促性腺激素释放激素对促黄体生成素释放的刺激作用：一种配体-受体-效应器模型。
Gonadotropin-releasing hormone stimulation of luteinizing hormone release: A ligand-receptor-effector model.
作者信息
Blum J J, Conn P M
出版信息
Proc Natl Acad Sci U S A. 1982 Dec;79(23):7307-11. doi: 10.1073/pnas.79.23.7307.
Abstract
A divalent antibody conjugate of a pure antagonist of gonadotropin-releasing hormone (GnRH) behaved as an agonist--i.e., released luteinizing hormone (LH) from pituitary cultures. Release was measured over a wide range of conjugate concentrations; it rose to a maximum of 66% of the LH released by the optimal concentration of GnRH and declined to basal levels at very high concentrations. This behavior was modeled on the assumption that the antibody conjugate, A, can react with a receptor, R, to form a complex, A . R2. This dimer then can react with a quiescent effector, E (e.g., a closed Ca2+ ion channel), to form A . R2 . E, which contains activated effector and leads to cellular responses. The equilibrium equations governing the behavior of this model were derived, solved, and found to yield a good fit to the experimental data. Consideration of our data in this model system, and of other available data describing the behavior of ligands in other cells, suggests that the present model may be of wide applicability.
摘要
促性腺激素释放激素（GnRH）纯拮抗剂的二价抗体偶联物表现为激动剂——即从垂体培养物中释放促黄体生成素（LH）。在广泛的偶联物浓度范围内测量释放量；它上升至GnRH最佳浓度释放的LH的66%的最大值，并在非常高的浓度下降至基础水平。这种行为是基于这样的假设建模的，即抗体偶联物A可以与受体R反应形成复合物A·R2。然后这种二聚体可以与静止效应器E（例如封闭的Ca2+离子通道）反应形成A·R2·E，其包含活化的效应器并导致细胞反应。推导、求解了控制该模型行为的平衡方程，并发现其与实验数据拟合良好。在该模型系统中考虑我们的数据，以及描述其他细胞中配体行为的其他可用数据，表明本模型可能具有广泛的适用性。
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