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Demetrios H Kostomiris

Explore the profile of Demetrios H Kostomiris including associated specialties, affiliations and a list of published articles. Areas
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Citations 58
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Recent Articles
1.
McCoull W, Thomson C, Braybrooke E, Chan C, Colclough N, Cortes Gonzalez M, et al.
J Med Chem . 2025 Jan; 68(3):3700-3748. PMID: 39869768
Despite recent advances in the inhibition of EGFR (epidermal growth factor receptor), there remains a clinical need for new EGFR Exon20 insertion (Ex20Ins) inhibitors that spare EGFR WT. Herein, we...
2.
Thomson C, Braybrooke E, Colclough N, Davies N, Floch N, Greenwood R, et al.
J Med Chem . 2024 Sep; PMID: 39340451
Herein, we report the optimization of a series of epidermal growth factor receptor (EGFR) Exon20 insertion (Ex20Ins) inhibitors using structure-based drug design (SBDD), leading to the discovery of compound ,...
3.
Edwardes L, Caswell S, Giurrandino M, Zhai X, Gohlke A, Kostomiris D, et al.
Biochemistry . 2022 Sep; 61(18):1974-1987. PMID: 36070615
Human lysine methyltransferase 2D (hKMT2D) is an epigenetic writer catalyzing the methylation of histone 3 lysine 4. hKMT2D by itself has little catalytic activity and reaches full activation as part...
4.
Mellott D, Tseng C, Drelich A, Fajtova P, Chenna B, Kostomiris D, et al.
ACS Chem Biol . 2021 Mar; 16(4):642-650. PMID: 33787221
Host-cell cysteine proteases play an essential role in the processing of the viral spike protein of SARS coronaviruses. K777, an irreversible, covalent inactivator of cysteine proteases that has recently completed...
5.
Mellott D, Tseng C, Drelich A, Fajtova P, Chenna B, Kostomiris D, et al.
bioRxiv . 2020 Nov; PMID: 33140046
K777 is a di-peptide analog that contains an electrophilic vinyl-sulfone moiety and is a potent, covalent inactivator of cathepsins. Vero E6, HeLa/ACE2, Caco-2, A549/ACE2, and Calu-3, cells were exposed to...