Young P C, Keen F K, Einhorn L H, Stanich B M, Ehrlich C E, Cleary R E
Am J Obstet Gynecol. 1980 Jun 1;137(3):284-92. doi: 10.1016/0002-9378(80)90911-4.
Human mammary tumor cytosol containing macromolecules which bound 3H-MPA (3H-medroxyprogesterone acetate or 1,2-3H-6 Alpha-methyl-17 alpha-acetoxy-pregn-4-ene-3,20-dione) and 3H-R5020 (6,7-3H-17,21-dimethyl-19-nor-pregna-4,9-diene-3,20-dione) similarly with high affinity (Ka approximately equal to 2 nM-1) and specificity. The progestin-binding components had sedimentation coefficients of about 4S and 7S in sucrose gradients and had approximately the same number of binding sites for Ma and R5020 as revealed by gradient centrifugation and saturation analysis. Among the steroids tested, these components had the highest affinities for progestins and were probably progesterone receptors of human breast cancer. A 4S component of human serum bound 3H-R5020 but not 3H-MPA. With 3H-MPA and 3H-estradiol used as the tracers, the concentrations of progesterone and estrogen receptors have been determined in 236 human breast cancers by saturation analysis. Our results on the receptor content and response of 31 of these tumors to endocrine therapy suggest that progesterone receptor may be a better marker of a hormonally responsive breast cancer.
人乳腺肿瘤胞质溶胶含有能与³H-MPA（³H-醋酸甲羟孕酮或1,2-³H-6α-甲基-17α-乙酰氧基-孕-4-烯-3,20-二酮）和³H-R5020（6,7-³H-17,21-二甲基-19-去甲-孕-4,9-二烯-3,20-二酮）以相似的高亲和力（Ka约等于2nM⁻¹）和特异性结合的大分子。在蔗糖梯度中，孕激素结合成分的沉降系数约为4S和7S，通过梯度离心和饱和分析显示，它们对³H-MPA和³H-R5020的结合位点数量大致相同。在所测试的类固醇中，这些成分对孕激素具有最高的亲和力，可能是人乳腺癌的孕激素受体。人血清的一种4S成分能结合³H-R5020，但不能结合³H-MPA。以³H-MPA和³H-雌二醇作为示踪剂，通过饱和分析测定了236例人乳腺癌中孕激素和雌激素受体的浓度。我们对其中31例肿瘤的受体含量以及对内分泌治疗反应的研究结果表明，孕激素受体可能是激素反应性乳腺癌更好的标志物。
