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 …
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
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 …
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 …
(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 …
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?
The ATP site of kinases displays remarkable conformational flexibility when accommodating
chemically diverse small molecule inhibitors. The so-called activation segment, whose …
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 …
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 …
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
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 …
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 …
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 …
implicated in a wide variety of cancers. Despite a high level of sequence homology in the …