology to identify a form of theMEK protein which can be produced in large quantities and which is suitable for structure-based drug discovery. In the case of MEK, this was challenging because conventionalmethods proved unsuccessful, however Domainex’s CDH technology allowed the problem tobe solved rapidly.“The partnership with Domainex has been invaluable for our MEK discovery program.Successful collaborations, such as this, are a key part of UCB’s innovative and cutting-edgeresearch. We hope that the novel class of MEK inhibitors which the UCB team discovered willbring benefits to patients,” said Neil Weir, Senior Vice President, Discovery Research UCB.CDH is a biotechnological method that enables the identification of proteins for drug discoveryand other applications. It involves the random fragmentation of DNA, and the screening ofthousands of DNA fragments to identify those that produce large amounts of the protein ofinterest.Trevor Perrior, Research Director at Domainex said: “Producing high-quality protein is crucialfor successful drug research. Once again, Domainex’s CDH technology has proven to beinvaluable, and the rapid identification of the best form of MEK from tens of thousands ofother possibilities further validates our technology. We were extremely pleased that UCBcould successfully utilize the constructs to generate high-resolution structural informationand, most importantly, to use it to optimize their chemical series.”Further InformationScott Fleming, Head of UK CommunicationsT +447702777378, E scott.fleming@ucb.comJoanne McCudden, Head of Business DevelopmentT +44 07775 437107, E Joanne.mccudden@domainex.co.ukAbout UCBUCB, Brussels, Belgium (www.ucb.com) is a global biopharmaceutical company focused on thediscovery and development of innovative medicines and solutions to transform the lives of people livingwith severe diseases of the immune system or of the central nervous system. With more than 8,000people in about 40 countries, the company generated revenue of EUR 3.2 billion in 2011. UCB is listedon Euronext Brussels (symbol: UCB).Feb 2012: UK/12MIS0021 1/2
  2. 2. Forward looking statements: UCBThis press release contains forward-looking statements based on current plans, estimates and beliefs ofmanagement. All statements, other than statements of historical fact, are statements that could bedeemed forward-looking statements, including estimates of revenues, operating margins, capitalexpenditures, cash, other financial information, expected legal, political, regulatory or clinical resultsand other such estimates and results. By their nature, such forward-looking statements are notguarantees of future performance and are subject to risks, uncertainties and assumptions which couldcause actual results to differ materially from those that may be implied by such forward-lookingstatements contained in this press release. Important factors that could result in such differencesinclude: changes in general economic, business and competitive conditions, the inability to obtainnecessary regulatory approvals or to obtain them on acceptable terms, costs associated with researchand development, changes in the prospects for products in the pipeline or under development by UCB,effects of future judicial decisions or governmental investigations, product liability claims, challenges topatent protection for products or product candidates, changes in laws or regulations, exchange ratefluctuations, changes or uncertainties in tax laws or the administration of such laws and hiring andretention of its employees. UCB is providing this information as of the date of this press release andexpressly disclaims any duty to update any information contained in this press release, either to confirmthe actual results or to report a change in its expectations.There is no guarantee that new product candidates in the pipeline will progress to product approval orthat new indications for existing products will be developed and approved. Products or potentialproducts which are the subject of partnerships, joint ventures or licensing collaborations may be subjectto differences between the partners. Also, UCB or others could discover safety, side effects ormanufacturing problems with its products after they are marketed.Moreover, sales may be impacted by international and domestic trends toward managed care andhealth care cost containment and the reimbursement policies imposed by third-party payers as well aslegislation affecting biopharmaceutical pricing and reimbursement.About DomainexDomainex uses unique and proprietary technologies to resolve common bottlenecks facing thepharmaceutical and biotechnology industries in the post-genomic era. Major discovery gaps existbetween the vast amount of genomic information that is now available, the accessibility of thecorresponding proteins for use in target validation and drug discovery, and the identification of robusthits in a cost effective manner. Founded in 2001, Domainex is a privately owned company based inCambridge, UK.Domainex has developed a discovery platform, which enables rapid progression of drug discoveryprojects from novel target through to Candidate Drug by means of its Combinatorial Domain Huntingtechnology, LeadBuilder virtual hit screening software, and its integrated approach to medicinal andcomputational chemistry.Domainex’s patented CDH technology enables the cloning and expression of soluble drug target proteindomains in E. coli, followed by the identification of those constructs that are able to bind a ligand. Thisenables binding assays to be developed, facilitating hit identification studies. In only 3-4 months, allexpressible ligand binding domains of a target protein are identified (from libraries of 20,000-100,000constructs), enabling key rate limiting steps in early drug discovery to be easily overcome and resultingin large time savings over standard approaches.Domainex has also developed LeadBuilder - a virtual screening approach for targets which is specificallyaimed at quickly identifying hit molecules that are ideally suited for further development.The experienced medicinal chemistry team has a proven track record in supporting biotech or universitygroups by providing expertise to take hit compounds through lead optimization and on to candidateselection. Three compounds to date arising from these collaborations are currently in clinicalevaluation, with two additional drugs in preclinical studies.References1. Meier C, Brookings DC, Ceska TA, Doyle C, Gong H, McMillan D, Saville GP et al. Engineering human MEK for structural studies: A case study of combinatorial domain hunting. Journal of Structural Biology (2012); 177:329-34.Feb 2012: UK/12MIS0021 2/2