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 …

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 …

Kinase inhibitors: the road ahead

FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

DeepDTA: deep drug–target binding affinity prediction

H Öztürk, A Özgür, E Ozkirimli - Bioinformatics, 2018 - academic.oup.com
Motivation The identification of novel drug–target (DT) interactions is a substantial part of the
drug discovery process. Most of the computational methods that have been proposed to …

Kinase-targeted cancer therapies: progress, challenges and future directions

KS Bhullar, NO Lagarón, EM McGowan, I Parmar… - Molecular cancer, 2018 - Springer
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

Fibroblast growth factor receptors (FGFRs): structures and small molecule inhibitors

S Dai, Z Zhou, Z Chen, G Xu, Y Chen - Cells, 2019 - mdpi.com
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases
expressed on the cell membrane that play crucial roles in both developmental and adult …

Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

P Wu, TE Nielsen, MH Clausen - Drug discovery today, 2016 - Elsevier
Highlights•A dramatic increase in the approval of small molecule kinase inhibitors
(SMKIs).•The molecular weight of most approved SMKIs is in the range of 400–600.•The …

Large-scale investigation of the reasons why potentially important genes are ignored

T Stoeger, M Gerlach, RI Morimoto… - PLoS …, 2018 - journals.plos.org
Biomedical research has been previously reported to primarily focus on a minority of all
known genes. Here, we demonstrate that these differences in attention can be explained, to …

Ten things you should know about protein kinases: IUPHAR R eview 14

D Fabbro, SW Cowan‐Jacob… - British journal of …, 2015 - Wiley Online Library
Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

T Anastassiadis, SW Deacon, K Devarajan, H Ma… - Nature …, 2011 - nature.com
Small-molecule protein kinase inhibitors are widely used to elucidate cellular signaling
pathways and are promising therapeutic agents. Owing to evolutionary conservation of the …