Journal article

Challenges in the design of insulin and relaxin/insulin-like peptide mimetics

Mohammed Akhter Hossain, Ross AD Bathgate

BIOORGANIC & MEDICINAL CHEMISTRY | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2018

Abstract

Peptidomimetics are designed to overcome the poor pharmacokinetics and pharmacodynamics associated with the native peptide or protein on which they are based. The design of peptidomimetics starts from developing structure-activity relationships of the native ligand-target pair that identify the key residues that are responsible for the biological effect of the native peptide or protein. Then minimization of the structure and introduction of constraints are applied to create the core active site that can interact with the target with high affinity and selectivity. Developing peptidomimetics is not trivial and often challenging, particularly when peptides' interaction mechanism with their targ..

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Grants

Awarded by NHMRC (Australia) project


Awarded by ARC


Funding Acknowledgements

This research was partly funded by NHMRC (Australia) project grants (1122170, 1023321, 1065481, and 1100676) and ARC linkage grant (LP120100654) to M.A.H. and R.A.D.B. Research at The Florey Institute of Neuroscience and Mental Health is supported by the Victorian Government Operational Infrastructure Support Program. Some of the figures were prepared by Praveen, a PhD student at the Florey.