Synthesis and biological activity of N-terminal lipidated and/or fluorescently labeled conjugates of astressin as corticotropin releasing factor antagonists

Rijkers, D.T.S., den Hartog, J.A.J. and Liskamp, R.M.J. (2004) Synthesis and biological activity of N-terminal lipidated and/or fluorescently labeled conjugates of astressin as corticotropin releasing factor antagonists. Bioorganic and Medicinal Chemistry, 12(19), pp. 5099-5106. (doi: 10.1016/j.bmc.2004.07.035)

Abstract

This report describes the synthesis of eight N-terminally modified astressin analogs and their biochemical evaluation as corticotropin releasing factor (CRF) antagonists. The lipidated astressin derivatives were tested on rat CRF receptor type 1 and 2α and were found to be active as CRF antagonists (rCRFR1: pA₂ = 7.5–8.3; rCRFR2α: pA₂ = 7.5–9.0) with nearly equal activities as compared to unmodified astressin (rCRFR1: pA₂ = 8.3 ± 0.09; rCRFR2α: pA₂ = 8.7 ± 0.08).

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Liskamp, Professor Robert
• Authors: Rijkers, D.T.S., den Hartog, J.A.J., and Liskamp, R.M.J.
• College/School: College of Science and Engineering > School of Chemistry
• Journal Name: Bioorganic and Medicinal Chemistry
• ISSN: 0968-0896
• ISSN (Online): 1464-3391