George Ösapay

New application of peptide cyclization on an oxime resin (the PCOR method): preparation of lanthionine peptides

Peptides containing an orthogonally protected lanthionine amino acid unit at the N-terminus, prepared on a Kaiser-oxime resin using Boc-chemistry and the BOP peptide coupling method, have been cyclized via peptide cyclization on an oxime resin.

Therapeutic applications of somatostatin analogues

The neuropeptide somatostatin is widely expressed both in the periphery and in the central nervous system (CNS) and has multiple functions: it regulates endocrine and exocrine secretion, it possesses antiproliferative properties and it acts as a neurotransmitter/neuromodulator. These diverse physiological effects are mediated by a family of G-protein-coupled cell surface receptors, the somatostatin receptors, named sst1 through sst5. Short synthetic somatostatin analogues (octreotide, lanreotide) that are in clinical use (e.g., for cancer therapy, gastrointestinal disorders) primarily interact with sst2. Somatostatin analogues with selective receptor binding can be useful in the treatment of gastrointestinal, cardiovascular, endocrine, immunological or CNS diseases such as epilepsy and Alzheimer’s disease. This paper reviews selected somatostatin related publications and patents issued between 1995 and 1998 for new drug candidates and their possible therapeutic applications.