Display Settings:

Format

Send to:

Choose Destination
See comment in PubMed Commons below
Curr Opin Investig Drugs. 2008 Dec;9(12):1264-76.

HER-2-directed, small-molecule antagonists.

Author information

  • 1Department of Medicine and Comprehensive Cancer Center, Box 0875, San Francisco, CA 94143-0875, USA.

Abstract

Inactivation of the human epidermal growth factor receptor-2 (HER-2) tyrosine kinase holds significant promise as a cancer treatment hypothesis, making it a high-value target for drug discovery. Screening and structure-based efforts have led to the development of several classes of ATP analog inhibitors of the HER-2 tyrosine kinase. These efforts have been further enhanced by detailed structural information regarding its sibling kinase, the EGF receptor, and structural properties that can be exploited to confer activity and even selectivity toward HER-2 kinase. Signaling and structural studies also suggest a critical involvement of the kinase inactive HER-3 in the regulation of HER-2, creating unique challenges in the efforts to inactivate the latter.

PMID:
19037833
[PubMed - indexed for MEDLINE]
PMCID:
PMC3031872
Free PMC Article

Images from this publication.See all images (6)Free text

Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for PubMed Central
    Loading ...
    Write to the Help Desk