Also known as THR790MET, RS121434569
T790M, also known as Thr790Met, is a gatekeeper mutation of the epidermal growth factor receptor (EGFR). The mutation substitutes a threonine (T) with a methionine (M) at position 790 of exon 20, affecting the ATP binding pocket of the EGFR kinase domain. Threonine is a small polar amino acid; methionine is a larger nonpolar amino acid. Rather than directly blocking inhibitor binding to the active site, T790M increases the affinity for ATP so that the inhibitors are outcompeted; irreversible covalent inhibitors such as osimertinib can overcome this resistance.
T790M ，也稱為Thr790Met ，是一種發生在表皮生長因子受體（EGFR）基因上的看守突變（gatekeeper mutation）。這個突變發生在EGFR基因的第20個外顯子上、第790個位點的蘇胺酸（T）被甲硫胺酸（Ｍ）所取代，因此影響了EGFR激酶區的ATP結合囊袋。蘇胺酸是具極性的小型胺基酸；而甲硫胺酸則是非極性的較大胺基酸。T790M藉由增加ATP與EGFR上的活性位之間的親和力（而非直接阻礙抑制劑與活性位結合），使ATP比抑制劑更具有與活性位結合的優勢。然而，共價抑制劑（covalent inhibitors），例如，可以克服此一抗藥性。
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Discovered by embedding cosine similarity (sentence-transformers MiniLM, 384-dim).