Cunningham B C, Bass S, Fuh G, Wells J A
Department of Protein Engineering, Genentech, Inc., South San Francisco, CA 94080.
Science. 1990 Dec 21;250(4988):1709-12. doi: 10.1126/science.2270485.
Human growth hormone (hGH) elicits a diverse set of biological activities including lactation that derives from binding to the prolactin (PRL) receptor. The binding affinity of hGH for the extracellular binding domain of the hPRL receptor (hPRLbp) was increased about 8000-fold by addition of 50 micromolar ZnCl2. Zinc was not required for binding of hGH to the hGH binding protein (hGHbp) or for binding of hPRL to the hPRLbp. Other divalent metal ions (Ca2+, Mg2+, Cu2+, Mn2+, and Co2+) at physiological concentrations did not support such strong binding. Scatchard analysis indicated a stoichiometry of one Zn2+ per hGH.hPRLbp complex. Mutational analysis showed that a cluster of three residues (His18, His21, and Glu174) in hGH and His188 from the hPRLbp (conserved in all PRL receptors but not GH receptors) are probable Zn2+ ligands. This polypeptide hormone.receptor "zinc sandwich" provides a molecular mechanism to explain why nonprimate GHs are not lactogenic and offers a molecular link between zinc deficiency and its association with altered functions of hGH.
人生长激素(hGH)引发多种生物学活性,包括因与催乳素(PRL)受体结合而产生的泌乳作用。通过添加50微摩尔的ZnCl₂,hGH对人PRL受体(hPRLbp)细胞外结合域的结合亲和力提高了约8000倍。Zn对于hGH与人GH结合蛋白(hGHbp)的结合或hPRL与hPRLbp的结合并非必需。生理浓度下的其他二价金属离子(Ca²⁺、Mg²⁺、Cu²⁺、Mn²⁺和Co²⁺)不支持这种强结合。Scatchard分析表明,每个hGH·hPRLbp复合物的化学计量为一个Zn²⁺。突变分析表明,hGH中的三个残基簇(His18、His21和Glu174)以及hPRLbp中的His188(在所有PRL受体中保守,但在GH受体中不保守)可能是Zn²⁺配体。这种多肽激素-受体“锌夹心”提供了一种分子机制,用以解释为何非灵长类动物的GH不具有泌乳作用,并为锌缺乏及其与hGH功能改变的关联提供了分子联系。