Selcia Limited Introduces New Prolyl Isomerase Screening Service
Published: Nov 27, 2012
The scope of service encompasses drug screening and functional assays, as well as profiling of compounds and determining specificity of inhibition against a representative panel of enzymes.
Whilst relatively neglected by pharmaceutical companies in the past, understanding of the involvement of PPIases in many diseases is currently emerging. All PPIase inhibitors presently in clinical use or in development are natural products, natural product derivatives or have structures inspired by natural products. By combining its in-house expertise in screening services and medicinal chemistry, Selcia has already commenced delivery of clinical PPIase inhibitors to pharma clients.
The principal function of PPIases is to catalyse the cis-trans isomerisation of the X-Pro peptide bonds in polypeptide chains (where X is any amino acid). The isomerisation of peptide bonds to proline is more difficult than that of non-proline peptide bonds and is of physiological relevance in protein folding and in shape changes of fully folded proteins. This latter aspect represents an “on-off switch” of physiological properties of proteins.
Selcia has developed assays for members of all PPIase families and is constantly expanding the set of enzymes available for screening and profiling. Inhibitors of PPIases have important therapeutic potential in the area of infections (viruses, bacteria, yeast and moulds, and protozoa), inflammation, neuroprotection and cancer.
Simon Bury, Business Development Director – Discovery, comments: “PPIases are a large and unexploited family of drugable targets. They are not amenable to HTS and assays are difficult. Selcia is the only company offering this PPIase screening service and has the capability to take a PPIase target from hit finding to candidate stage. Selcia’s unique panel of PPIase screening assays was developed by our biology team to enable screening of compounds designed and synthesised by our medicinal chemists for several integrated drug discovery programs. We are delighted to be able to offer this panel of PPIases assays to researchers working in this area”.
Selcia (www.selcia.com) is a leading provider of contract research services to the global life science industry. The company’s headquarters are in Ongar, Essex and we have a branch in Hopkinton, MA.
Selcia operates two divisions, Selcia Discovery, which provides integrated small molecule drug discovery to pharmaceutical and biotech clients, and Selcia Radiochemistry which specializes in 14C GMP radiolabelling. In addition to general medicinal chemistry and biology capabilities applicable across a broad range of target classes, Selcia Discovery has particular strengths in three unique and highly synergistic technologies:
(1) protein-protein interaction targets, in particular peptidyl-prolyl isomerases
. (2) Capillary electrophoresis-based fragment and natural product screening
(3) Medicinal chemistry of complex natural products
Whilst relatively neglected by pharmaceutical companies in the past, understanding of the involvement of PPIases in many diseases is currently emerging. All PPIase inhibitors presently in clinical use or in development are natural products, natural product derivatives or have structures inspired by natural products.
The combination of these technologies has enabled Selcia to deliver several clinical PPIase inhibitors to clients, but has also generated IP for Selcia, which we have recently demerged into a new company, Mitopharm Limited which is in advanced license negotiations for a breakthrough drug in the field of acute and chronic neurodegenerative diseases. Other applications in the fields of chronic inflammatory diseases, oncology, COPD, and viral infections will be developed by Mitopharm either via investment or via joint R&D programs with pharmaceutical companies.
Selcia has also recently established Selcia Pharma, a spin out company focussed on the optimisation/preclinical development and partnering of Selcia’s internal preclinical antimicrobial (antibacterial & antifungal) assets. Selcia’s headquarters are in Ongar, Essex UK and the company has a branch in Hopkinton, Massachussetts.
All media enquiries:
Phone: +44 7967 153753
For further details about Selcia’s PPIase screening service please contact:
Business Development Director – Discovery
Phone: +44 1277 367000