[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

Mechanisms of assembly and remodelling of the extracellular matrix

A Naba - Nature Reviews Molecular Cell Biology, 2024 - nature.com
The extracellular matrix (ECM) is the complex meshwork of proteins and glycans that forms
the scaffold that surrounds and supports cells. It exerts key roles in all aspects of metazoan …

An atlas of substrate specificities for the human serine/threonine kinome

JL Johnson, TM Yaron, EM Huntsman, A Kerelsky… - Nature, 2023 - nature.com
Protein phosphorylation is one of the most widespread post-translational modifications in
biology,. With advances in mass-spectrometry-based phosphoproteomics, 90,000 sites of …

Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Kinase drug discovery 20 years after imatinib: progress and future directions

P Cohen, D Cross, PA Jänne - Nature reviews drug discovery, 2021 - nature.com
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - Signal transduction and …, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

The intrinsic substrate specificity of the human tyrosine kinome

TM Yaron-Barir, BA Joughin, EM Huntsman, A Kerelsky… - Nature, 2024 - nature.com
Phosphorylation of proteins on tyrosine (Tyr) residues evolved in metazoan organisms as a
mechanism of coordinating tissue growth. Multicellular eukaryotes typically have more than …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update

R Roskoski Jr - Pharmacological research, 2022 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21st century. There …

[HTML][HTML] Pan-cancer analysis of post-translational modifications reveals shared patterns of protein regulation

Y Geffen, S Anand, Y Akiyama, TM Yaron, Y Song… - Cell, 2023 - cell.com
Post-translational modifications (PTMs) play key roles in regulating cell signaling and
physiology in both normal and cancer cells. Advances in mass spectrometry enable high …

Dissecting the role of protein phosphorylation: a chemical biology toolbox

T Bilbrough, E Piemontese, O Seitz - Chemical Society Reviews, 2022 - pubs.rsc.org
Protein phosphorylation is a crucial regulator of protein and cellular function, yet, despite
identifying an enormous number of phosphorylation sites, the role of most is still unclear …