Comparative structure-activity studies on mammalian [Arg8] LH-RH and chicken [Gln8] LH-RH by fluorimetric titration

de L Milton, R. C., King, J. A., Badminton, Michael Norman, Tobler, C. J., Lindsey, G. G., Fridkin, M. and Millar, R. P. 1983. Comparative structure-activity studies on mammalian [Arg8] LH-RH and chicken [Gln8] LH-RH by fluorimetric titration. Biochemical and Biophysical Research Communications 111 (3) , pp. 1082-1088. 10.1016/0006-291X(83)91410-9

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Abstract

Fluorimetric titrations of mammalian [Arg8] LH-RH, chicken [Gln8] LH-RH and an analogue [Lys8] LH-RH revealed pK values of 5.80, 6.22 and 6.01 for His2, and 9.65, 9.88 and 9.88 for Tyr5. The titration ranges for His2 were 1.72, 2.03 and 1.71 while the range for Tyr5 was rather similar (approximately 1.7) for all three peptides. Biological activity and receptor binding in the mammalian system for chicken LH-RH was 1% relative to mammalian LH-RH while [Lys8] LH-RH had a relative activity of approximately 10%. In contrast, mammalian and chicken LH-RH were equipotent in stimulating LH release from chicken pituitary cells. The results indicate differences in the receptors related to the conformations of LH-RH and position 8-substituted analogues.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Medicine
Subjects:	R Medicine > R Medicine (General)
Publisher:	Elsevier
ISSN:	0006-291X
Last Modified:	04 Jun 2017 04:20
URI:	https://orca.cardiff.ac.uk/id/eprint/37286

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