The quantitative study of the rates of association, dissociation, and translocation of a lipophilic signaling molecule, such as a steroid or thyroid hormone, with its specific receptor located within the cytoplasm or nucleus of a target cell. Kinetics describes the time-dependent changes in receptor binding affinity and the speed at which the activated hormone-receptor complex moves to the nucleus to modulate gene transcription. This dynamic process determines the magnitude and duration of the hormonal response.
Origin
This concept is foundational to molecular endocrinology and pharmacology, particularly concerning steroid and thyroid hormone action, which utilize intracellular receptors rather than cell-surface receptors. The term “Kinetics” applies the principles of chemical reaction rates to the biological interactions occurring inside the cell. Understanding these rates is crucial for predicting the latency and persistence of hormone action.
Mechanism
Upon entering the cell, the lipophilic hormone binds to its intracellular receptor, causing a conformational change that often releases heat shock proteins, which were previously masking the nuclear localization signal. This activated complex then translocates into the nucleus, where it binds to specific DNA sequences known as hormone response elements (HREs) in the promoter regions of target genes. The rate of this entire process, from binding to transcriptional modulation, defines the Intracellular Receptor Kinetics.
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