FDA-approved small-molecule kinase inhibitors

P Wu, TE Nielsen, MH Clausen - Trends in pharmacological sciences, 2015 - cell.com
Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …

The two faces of Hippo: targeting the Hippo pathway for regenerative medicine and cancer treatment

R Johnson, G Halder - Nature reviews Drug discovery, 2014 - nature.com
The Hippo signalling pathway is an emerging growth control and tumour suppressor
pathway that regulates cell proliferation and stem cell functions. Defects in Hippo signalling …

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 …

Vemurafenib: the first drug approved for BRAF-mutant cancer

G Bollag, J Tsai, J Zhang, C Zhang, P Ibrahim… - Nature reviews Drug …, 2012 - nature.com
The identification of driver oncogenes has provided important targets for drugs that can
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …

Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?

Z Zhao, H Wu, L Wang, Y Liu, S Knapp, Q Liu… - ACS chemical …, 2014 - ACS Publications
The ATP site of kinases displays remarkable conformational flexibility when accommodating
chemically diverse small molecule inhibitors. The so-called activation segment, whose …

Allosteric small-molecule kinase inhibitors

P Wu, MH Clausen, TE Nielsen - Pharmacology & therapeutics, 2015 - Elsevier
Small-molecule kinase inhibitors are invaluable targeted therapeutics for the treatment of
various human diseases, especially cancers. While the majority of approved and developed …

[HTML][HTML] Tyrosine kinase inhibitors

RJ Thomson, M Moshirfar, Y Ronquillo - StatPearls [Internet], 2023 - ncbi.nlm.nih.gov
Tyrosine Kinase Inhibitors - StatPearls - NCBI Bookshelf US flag An official website of the
United States government Here's how you know NIH NLM Logo Access keys NCBI Homepage …

How many kinases are druggable? A review of our current understanding

B Anderson, P Rosston, HW Ong… - Biochemical …, 2023 - portlandpress.com
There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …

Kinases as novel therapeutic targets in asthma and chronic obstructive pulmonary disease

PJ Barnes, C Page - Pharmacological Reviews, 2016 - Elsevier
Multiple kinases play a critical role in orchestrating the chronic inflammation and structural
changes in the respiratory tract of patients with asthma and chronic obstructive pulmonary …

Structural insights into FGFR kinase isoform selectivity: diverse binding modes of AZD4547 and ponatinib in complex with FGFR1 and FGFR4

JA Tucker, T Klein, J Breed, AL Breeze, R Overman… - Structure, 2014 - cell.com
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases has been
implicated in a wide variety of cancers. Despite a high level of sequence homology in the …