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Michael A McDonough

Explore the profile of Michael A McDonough including associated specialties, affiliations and a list of published articles. Areas
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Articles 117
Citations 5255
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Recent Articles
11.
Brem J, Panduwawala T, Ulf Hansen J, Hewitt J, Liepins E, Donets P, et al.
Nat Chem . 2021 Dec; 14(1):15-24. PMID: 34903857
Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1...
12.
Shishodia S, Demetriades M, Zhang D, Tam N, Maheswaran P, Clunie-OConnor C, et al.
J Med Chem . 2021 Nov; 64(22):16609-16625. PMID: 34762429
FTO catalyzes the Fe(II) and 2-oxoglutarate (2OG)-dependent modification of nucleic acids, including the demethylation of -methyladenosine (mA) in mRNA. FTO is a proposed target for anti-cancer therapy. Using information from...
13.
Islam M, Thinnes C, Holt-Martyn J, Chowdhury R, McDonough M, Schofield C
ChemMedChem . 2021 Sep; 17(1):e202100398. PMID: 34581506
Studies on the inhibition of the human 2-oxoglutarate dependent oxygenase JMJD6, which is a cancer target, by 2-oxoglutarate mimics / competitors, including human drugs, drug candidates, and metabolites relevant to...
14.
Rabe P, Kamps J, Sutherlin K, Linyard J, Aller P, Pham C, et al.
Sci Adv . 2021 Aug; 7(34). PMID: 34417180
Isopenicillin synthase (IPNS) catalyzes the unique reaction of l-δ-(α-aminoadipoyl)-l-cysteinyl-d-valine (ACV) with dioxygen giving isopenicillin (IPN), the precursor of all natural penicillins and cephalosporins. X-ray free-electron laser studies including time-resolved crystallography...
15.
Wu Y, Li Z, McDonough M, Schofield C, Zhang X
J Med Chem . 2021 May; 64(11):7189-7209. PMID: 34029087
Factor inhibiting hypoxia-inducible factor (FIH) is a JmjC domain 2-oxogluarate and Fe(II)-dependent oxygenase that catalyzes hydroxylation of specific asparagines in the C-terminal transcriptional activation domain of hypoxia-inducible factor alpha (HIF-α)...
16.
Brasnett A, Pfeffer I, Brewitz L, Chowdhury R, Nakashima Y, Tumber A, et al.
Angew Chem Int Ed Engl . 2021 Apr; 60(26):14657-14663. PMID: 33887099
Aspartate/asparagine-β-hydroxylase (AspH) is a human 2-oxoglutarate (2OG) and Fe oxygenase that catalyses C3 hydroxylations of aspartate/asparagine residues of epidermal growth factor-like domains (EGFDs). Unusually, AspH employs two histidine residues to...
17.
Figg Jr W, McDonough M, Chowdhury R, Nakashima Y, Zhang Z, Holt-Martyn J, et al.
ChemMedChem . 2021 Apr; 16(13):2082-2088. PMID: 33792169
Human prolyl-hydroxylases (PHDs) are hypoxia-sensing 2-oxoglutarate (2OG) oxygenases, catalysis by which suppresses the transcription of hypoxia-inducible factor target genes. PHD inhibition enables the treatment of anaemia/ischaemia-related disease. The PHD inhibitor...
18.
Lucic A, Hinchliffe P, Malla T, Tooke C, Brem J, Calvopina K, et al.
Eur J Med Chem . 2021 Feb; 215:113257. PMID: 33618159
Penems have demonstrated potential as antibacterials and β-lactamase inhibitors; however, their clinical use has been limited, especially in comparison with the structurally related carbapenems. Faropenem is an orally active antibiotic...
19.
Davydova E, Shimazu T, Schuhmacher M, Jakobsson M, Willemen H, Liu T, et al.
Nat Commun . 2021 Feb; 12(1):891. PMID: 33563959
Post-translational methylation plays a crucial role in regulating and optimizing protein function. Protein histidine methylation, occurring as the two isomers 1- and 3-methylhistidine (1MH and 3MH), was first reported five...
20.
Brewitz L, Tumber A, Pfeffer I, McDonough M, Schofield C
Sci Rep . 2020 Dec; 10(1):22398. PMID: 33349651
No abstract available.