An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase
SW Deacon, A Beeser, JA Fukui, UEE Rennefahrt… - Chemistry & biology, 2008 - cell.com
Autoregulatory domains found within kinases may provide more unique targets for chemical
inhibitors than the conserved ATP-binding pocket targeted by most inhibitors. The kinase …
inhibitors than the conserved ATP-binding pocket targeted by most inhibitors. The kinase …
New approaches to molecular cancer therapeutics
I Collins, P Workman - Nature chemical biology, 2006 - nature.com
Cancer drug development is leading the way in exploiting molecular biological and genetic
information to develop'personalized'medicine. The new paradigm is to develop agents that …
information to develop'personalized'medicine. The new paradigm is to develop agents that …
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives
J Hu, D Zhang, K Tian, C Ren, H Li, C Lin… - European Journal of …, 2023 - Elsevier
Leucine-rich repeat kinase 2 (LRRK2) is a multifunctional protein that orchestrates a diverse
array of cellular processes, including vesicle transport, autophagy, lysosome degradation …
array of cellular processes, including vesicle transport, autophagy, lysosome degradation …
FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo
T Sato, X Yang, S Knapper, P White… - Blood, The Journal …, 2011 - ashpublications.org
We examined in vivo FLT3 inhibition in acute myeloid leukemia patients treated with
chemotherapy followed by the FLT3 inhibitor lestaurtinib, comparing newly diagnosed acute …
chemotherapy followed by the FLT3 inhibitor lestaurtinib, comparing newly diagnosed acute …
Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis
S Wyllie, M Thomas, S Patterson, S Crouch… - Nature, 2018 - nature.com
Visceral leishmaniasis causes considerable mortality and morbidity in many parts of the
world. There is an urgent need for the development of new, effective treatments for this …
world. There is an urgent need for the development of new, effective treatments for this …
Discovery of new quinazolin-4 (3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation
IH Eissa, AGA El-Helby, HA Mahdy, MM Khalifa… - Bioorganic …, 2020 - Elsevier
Sixteen novel quinazoline-based derivatives were designed and synthesized via
modification of the VEGFR-2 reported inhibitor 7 in order to increase the binding affinity of …
modification of the VEGFR-2 reported inhibitor 7 in order to increase the binding affinity of …
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
The human FGF receptors (FGFRs) play critical roles in various human cancers, and several
FGFR inhibitors are currently under clinical investigation. Resistance usually results from …
FGFR inhibitors are currently under clinical investigation. Resistance usually results from …
Precision medicine and driver mutations: computational methods, functional assays and conformational principles for interpreting cancer drivers
R Nussinov, H Jang, CJ Tsai… - PLoS computational …, 2019 - journals.plos.org
At the root of the so-called precision medicine or precision oncology, which is our focus
here, is the hypothesis that cancer treatment would be considerably better if therapies were …
here, is the hypothesis that cancer treatment would be considerably better if therapies were …
Design, synthesis, molecular modeling, in vivo studies and anticancer evaluation of quinazolin-4 (3H)-one derivatives as potential VEGFR-2 inhibitors and apoptosis …
HA Mahdy, MK Ibrahim, AM Metwaly, A Belal… - Bioorganic …, 2020 - Elsevier
Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer.
Accordingly, new quinazoline-based derivatives having the structural features of VEGFR-2 …
Accordingly, new quinazoline-based derivatives having the structural features of VEGFR-2 …
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases
Protein kinases play a pivotal role in cell signaling, and dysregulation of many kinases has
been linked to disease development. A large number of kinase inhibitors are therefore …
been linked to disease development. A large number of kinase inhibitors are therefore …