Selcia Introduces New Prolyl Isomerase Screening Service
News Feb 01, 2013
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”.
Microorganisms often assemble natural products similar to industrial assembly lines. Certain enzymes, non-ribosomal peptide synthetases (NRPS) play a key role in this process. Biotechnologists have now discovered how these enzymes interact with each other, bringing them one step closer to their goal of engineering peptide natural products.READ MORE