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Targeting gastrin-releasing peptide receptors for cancer treatment

Zhou, Jiehuaa; Chen, Jiana; Mokotoff, Michaelb; Ball, Edward D.a


Growth factor receptors play critical roles in cancer cell proliferation and progression. A number of such receptors have been targeted for cancer treatment by either a monoclonal antibody or a specifically designed small molecule to inhibit the receptor function. Bombesin/gastrin-releasing peptide receptors (BN/GRP-Rs) are expressed in a variety of cancer cells and have limited distribution in normal human tissue. Inhibition of BN/GRP-Rs has been shown to block small cell lung cancer growth in vitro. Early phase clinical trials targeting human GRP-R showed anti-cancer activity. This review will focus on the study of the distribution of BN/GRP-Rs in normal and malignant tissues, and various approaches to targeting BN-GRP-Rs for cancer diagnosis and treatment.

aDivision of Blood and Marrow Transplantation, Department of Medicine and Moores UCSD Cancer Center, University of California San Diego, La Jolla, CA, USA

bDepartment of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA, USA

Sponsorship: The research reported here was supported by a grant to E. D. B. from the University of California, Tobacco Related Disease Research Program. E. D. B. is a shareholder in Medarex, Inc. who has certain rights to the BsMol discussed in this review.

Correspondence to E. D. Ball, Blood and Marrow Transplantation Program and Division, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0960, USA

Tel: +1 858 657-7053; fax: +1 858 657-6837;


Received 15 July 2004 Accepted 21 July 2004

© 2004 Lippincott Williams & Wilkins, Inc.