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Ref Type

Journal Article

PMID

(30341394)

Authors

Caeser R, Collord G, Yao WQ, Chen Z, Vassiliou GS, Beer PA, Du MQ, Scott MA, Follows GA, Hodson DJ

Title

Targeting MEK in vemurafenib-resistant hairy cell leukemia.

Journal	Vol	Issue	Date	Pages	Journal Short Title
Leukemia			2018 Oct 19	541-545	Leukemia

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Gene	Variant	Impact	Protein Effect	Variant Description	Associated with drug Resistance
MAP2K1	F53C	missense	gain of function	MAP2K1 F53C lies within the negative regulatory region of the Map2k1 protein (PMID: 24241536). F53C confers a gain of function to Map2k1 as demonstrated by increased Erk1/2 phosphorylation (PMID: 30341394) and transformation activity in cultured cells and increased proliferation in a competition assay (PMID: 36442478), and is associated with resistance to BRAF inhibitors (PMID: 30341394, PMID: 36442478).	Y
MAP2K1	K57T	missense	gain of function	MAP2K1 K57T lies within the negative regulatory region of the Map2k1 protein (PMID: 24241536). K57T confers a gain of function to Map2k1 as demonstrated by increased Erk1/2 phosphorylation (PMID: 30341394, PMID: 32641410) and transformation activity in cultured cells and increased proliferation in a competition assay (PMID: 36442478), and occurs as a secondary drug resistance mutation in the context of BRAF inhibitors (PMID: 26644315, PMID: 28819429, PMID: 30341394).	Y

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
BRAF V600E MAP2K1 K57T	hairy cell leukemia	predicted - resistant	Vemurafenib	Case Reports/Case Series	Actionable	In a clinical case study, a single patient with hairy cell leukemia harboring BRAF V600E, who relapsed after a 38 week remission in response to Zelboraf (vemurafenib) treatment, was found to have acquired multiple clones with Mek/Erk activating mutations, of which the MAP2K1 K57T clone became dominant (PMID: 30341394).	30341394
BRAF V600E MAP2K1 K57T	refractory hairy cell leukemia	predicted - sensitive	Cobimetinib + Vemurafenib	Case Reports/Case Series	Actionable	In a clinical case study, a patient with hairy cell leukemia harboring BRAF V600E who relapsed after initial response to Zelboraf (vemurafenib) and was found to have acquired multiple clones with Mek/Erk activating mutations, including MAP2K1 K57T, demonstrated a sustained response greater than 12 months to combined Zelboraf (vemurafenib) and Cotellic (cobimetinib) treatment (PMID: 30341394).	30341394
MAP2K1 F53C	lymphoma	predicted - resistant	Vemurafenib	Preclinical - Cell culture	Actionable	In a preclinical study, expression of MAP2K1 F53C in a lymphoma cell line conferred resistance to inhibition of Erk phosphorylation by Zelboraf (vemurafenib) in culture (PMID: 30341394).	30341394

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