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 …

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 …

[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 …

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 …

Tyrosine kinases in autoimmune and inflammatory skin diseases

KP Szilveszter, T Németh, A Mócsai - Frontiers in immunology, 2019 - frontiersin.org
Tyrosine kinases relay signals from diverse leukocyte antigen receptors, innate immune
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 …

Molecular medicinal insights into scaffold hopping-based drug discovery success

A Acharya, M Yadav, M Nagpure, S Kumarsan… - Drug Discovery …, 2023 - Elsevier
In both academia and the pharmaceutical industry, innovative hypotheses, methodologies
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 …

[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 …

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 …