Molecular bases of VEGFR-2-mediated physiological function and pathological role

X Wang, AM Bove, G Simone, B Ma - Frontiers in Cell and …, 2020 - frontiersin.org
The vascular endothelial growth factors (VEGFs) and their receptors (VEGFRs) play crucial
roles in vasculogenesis and angiogenesis. Angiogenesis is an important mechanism in …

CSF-1 receptor signaling in myeloid cells

ER Stanley, V Chitu - Cold Spring Harbor perspectives …, 2014 - cshperspectives.cshlp.org
The CSF-1 receptor (CSF-1R) is activated by the homodimeric growth factors colony-
stimulating factor-1 (CSF-1) and interleukin-34 (IL-34). It plays important roles in …

Structure-guided blockade of CSF1R kinase in tenosynovial giant-cell tumor

WD Tap, ZA Wainberg, SP Anthony… - … England Journal of …, 2015 - Mass Medical Soc
Background Expression of the colony-stimulating factor 1 (CSF1) gene is elevated in most
tenosynovial giant-cell tumors. This observation has led to the discovery and clinical …

CSF1R inhibitors are emerging immunotherapeutic drugs for cancer treatment

J Wen, S Wang, R Guo, D Liu - European Journal of Medicinal Chemistry, 2023 - Elsevier
Abstract ABSTRACT: Colony-Stimulating Factor-1 Receptor (CSF1R) is a receptor tyrosine
kinase that controls the differentiation and maintenance of most tissue-resident …

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

M McTigue, BW Murray, JH Chen… - Proceedings of the …, 2012 - National Acad Sciences
Analyses of compounds in clinical development have shown that ligand efficient-molecules
with privileged physical properties and low dose are less likely to fail in the various stages of …

Activating mutations in CSF1R and additional receptor tyrosine kinases in histiocytic neoplasms

BH Durham, E Lopez Rodrigo, J Picarsic… - Nature medicine, 2019 - nature.com
Histiocytoses are clonal hematopoietic disorders frequently driven by mutations mapping to
the BRAF and MEK1 and MEK2 kinases. Currently, however, the developmental origins of …

Structure and function of VEGF receptors

E Stuttfeld, K Ballmer‐Hofer - IUBMB life, 2009 - Wiley Online Library
Vascular endothelial growth factors (VEGFs) regulate blood and lymphatic vessel
development and homeostasis. VEGFs are predominantly produced by endothelial …

Platelet-derived growth factors and their receptors: structural and functional perspectives

PH Chen, X Chen, X He - Biochimica et Biophysica Acta (BBA)-Proteins …, 2013 - Elsevier
The four types of platelet-derived growth factors (PDGFs) and the two types of PDGF
receptors (PDGFRs, which belong to class III receptor tyrosine kinases) have important …

Activity‐based kinase profiling of approved tyrosine kinase inhibitors

D Kitagawa, K Yokota, M Gouda, Y Narumi… - Genes to …, 2013 - Wiley Online Library
The specificities of nine approved tyrosine kinase inhibitors (imatinib, dasatinib, nilotinib,
gefitinib, erlotinib, lapatinib, sorafenib, sunitinib, and pazopanib) were determined by activity …

What makes a kinase promiscuous for inhibitors?

SM Hanson, G Georghiou, MK Thakur, WT Miller… - Cell chemical …, 2019 - cell.com
ATP-competitive kinase inhibitors often bind several kinases due to the high conservation of
the ATP binding pocket. Through clustering analysis of a large kinome profiling dataset, we …