Click chemistry for drug development and diverse chemical–biology applications

P Thirumurugan, D Matosiuk, K Jozwiak - Chemical reviews, 2013 - ACS Publications
Chemistry, traditionally being the science of synthesis and structural manipulations of
molecules, has gradually undertaken the more challenging task of biology-oriented …

Stem cell factor receptor/c-Kit: from basic science to clinical implications

J Lennartsson, L Rönnstrand - Physiological reviews, 2012 - journals.physiology.org
Stem cell factor (SCF) is a dimeric molecule that exerts its biological functions by binding to
and activating the receptor tyrosine kinase c-Kit. Activation of c-Kit leads to its …

The human kinome and kinase inhibition

KC Duong‐Ly, JR Peterson - Current protocols in …, 2013 - Wiley Online Library
Protein and lipid kinases play key regulatory roles in a number of biological processes.
Unsurprisingly, activating mutations in kinases have been linked to a number of disorders …

[HTML][HTML] Cyclin-dependent kinase inhibitors as marketed anticancer drugs: where are we now? A short survey

G Mariaule, P Belmont - Molecules, 2014 - mdpi.com
In the early 2000s, the anticancer drug imatinib (Glivec®) appeared on the market, exhibiting
a new mode of action by selective kinase inhibition. Consequently, kinases became a …

Toxic essential oils. Part II: Chemical, toxicological, pharmacological and microbiological profiles of Artemisia annua L. volatiles

NS Radulović, PJ Randjelović, NM Stojanović… - Food and chemical …, 2013 - Elsevier
Botanical drugs based on Artemisia annua L.(Asteraceae) are important in the treatment of
malaria. Alongside with artemisinin, this aromatic species produces high and variable …

The different flexibility of c-Src and c-Abl kinases regulates the accessibility of a druggable inactive conformation

S Lovera, L Sutto, R Boubeva, L Scapozza… - Journal of the …, 2012 - ACS Publications
c-Src and c-Abl are two closely related protein kinases that constitute important anticancer
targets. Despite their high sequence identity, they show different sensitivities to the …

Selectivity and ranking of tight-binding JAK-STAT inhibitors using Markovian milestoning with Voronoi tessellations

AA Ojha, A Srivastava, LW Votapka… - Journal of Chemical …, 2023 - ACS Publications
Janus kinases (JAK), a group of proteins in the nonreceptor tyrosine kinase (NRTKs) family,
play a crucial role in growth, survival, and angiogenesis. They are activated by cytokines …

Design, synthesis and molecular docking of novel pyrazolo [1, 5-a][1, 3, 5] triazine derivatives as CDK2 inhibitors

KH Oudah, MAA Najm, N Samir, RAT Serya… - Bioorganic …, 2019 - Elsevier
Abstract Cyclin Dependent Kinases CDKs unpredictable activity has been accounted for a
wide assortment of human malignancies, so it might be conceivable to design …

The design and discovery of water soluble 4-substituted-2, 6-dimethylfuro [2, 3-d] pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule …

X Zhang, S Raghavan, M Ihnat, JE Thorpe… - Bioorganic & medicinal …, 2014 - Elsevier
The design, synthesis and biological evaluations of fourteen 4-substituted 2, 6-dimethylfuro
[2, 3-d] pyrimidines are reported. Four compounds (11–13, 15) inhibit vascular endothelial …

Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling

L Zhang, IP Holmes, F Hochgräfe… - Journal of proteome …, 2013 - ACS Publications
Kinase enrichment utilizing broad-spectrum kinase inhibitors enables the identification of
large proportions of the expressed kinome by mass spectrometry. However, the existing …