Ligand-based receptor tyrosine kinase partial agonists: New paradigm for cancer drug discovery?

DJ Riese - Expert opinion on drug discovery, 2011 - Taylor & Francis
Introduction: Receptor tyrosine kinases (RTKs) are validated targets for oncology drug
discovery and RTK antagonists are available to treat human malignancies. Nonetheless, the …

[PDF][PDF] ErbB receptor tyrosine kinase inhibitors as therapeutic agents

NG Anderson, T Ahmad - Front Biosci, 2002 - article.imrpress.com
Introduction 3. Structure and biological functions of ErbB receptors 4. Regulation of receptor
activity 4.1. ErbB Ligands 4.2. Receptor activation and signaling 4.3. Receptor …

ErbB family targeting.

JD Black, MG Brattain, SA Krishnamurthi… - Current Opinion in …, 2003 - europepmc.org
Drugs for specific molecular targets have generated a great deal of excitement for their
potential in cancer treatment, particularly with respect to our molecular understanding of …

Principles of receptor-based inhibition of erbB family receptor kinases: prospects for new therapies for human cancers.

DM O'Rourke, X Zhang, MI Greene - Proceedings of the Association …, 1997 - europepmc.org
The erbB family of receptor tyrosine kinases is composed of growth factor receptors that are
overexpressed or mutated in a large variety of human cancers. The study of erbB-mediated …

Site-directed irreversible inhibitors of the erbB family of receptor tyrosine kinases as novel chemotherapeutic agents for cancer

DW Fry - Anti-cancer drug design, 2000 - ingentaconnect.com
The erbB family of tyrosine kinases represents a versatile set of four plasma membrane
receptors that possesses enormous diversity in signaling capability. The rationale to target …

Effector mechanisms of therapeutic antibodies against ErbB receptors

M Peipp, M Dechant, T Valerius - Current opinion in immunology, 2008 - Elsevier
ErbB1 and ErbB2 constitute validated target antigens for tumor therapy—as documented by
the approval of antibodies and tyrosine kinase inhibitors (TKIs) against both antigens …

ERBB receptors and cancer: the complexity of targeted inhibitors

NE Hynes, HA Lane - Nature Reviews Cancer, 2005 - nature.com
ERBB receptor tyrosine kinases have important roles in human cancer. In particular, the
expression or activation of epidermal growth factor receptor and ERBB2 are altered in many …

Targeting ErbB receptor signaling: a pan-ErbB approach to cancer

CD Britten - Molecular cancer therapeutics, 2004 - AACR
The ErbB receptors are localized to the cell membrane where they are activated by ligand to
trigger a network of signaling pathways. In some cancer cells, dysregulation of ErbB …

The erbB family: targets for therapeutic development against cancer and therapeutic strategies using monoclonal antibodies and tyrosine kinase inhibitors

EK Rowinsky - Annu. Rev. Med., 2004 - annualreviews.org
The overexpression and aberrant function of members of the erbB family of receptors,
particularly erbB1 (also known as epidermal growth factor receptor), and its ligands in many …

Targeting ERBB receptors in cancer

NE Hynes - Targeted Interference with Signal Transduction Events, 2007 - Springer
Tyrosine kinases are a large and diverse family of proteins found only in metazoans. The
ERBB family, which encompasses subgroup I of the receptor tyrosine kinase (RTK) …