Michael J Eck
Overview
Explore the profile of Michael J Eck including associated specialties, affiliations and a list of published articles.
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119
Citations
15053
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Recent Articles
1.
Latorre-Muro P, Vitale T, Ravichandran M, Zhang K, Palozzi J, Bennett C, et al.
Nat Cell Biol
. 2025 Jan;
27(1):130-140.
PMID: 39753947
Outer mitochondrial membrane (OMM) proteins communicate with the cytosol and other organelles, including the endoplasmic reticulum. This communication is important in thermogenic adipocytes to increase the energy expenditure that controls...
2.
Wittlinger F, Chitnis S, Pham C, Damghani T, Patel K, Mollers M, et al.
J Med Chem
. 2024 Dec;
67(23):21438-21469.
PMID: 39626019
Binding multiple sites within proteins with bivalent compounds is a strategy for developing uniquely active agents. A new class of dual-site inhibitors has emerged targeting the epidermal growth factor receptor...
3.
Zhao H, Beyett T, Jiang J, Rana J, Schaeffner I, Santana J, et al.
Proc Natl Acad Sci U S A
. 2024 Oct;
121(45):e2417144121.
PMID: 39471218
Somatic mutations in the epidermal growth factor receptor (EGFR) are a major cause of non-small cell lung cancer. Among these structurally diverse alterations, exon 20 insertions represent a unique subset...
4.
Li Z, Jiang J, Ficarro S, Beyett T, To C, Tavares I, et al.
ACS Cent Sci
. 2024 Jul;
10(6):1156-1166.
PMID: 38947214
A systematic strategy to develop dual-warhead inhibitors is introduced to circumvent the limitations of conventional covalent inhibitors such as vulnerability to mutations of the corresponding nucleophilic residue. Currently, all FDA-approved...
5.
Beyett T, Rana J, Schaeffner I, Heppner D, Eck M
ChemMedChem
. 2024 Mar;
19(12):e202300343.
PMID: 38523074
A novel macrocyclic inhibitor of mutant EGFR (BI-4020) has shown promise in pre-clinical studies of T790M and C797S drug-resistant non-small cell lung cancer. To better understand the molecular basis for...
6.
Wittlinger F, Ogboo B, Shevchenko E, Damghani T, Pham C, Schaeffner I, et al.
Commun Chem
. 2024 Feb;
7(1):38.
PMID: 38378740
Bivalent molecules consisting of groups connected through bridging linkers often exhibit strong target binding and unique biological effects. However, developing bivalent inhibitors with the desired activity is challenging due to...
7.
Jeon H, Tkacik E, Eck M
Annu Rev Biochem
. 2024 Feb;
93(1):289-316.
PMID: 38316136
RAF family protein kinases are a key node in the RAS/RAF/MAP kinase pathway, the signaling cascade that controls cellular proliferation, differentiation, and survival in response to engagement of growth factor...
8.
Li Z, Lu W, Beyett T, Ficarro S, Jiang J, Tse J, et al.
J Med Chem
. 2024 Feb;
67(4):2837-2848.
PMID: 38300264
The pyrazolopyrimidine (PP) heterocycle is a versatile and widely deployed core scaffold for the development of kinase inhibitors. Typically, a 4-amino-substituted pyrazolopyrimidine binds in the ATP-binding pocket in a conformation...
9.
Kim J, Schaeffner I, Heppner D, To C, Janne P, Beyett T, et al.
Mol Pharmacol
. 2024 Jan;
105(2):97-103.
PMID: 38164587
Lung cancer is commonly caused by activating mutations in the epidermal growth factor receptor (EGFR). Allosteric kinase inhibitors are unaffected by common ATP-site resistance mutations and represent a promising therapeutic...
10.
Park E, Rawson S, Schmoker A, Kim B, Oh S, Song K, et al.
Nat Commun
. 2023 Sep;
14(1):5517.
PMID: 37679375
No abstract available.