The role of N-acyl groups in the inhibitory activity of LH-RH analogues |
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| Authors: | Imre Mezö János Seprödi Judit Érchegyi István Teplán Magdolna Kovacs Bela Flerkó |
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| Institution: | 1. 1st Institute of Biochemistry, Semmelweis University Medical School, Budapest, Hungary;2. Institute of Anatomy, University Medical School, Pécs, Hungary |
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| Abstract: | Inhibitory analogues of luteinizing hormone-releasing hormone (LH-RH) were prepared with formyl-D-Trp1, acetyl-D-Trp1, valeryl-D-Trp1, tartaryl-D-Trp1, diacetyl-tartaryl-D-Trp1, acetyl-Gly1, and acetyl-Sar1 successively replacing the position one in the analogue D-Trp1, D-p-Cl-Phe2, D-Trp3, D-Phe6, D-Ala10]-LH-RH. The formyl-D-Trp1 and acetyl-D-Trp1 analogues yielded 100% blockade of ovulation at the 10 μg dose; the others were less potent and inhibited ovulation at the 50 μg dose. The inhibitory potency seems to correlate with the polarity of the acyl group. |
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| Keywords: | LH-RH LH-RH inhibitors Inhibition of ovulation Solid phase peptide synthesis |
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