Irreversible protein kinase inhibitors: balancing the benefits and risks

T Barf, A Kaptein - Journal of medicinal chemistry, 2012 - ACS Publications
In the relatively young but expanding field of irreversible kinase inhibitor drug discovery,
there are two main developments that are of central importance. First, the patients have …

Kinetic and catalytic mechanisms of protein kinases

JA Adams - Chemical reviews, 2001 - ACS Publications
The reversible phosphorylation of proteins ranks among the most important posttranslational
modifications that occur in the cell. In the last several decades, protein phosphorylation has …

Close similarity of epidermal growth factor receptor and v-erb-B oncogene protein sequences

J Downward, Y Yarden, E Mayes, G Scrace, N Totty… - Nature, 1984 - nature.com
Each of six peptides derived from the human epidermal growth factor (EGF) receptor very
closely matches a part of the deduced sequence of the v-erb-B transforming protein of avian …

Insect cell-expressed p180erbB3 possesses an impaired tyrosine kinase activity.

PM Guy, JV Platko, LC Cantley… - Proceedings of the …, 1994 - National Acad Sciences
Protein kinases share a number of highly conserved or invariant amino acid residues in their
catalytic domains, suggesting that these residues are necessary for kinase activity. In …

Autophosphorylation sites on the epidermal growth factor receptor

J Downward, P Parker, MD Waterfield - Nature, 1984 - nature.com
The epidermal growth factor (EGF) receptor is a tyrosine-specific protein kinase with
autophosphorylating activity1–4. A 300 amino acid-long region of the receptor's cytoplasmic …

Ganglioside-mediated modulation of cell growth. Specific effects of GM3 on tyrosine phosphorylation of the epidermal growth factor receptor.

EG Bremer, J Schlessinger, SI Hakomori - Journal of Biological Chemistry, 1986 - ASBMB
Glycosphingolipids added exogenously to 3T3 cells in culture were shown to inhibit cell
growth, alter the membrane affinity to platelet-derived growth factor binding, and reduce …

Monoclonal anti-epidermal growth factor receptor antibodies which are inhibitors of epidermal growth factor binding and antagonists of epidermal growth factor …

GN Gill, T Kawamoto, C Cochet, A Le, JD Sato… - Journal of Biological …, 1984 - ASBMB
Four mouse monoclonal antibodies specific for human epidermal growth factor (EGF)
receptors have been prepared using EGF receptor protein from human A431 epidermoid …

Protein kinase C phosphorylation of the EGF receptor at a threonine residue close to the cytoplasmic face of the plasma membrane

T Hunter, N Ling, JA Cooper - Nature, 1984 - nature.com
The receptor for epidermal growth factor (EGF) is a 170,000–180,000 molecular weight
single-chain glycoprotein of 1,186 amino acids1. Its sequence suggests that it has an …

Expression of epidermal growth factor receptors in human brain tumors

TA Libermann, N Razon, AD Bartal, Y Yarden… - Cancer research, 1984 - AACR
The expression of receptors for epidermal growth factor (EGF-R) was determined in 29
samples of brain tumors from 22 patients. Primary gliogenous tumors, of various degrees of …

Redox regulation of epidermal growth factor receptor signaling through cysteine oxidation

TH Truong, KS Carroll - Biochemistry, 2012 - ACS Publications
Epidermal growth factor receptor (EGFR) exemplifies the family of receptor tyrosine kinases
that mediate numerous cellular processes, including growth, proliferation, and …