de L Milton R C, King J A, Badminton M N, Tobler C J, Lindsey G G, Fridkin M, Millar R P
Biochem Biophys Res Commun. 1983 Mar 29;111(3):1082-8. doi: 10.1016/0006-291x(83)91410-9.
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.
对哺乳动物的[精氨酸8]促黄体激素释放激素、鸡的[谷氨酰胺8]促黄体激素释放激素和一种类似物[赖氨酸8]促黄体激素释放激素进行荧光滴定，结果显示组氨酸2的pK值分别为5.80、6.22和6.01，酪氨酸5的pK值分别为9.65、9.88和9.88。组氨酸2的滴定范围分别为1.72、2.03和1.71，而三种肽的酪氨酸5的滴定范围相当相似（约为1.7）。在哺乳动物系统中，鸡促黄体激素释放激素的生物活性和受体结合相对于哺乳动物促黄体激素释放激素为1%，而[赖氨酸8]促黄体激素释放激素的相对活性约为10%。相比之下，哺乳动物和鸡促黄体激素释放激素在刺激鸡垂体细胞释放促黄体激素方面具有同等效力。结果表明，与促黄体激素释放激素及其8位取代类似物的构象相关的受体存在差异。
