Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update

R Roskoski Jr - Pharmacological research, 2021 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, the
protein kinase enzyme family has become one of the most important drug targets in the 21st …

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Cyclins and cyclin-dependent protein kinases (CDKs) are important proteins that are
required for the regulation and expression of the large number of components necessary for …

The ErbB/HER family of protein-tyrosine kinases and cancer

R Roskoski Jr - Pharmacological research, 2014 - Elsevier
The human epidermal growth factor receptor (EGFR) family consists of four members that
belong to the ErbB lineage of proteins (ErbB1–4). These receptors consist of a glycosylated …

Estrogen-Induced Activation of Erk-1 and Erk-2 Requires the G Protein-Coupled Receptor Homolog, GPR30, and Occurs via Trans-Activation of the Epidermal Growth …

EJ Filardo, JA Quinn, KI Bland… - Molecular …, 2000 - academic.oup.com
Estrogen rapidly activates the mitogen-activated protein kinases, Erk-1 and Erk-2, via an as
yet unknown mechanism. Here, evidence is provided that estrogen-induced Erk-1/-2 …

Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs)

R Roskoski Jr - Pharmacological Research, 2021 - Elsevier
Because dysregulation of protein kinases owing to mutations or overexpression plays
causal roles in human diseases, this family of enzymes has become one of the most …

Molecular markers for breast cancer: prediction on tumor behavior

BK Banin Hirata, JMM Oda… - Disease …, 2014 - Wiley Online Library
Breast cancer is one of the most common cancers with greater than 1,300,000 cases and
450,000 deaths each year worldwide. The development of breast cancer involves a …

Elevated insulin receptor content in human breast cancer.

V Papa, V Pezzino, A Costantino… - The Journal of …, 1990 - Am Soc Clin Investig
The growth of breast cancer cells is under the regulation of hormones, growth factors, and
their receptors. In the present study, we have employed a new, sensitive, and specific …

Epidermal growth factor receptor (EGFR) transactivation by estrogen via the G-protein-coupled receptor, GPR30: a novel signaling pathway with potential significance …

EJ Filardo - The Journal of steroid biochemistry and molecular …, 2002 - Elsevier
The biological and biochemical effects of estrogen have been ascribed to its known
receptors, which function as ligand-inducible transcription factors. However, estrogen also …

Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: a …

A Howell, JFR Robertson, P Abram… - Journal of Clinical …, 2004 - ascopubs.org
Purpose To evaluate the efficacy and tolerability of fulvestrant (Faslodex; AstraZeneca
Pharmaceuticals LP, Wilmington, DE), a new estrogen receptor (ER) antagonist that …