[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 …

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 …

The reactome pathway knowledgebase 2022

M Gillespie, B Jassal, R Stephan, M Milacic… - Nucleic acids …, 2022 - academic.oup.com
Abstract The Reactome Knowledgebase (https://reactome. org), an Elixir core resource,
provides manually curated molecular details across a broad range of physiological and …

Understudied proteins: opportunities and challenges for functional proteomics

G Kustatscher, T Collins, AC Gingras, T Guo… - Nature …, 2022 - nature.com
Most research aiming at understanding the molecular foundations of life and disease has
focused on a limited set of increasingly well-known proteins while the biological functions of …

G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

QSAR without borders

EN Muratov, J Bajorath, RP Sheridan… - Chemical Society …, 2020 - pubs.rsc.org
Prediction of chemical bioactivity and physical properties has been one of the most
important applications of statistical and more recently, machine learning and artificial …

The reactome pathway knowledgebase 2024

M Milacic, D Beavers, P Conley, C Gong… - Nucleic acids …, 2024 - academic.oup.com
Abstract The Reactome Knowledgebase (https://reactome. org), an Elixir and GCBR core
biological data resource, provides manually curated molecular details of a broad range of …

Artificial intelligence for drug discovery: Are we there yet?

C Hasselgren, TI Oprea - Annual Review of Pharmacology and …, 2024 - annualreviews.org
Drug discovery is adapting to novel technologies such as data science, informatics, and
artificial intelligence (AI) to accelerate effective treatment development while reducing costs …

The PROTACtable genome

M Schneider, CJ Radoux, A Hercules… - Nature reviews Drug …, 2021 - nature.com
Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer
new opportunities to circumvent some of the limitations associated with traditional small …

A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models

F Ren, A Aliper, J Chen, H Zhao, S Rao, C Kuppe… - Nature …, 2024 - nature.com
Idiopathic pulmonary fibrosis (IPF) is an aggressive interstitial lung disease with a high
mortality rate. Putative drug targets in IPF have failed to translate into effective therapies at …