Baker M E
FEBS Lett. 1984 Sep 17;175(1):41-4. doi: 10.1016/0014-5793(84)80565-7.
We find that gossypol, a male anti-fertility compound, is a reversible competitive inhibitor of estrogen binding to rat alpha-fetoprotein (AFP). The Kd of gossypol for rat AFP is 1.75 microM, which is similar to gossypol's affinity for lactate dehydrogenase isozyme X, the putative site where gossypol exerts its anti-fertility effects. Reacting sodium cyanoborohydride with gossypol reduces its affinity for AFP, showing that intact aldehyde groups on gossypol are important for binding to rat AFP and indicating that gossypol is specifically inter-acting with a nucleophilic site on AFP that influences estrogen binding.
我们发现棉酚，一种男性抗生育化合物，是雌激素与大鼠甲胎蛋白（AFP）结合的可逆竞争性抑制剂。棉酚对大鼠AFP的解离常数（Kd）为1.75微摩尔，这与棉酚对乳酸脱氢酶同工酶X的亲和力相似，乳酸脱氢酶同工酶X被认为是棉酚发挥抗生育作用的位点。氰基硼氢化钠与棉酚反应会降低其对AFP的亲和力，这表明棉酚上完整的醛基对于与大鼠AFP结合很重要，并且表明棉酚与AFP上影响雌激素结合的亲核位点特异性相互作用。
