Synthesis of conformationally restricted b-turn mimetics for incorporation into peptide hormones used as drugs

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Project objective

Research objectives and content The project describes an innovative and general approach to the synthesis of conformationally restricted mimetics of b-turns in biologically active peptides and proteins. The approach will be applied to the peptides hormones vasopressin, oxytocin and LHRH which are used as drugs. The pharmacodynamic and pharmacokinetic properties of the resulting hormone analogues will be evaluated in collaboration with FERRING Pharmaceuticals in Malmoe Sweden. It is expected that the analogues will display increased stability on oral administration, resulting in prolonged duration, and that information on the biologically active conformation of the hormones will be obtained. Training content (objective, benefit and expected impact) The project will widen my knowledge in synthetic organic chemistry, especially in synthesis of peptides, and also give me insight into very modern techniques like combinatorial chemistry, molecular modelling and conformational studies of peptides and peptidomimetics. All these techniques are of great interest and relevance for my planned career in chemical industry. In Addition, I will learn a new language (Swedish) and will widen my knowledge in English by permanent training. Links with industry / industrial relevance (22) The pharmacological properties of the synthetic peptidomimetics to be prepared in this project will be evaluated in collabo- ration with FERRING Pharmaceuticals in Malmoe Sweden. FERRING's main products are analogues of the hormones vasopressin and oxytocin which are used in treatment of diabetis insipidus and premature labour, respectively. In addition, the group is collaborating with PHARMACIA Immunology/Oncology in Lund in combinatorial chemistry and with scientists at ASTRA DRACO in Lund concerning synthesis of glycopeptides.

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Participants

• Umeä Universitet · UmeåCoordinatorSweden

Links

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