Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001–2011)

J Wang, M Sánchez-Roselló, JL Aceña… - Chemical …, 2014 - ACS Publications
1.1. Brief Historical Overview As expected from the fluorine position on the periodic table of
elements, it possesses some extreme properties, in particular, ultimate electronegativity and …

Small-molecule modulation of protein homeostasis

GM Burslem, CM Crews - Chemical reviews, 2017 - ACS Publications
Control of protein levels by nucleic-acid-based technologies has proven to be a useful
research tool but lacks the advantages of small molecules with respect to cell permeability …

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

W Pao, J Chmielecki - Nature Reviews Cancer, 2010 - nature.com
Epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC) was
first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The …

Recent development of multi-target VEGFR-2 inhibitors for the cancer therapy

XJ Liu, HC Zhao, SJ Hou, HJ Zhang, L Cheng… - Bioorganic …, 2023 - Elsevier
Vascular epidermal growth factor receptor-2 (VEGFR-2), as an important tyrosine
transmembrane protein, plays an important role in regulating endothelial cell proliferation …

New therapies for hepatocellular carcinoma

MA Avila, C Berasain, B Sangro, J Prieto - Oncogene, 2006 - nature.com
Hepatocellular carcinoma (HCC), one of the most common cancers worldwide, is often
diagnosed at an advanced stage when most potentially curative therapies such as resection …

Structure and chemical inhibition of the RET tyrosine kinase domain

PP Knowles, J Murray-Rust, S Kjær, RP Scott… - Journal of biological …, 2006 - ASBMB
The RET proto-oncogene encodes a receptor tyrosine kinase for the glial cell line-derived
neurotrophic factor family of ligands. Loss-of-function mutations in RET are implicated in …

Lessons learned in the development of targeted therapy for malignant gliomas

AMP Omuro, S Faivre, E Raymond - Molecular cancer therapeutics, 2007 - AACR
The prognosis of patients with glioblastoma, anaplastic astrocytoma, and anaplastic
oligodendroglioma remains poor despite standard treatment with radiotherapy and …

The epidermal growth factor receptors and their family of ligands: their putative role in atherogenesis

AC Dreux, DJ Lamb, H Modjtahedi, GAA Ferns - Atherosclerosis, 2006 - Elsevier
The epidermal growth factor receptor is a member of type-I growth factor receptor family with
tyrosine kinase activity that is activated following the binding of multiple cognate ligands …

Cellular responses to EGFR inhibitors and their relevance to cancer therapy

PR Dutta, A Maity - Cancer letters, 2007 - Elsevier
EGFR is a trans-membrane receptor tyrosine kinase that belongs to the HER family of
receptors. The EGFR family plays an essential role in normal organ development by …