Kinase-targeted cancer therapies: progress, challenges and future directions

KS Bhullar, NO Lagarón, EM McGowan, I Parmar… - Molecular cancer, 2018 - Springer
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

Signaling pathways in inflammation and anti-inflammatory therapies

YT Yeung, F Aziz, A Guerrero-Castilla… - Current …, 2018 - ingentaconnect.com
During the past decade, an abundance of new evidence highlighted the importance of
inflammation in the development of chronic pathologies such as neurodegeneration, cancer …

Polo-like kinase 1 inhibitors in human cancer therapy: development and therapeutic potential

J Zhang, L Zhang, J Wang, L Ouyang… - Journal of medicinal …, 2022 - ACS Publications
Polo-like kinase 1 (PLK1) plays an important role in a variety of cellular functions, including
the regulation of mitosis, DNA replication, autophagy, and the epithelial–mesenchymal …

Signaling pathways in cancer: therapeutic targets, combinatorial treatments, and new developments

HYK Yip, A Papa - Cells, 2021 - mdpi.com
Molecular alterations in cancer genes and associated signaling pathways are used to inform
new treatments for precision medicine in cancer. Small molecule inhibitors and monoclonal …

Fibroblast growth factor receptors (FGFRs): structures and small molecule inhibitors

S Dai, Z Zhou, Z Chen, G Xu, Y Chen - Cells, 2019 - mdpi.com
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases
expressed on the cell membrane that play crucial roles in both developmental and adult …

Src protein-tyrosine kinase structure, mechanism, and small molecule inhibitors

R Roskoski Jr - Pharmacological research, 2015 - Elsevier
The physiological Src proto-oncogene is a protein-tyrosine kinase that plays key roles in cell
growth, division, migration, and survival signaling pathways. From the N-to C-terminus, Src …

Molecular recognition in chemical and biological systems

E Persch, O Dumele, F Diederich - … Chemie International Edition, 2015 - Wiley Online Library
Abstract Structure‐based ligand design in medicinal chemistry and crop protection relies on
the identification and quantification of weak noncovalent interactions and understanding the …

Comprehensive analysis of kinase inhibitor selectivity

MI Davis, JP Hunt, S Herrgard, P Ciceri… - Nature …, 2011 - nature.com
We tested the interaction of 72 kinase inhibitors with 442 kinases covering> 80% of the
human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more …

[HTML][HTML] Vascular endothelial growth factor receptor (VEGFR-2)/KDR inhibitors: medicinal chemistry perspective

SJ Modi, VM Kulkarni - Medicine in Drug Discovery, 2019 - Elsevier
New blood vessels formation from the existing vasculature is called angiogenesis. It is an
essential physiological process for the growth of cells, tissue repair, wound healing, and …

Atropisomerism in medicinal chemistry: challenges and opportunities

ST Toenjes, JL Gustafson - Future medicinal chemistry, 2018 - Future Science
Atropisomerism is a dynamic type of axial chirality that is ubiquitous in medicinal chemistry.
There are several examples of stable atropisomeric US FDA-approved drugs and …