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Although the open conformation remains elusive, this novel information has pushed the structure\u2013function studies to an unprecedented level. Electrophysiology, mutagenesis, photolabeling, and in silico simulations, guided by novel structural information, shed new light on the molecular mechanisms of receptor functioning. The main goal of this review is to present the current knowledge of GABA\n                    <jats:sub>A<\/jats:sub>\n                    R functional and structural properties. The review begins with an outline of the functional and structural studies of GABA\n                    <jats:sub>A<\/jats:sub>\n                    R, accompanied by some methodological considerations, especially biophysical methods, enabling the reader to follow how major breakthroughs in characterizing GABA\n                    <jats:sub>A<\/jats:sub>\n                    R features have been achieved. The main section provides a comprehensive analysis of the functional significance of specific structural elements in GABA\n                    <jats:sub>A<\/jats:sub>\n                    Rs. We additionally summarize the current knowledge on the binding sites for major GABA\n                    <jats:sub>A<\/jats:sub>\n                    R modulators, referring to the molecular underpinnings of their action. The final chapter of the review moves beyond examining GABA\n                    <jats:sub>A<\/jats:sub>\n                    R as an isolated macromolecule and describes the interactions of the receptor with other proteins in a broader context of inhibitory plasticity. In the final section, we propose a general conclusion that agonist binding to the orthosteric binding sites appears to rely on local interactions, whereas conformational transitions of bound macromolecule (gating) and allosteric modulation seem to reflect more global phenomena involving vast portions of the macromolecule.\n                  <\/jats:p>","DOI":"10.1017\/s0033583524000179","type":"journal-article","created":{"date-parts":[[2025,1,14]],"date-time":"2025-01-14T01:15:02Z","timestamp":1736817302000},"source":"Crossref","is-referenced-by-count":20,"title":["Molecular mechanisms of the GABA type A receptor function"],"prefix":"10.1017","volume":"58","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0158-9959","authenticated-orcid":false,"given":"Micha\u0142 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