Michael J Eck
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Explore the profile of Michael J Eck including associated specialties, affiliations and a list of published articles.
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119
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15053
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Recent Articles
11.
Park E, Rawson S, Schmoker A, Kim B, Oh S, Song K, et al.
Nat Commun
. 2023 Jul;
14(1):4580.
PMID: 37516774
RAF-family kinases are activated by recruitment to the plasma membrane by GTP-bound RAS, whereupon they initiate signaling through the MAP kinase cascade. Prior structural studies of KRAS with RAF have...
12.
Shui B, Beyett T, Chen Z, Li X, La Rocca G, Gazlay W, et al.
Mol Cell
. 2023 Jul;
83(14):2509-2523.e13.
PMID: 37402366
K-Ras frequently acquires gain-of-function mutations (K-Ras being the most common) that trigger significant transcriptomic and proteomic changes to drive tumorigenesis. Nevertheless, oncogenic K-Ras-induced dysregulation of post-transcriptional regulators such as microRNAs...
13.
Damghani T, Wittlinger F, Beyett T, Eck M, Laufer S, Heppner D
Methods Enzymol
. 2023 May;
685:171-198.
PMID: 37245901
Specificity for a desired enzyme target is an essential property of small-molecule inhibitors. Molecules targeting oncogenic driver mutations in the epidermal growth factor receptor (EGFR) kinase domain have had a...
14.
Tkacik E, Li K, Gonzalez-Del Pino G, Ha B, Vinals J, Park E, et al.
J Biol Chem
. 2023 Mar;
299(5):104634.
PMID: 36963492
Upon activation by RAS, RAF family kinases initiate signaling through the MAP kinase cascade to control cell growth, proliferation, and differentiation. Among RAF isoforms (ARAF, BRAF, and CRAF), oncogenic mutations...
15.
Heppner D, Wittlinger F, Beyett T, Shaurova T, Urul D, Buckley B, et al.
ACS Med Chem Lett
. 2022 Dec;
13(12):1856-1863.
PMID: 36518696
Lazertinib (YH25448) is a novel third-generation tyrosine kinase inhibitor (TKI) developed as a treatment for EGFR mutant non-small cell lung cancer. To better understand the nature of lazertinib inhibition, we...
16.
Amrhein J, Beyett T, Feng W, Kramer A, Weckesser J, Schaeffner I, et al.
J Med Chem
. 2022 Nov;
65(23):15679-15697.
PMID: 36384036
Activating mutations in the epidermal growth factor receptor (EGFR) are frequent oncogenic drivers of non-small-cell lung cancer (NSCLC). The most frequent alterations in EGFR are short in-frame deletions in exon...
17.
Bae H, Viennet T, Park E, Chu N, Salguero A, Eck M, et al.
Elife
. 2022 Aug;
11.
PMID: 35968932
Akt is a Ser/Thr protein kinase that plays a central role in metabolism and cancer. Regulation of Akt's activity involves an autoinhibitory intramolecular interaction between its pleckstrin homology (PH) domain...
18.
Hauseman Z, Fodor M, Dhembi A, Viscomi J, Egli D, Bleu M, et al.
Nature
. 2022 Jul;
609(7926):416-423.
PMID: 35830882
RAS-MAPK signalling is fundamental for cell proliferation and is altered in most human cancers. However, our mechanistic understanding of how RAS signals through RAF is still incomplete. Although studies revealed...
19.
Beyett T, To C, Heppner D, Rana J, Schmoker A, Jang J, et al.
Nat Commun
. 2022 May;
13(1):2530.
PMID: 35534503
Lung cancer is frequently caused by activating mutations in the epidermal growth factor receptor (EGFR). Allosteric EGFR inhibitors offer promise as the next generation of therapeutics, as they are unaffected...
20.
To C, Beyett T, Jang J, Feng W, Bahcall M, Haikala H, et al.
Nat Cancer
. 2022 Apr;
3(4):402-417.
PMID: 35422503
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although drug resistance eventually develops. Allosteric EGFR inhibitors, which...