Expanding the number of 'druggable'targets: non‐enzymes and protein–protein interactions

LN Makley, JE Gestwicki - Chemical biology & drug design, 2013 - Wiley Online Library
Following sequencing and assembly of the human genome, the preferred methods for
identification of new drug targets have changed dramatically. Modern tactics such as …

Monoamine oxidases: the biochemistry of the proteins as targets in medicinal chemistry and drug discovery

RR Ramsay - Current topics in medicinal chemistry, 2012 - ingentaconnect.com
Monoamine oxidase (MAO, EC. 1.4. 3.4) has been a drug target for 60 years, with the
primary rationale of developing drugs to treat neuropsychiatric disorders. The biological …

Effects of metformin and other biguanides on oxidative phosphorylation in mitochondria

HR Bridges, AJY Jones, MN Pollak… - Biochemical Journal, 2014 - portlandpress.com
The biguanide metformin is widely prescribed for Type II diabetes and has anti-neoplastic
activity in laboratory models. Despite evidence that inhibition of mitochondrial respiratory …

Impact of an N-terminal polyhistidine tag on protein thermal stability

WT Booth, CR Schlachter, S Pote, N Ussin, NJ Mank… - ACS …, 2018 - ACS Publications
For years, the use of polyhistidine tags (His-tags) has been a staple in the isolation of
recombinant proteins in immobilized metal affinity chromatography experiments. Their …

Baeyer–Villiger monooxygenases: tunable oxidative biocatalysts

MJLJ Fürst, A Gran-Scheuch, FS Aalbers… - ACS …, 2019 - ACS Publications
Pollution, accidents, and misinformation have earned the pharmaceutical and chemical
industry a poor public reputation, despite their undisputable importance to society …

Directed evolution unlocks oxygen reactivity for a nicotine-degrading flavoenzyme

M Dulchavsky, R Mitra, K Wu, J Li, K Boer, X Liu… - Nature Chemical …, 2023 - nature.com
The flavoenzyme nicotine oxidoreductase (NicA2) is a promising injectable treatment to aid
in the cessation of smoking, a behavior responsible for one in ten deaths worldwide. NicA2 …

Discovery and characterization of a 5-hydroxymethylfurfural oxidase from Methylovorus sp. strain MP688

WP Dijkman, MW Fraaije - Applied and environmental …, 2014 - Am Soc Microbiol
In the search for useful and renewable chemical building blocks, 5-hydroxymethylfurfural
(HMF) has emerged as a very promising candidate, as it can be prepared from sugars. HMF …

CRISPR-suppressor scanning reveals a nonenzymatic role of LSD1 in AML

ME Vinyard, C Su, AP Siegenfeld, AL Waterbury… - Nature chemical …, 2019 - nature.com
Understanding the mechanism of small molecules is a critical challenge in chemical biology
and drug discovery. Medicinal chemistry is essential for elucidating drug mechanism …

Mutations in respiratory complex I promote antibiotic persistence through alterations in intracellular acidity and protein synthesis

B Van den Bergh, H Schramke, JE Michiels… - Nature …, 2022 - nature.com
Antibiotic persistence describes the presence of phenotypic variants within an isogenic
bacterial population that are transiently tolerant to antibiotic treatment. Perturbations of …

Characterization and crystal structure of a robust cyclohexanone monooxygenase

E Romero, JRG Castellanos, A Mattevi… - Angewandte Chemie …, 2016 - Wiley Online Library
Cyclohexanone monooxygenase (CHMO) is a promising biocatalyst for industrial reactions
owing to its broad substrate spectrum and excellent regio‐, chemo‐, and enantioselectivity …