The role of protein loops and linkers in conformational dynamics and allostery
Proteins are dynamic entities that undergo a plethora of conformational changes that may
take place on a wide range of time scales. These changes can be as small as the rotation of …
take place on a wide range of time scales. These changes can be as small as the rotation of …
The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant …
PW Manley, L Barys, SW Cowan-Jacob - Leukemia research, 2020 - Elsevier
Asciminib is a potent, orally bioavailable, investigational drug that specifically and potently
inhibits the tyrosine kinase activity of native ABL1, together with that of the chimeric BCR …
inhibits the tyrosine kinase activity of native ABL1, together with that of the chimeric BCR …
Protein–ligand binding with the coarse-grained Martini model
The detailed understanding of the binding of small molecules to proteins is the key for the
development of novel drugs or to increase the acceptance of substrates by enzymes …
development of novel drugs or to increase the acceptance of substrates by enzymes …
Structure determination of high-energy states in a dynamic protein ensemble
JB Stiller, R Otten, D Häussinger, PS Rieder… - Nature, 2022 - nature.com
Macromolecular function frequently requires that proteins change conformation into high-
energy states,,–. However, methods for solving the structures of these functionally essential …
energy states,,–. However, methods for solving the structures of these functionally essential …
Src kinases as therapeutic targets for cancer
LC Kim, L Song, EB Haura - Nature reviews Clinical oncology, 2009 - nature.com
Src family kinases (SFKs) have a critical role in cell adhesion, invasion, proliferation,
survival, and angiogenesis during tumor development. SFKs comprise nine family members …
survival, and angiogenesis during tumor development. SFKs comprise nine family members …
The structural basis for control of eukaryotic protein kinases
JA Endicott, MEM Noble… - Annual review of …, 2012 - annualreviews.org
Eukaryotic protein kinases are key regulators of cell processes. Comparison of the structures
of protein kinase domains, both alone and in complexes, allows generalizations to be made …
of protein kinase domains, both alone and in complexes, allows generalizations to be made …
Activation pathway of Src kinase reveals intermediate states as targets for drug design
Unregulated activation of Src kinases leads to aberrant signalling, uncontrolled growth and
differentiation of cancerous cells. Reaching a complete mechanistic understanding of large …
differentiation of cancerous cells. Reaching a complete mechanistic understanding of large …
Allosteric activation of functionally asymmetric RAF kinase dimers
Although RAF kinases are critical for controlling cell growth, their mechanism of activation is
incompletely understood. Recently, dimerization was shown to be important for activation …
incompletely understood. Recently, dimerization was shown to be important for activation …
FYN: emerging biological roles and potential therapeutic targets in cancer
SF Peng, Y Fu - Journal of Translational Medicine, 2023 - Springer
Src family protein kinases (SFKs) play a key role in cell adhesion, invasion, proliferation,
survival, apoptosis, and angiogenesis during tumor development. In humans, SFKs consists …
survival, apoptosis, and angiogenesis during tumor development. In humans, SFKs consists …
[HTML][HTML] Regulation of the SRC family kinases by Csk
M Okada - International journal of biological sciences, 2012 - ncbi.nlm.nih.gov
The non-receptor tyrosine kinase Csk serves as an indispensable negative regulator of the
Src family tyrosine kinases (SFKs) by specifically phosphorylating the negative regulatory …
Src family tyrosine kinases (SFKs) by specifically phosphorylating the negative regulatory …