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)

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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

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