Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei, A Abad-García… - Chemical …, 2024 - ACS Publications
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …

Proteolytic Cleavage Mechanisms, Function, and “Omic” Approaches for a Near-Ubiquitous Posttranslational Modification

T Klein, U Eckhard, A Dufour, N Solis… - Chemical …, 2018 - ACS Publications
Proteases enzymatically hydrolyze peptide bonds in substrate proteins, resulting in a
widespread, irreversible posttranslational modification of the protein's structure and …

Getting intimate with trypsin, the leading protease in proteomics

E Vandermarliere, M Mueller… - Mass spectrometry …, 2013 - Wiley Online Library
Nowadays, mass spectrometry‐based proteomics is carried out primarily in a bottom‐up
fashion, with peptides obtained after proteolytic digest of a whole proteome lysate as the …

The NLRP1 inflammasome in human skin and beyond

G Fenini, T Karakaya, P Hennig, M Di Filippo… - International journal of …, 2020 - mdpi.com
Inflammasomes represent a group of protein complexes that contribute to host defense
against pathogens and repair processes upon the induction of inflammation. However …

The ins and outs of Bacillus proteases: activities, functions and commercial significance

CR Harwood, Y Kikuchi - FEMS Microbiology Reviews, 2022 - academic.oup.com
Because the majority of bacterial species divide by binary fission, and do not have
distinguishable somatic and germline cells, they could be considered to be immortal …

Evolution of the ribosome at atomic resolution

AS Petrov, CR Bernier, C Hsiao… - Proceedings of the …, 2014 - National Acad Sciences
The origins and evolution of the ribosome, 3–4 billion years ago, remain imprinted in the
biochemistry of extant life and in the structure of the ribosome. Processes of ribosomal RNA …

Reconstructing ancient proteins to understand the causes of structure and function

GKA Hochberg, JW Thornton - Annual review of biophysics, 2017 - annualreviews.org
A central goal in biochemistry is to explain the causes of protein sequence, structure, and
function. Mainstream approaches seek to rationalize sequence and structure in terms of their …

The enzymes of β-lactam biosynthesis

RB Hamed, JR Gomez-Castellanos, L Henry… - Natural product …, 2013 - pubs.rsc.org
Covering: up to May 2012The β-lactam antibiotics and related β-lactamase inhibitors are
amongst the most important small molecules in clinical use. Most, but not all, β-lactams …

Synthetic catalysts inspired by hydrolytic enzymes

MD Nothling, Z Xiao, A Bhaskaran, MT Blyth… - ACS …, 2018 - ACS Publications
Enzymes, as nature's catalysts, speed up the very reactions that make life possible.
Hydrolytic enzymes are a particularly important enzyme class responsible for the catalytic …