Kinase inhibition in autoimmunity and inflammation
AA Zarrin, K Bao, P Lupardus, D Vucic - Nature Reviews Drug …, 2021 - nature.com
Despite recent advances in the treatment of autoimmune and inflammatory diseases, unmet
medical needs in some areas still exist. One of the main therapeutic approaches to alleviate …
medical needs in some areas still exist. One of the main therapeutic approaches to alleviate …
Syk inhibitors in clinical development for hematological malignancies
D Liu, A Mamorska-Dyga - Journal of hematology & oncology, 2017 - Springer
Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is
mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B …
mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B …
[HTML][HTML] CD36 facilitates fatty acid uptake by dynamic palmitoylation-regulated endocytosis
JW Hao, J Wang, H Guo, YY Zhao, HH Sun… - Nature …, 2020 - nature.com
Fatty acids (FAs) are essential nutrients, but how they are transported into cells remains
unclear. Here, we show that FAs trigger caveolae-dependent CD36 internalization, which in …
unclear. Here, we show that FAs trigger caveolae-dependent CD36 internalization, which in …
Large-scale assessment of binding free energy calculations in active drug discovery projects
CEM Schindler, H Baumann, A Blum… - Journal of Chemical …, 2020 - ACS Publications
Accurate ranking of compounds with regards to their binding affinity to a protein using
computational methods is of great interest to pharmaceutical research. Physics-based free …
computational methods is of great interest to pharmaceutical research. Physics-based free …
Tyrosine kinases in autoimmune and inflammatory skin diseases
Tyrosine kinases relay signals from diverse leukocyte antigen receptors, innate immune
receptors, and cytokine receptors, and therefore mediate the recruitment and activation of …
receptors, and cytokine receptors, and therefore mediate the recruitment and activation of …
Evolution of CLL treatment—from chemoimmunotherapy to targeted and individualized therapy
JA Burger, S O'Brien - Nature reviews Clinical oncology, 2018 - nature.com
During the past 5 years, a number of highly active novel agents, including kinase inhibitors
targeting BTK or PI3Kδ, an antagonist of the antiapoptotic protein BCL-2, and new anti …
targeting BTK or PI3Kδ, an antagonist of the antiapoptotic protein BCL-2, and new anti …
Molecular medicinal insights into scaffold hopping-based drug discovery success
In both academia and the pharmaceutical industry, innovative hypotheses, methodologies
and technologies that can shorten the drug research and development, leading to higher …
and technologies that can shorten the drug research and development, leading to higher …
An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia
J Sharman, M Hawkins, K Kolibaba… - Blood, The Journal …, 2015 - ashpublications.org
Small-molecule inhibitors of kinases involved in B-cell receptor signaling are an important
advance in managing lymphoid malignancies. Entospletinib (GS-9973) is an oral, selective …
advance in managing lymphoid malignancies. Entospletinib (GS-9973) is an oral, selective …
[HTML][HTML] Best practices for constructing, preparing, and evaluating protein-ligand binding affinity benchmarks [article v1. 0]
DF Hahn, CI Bayly, ML Boby… - Living journal of …, 2022 - ncbi.nlm.nih.gov
Free energy calculations are rapidly becoming indispensable in structure-enabled drug
discovery programs. As new methods, force fields, and implementations are developed …
discovery programs. As new methods, force fields, and implementations are developed …
Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL
PM Barr, GB Saylors, SE Spurgeon… - Blood, The Journal …, 2016 - ashpublications.org
Although agents targeting B-cell receptor signaling have provided practice-changing results
in relapsed chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL), they …
in relapsed chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL), they …