Abstract
Targeted drug delivery to specific group of cells offers an attractive strategy to minimize the undesirable side effects and achieve the therapeutic effect with a lower dose. Both linear and cyclic peptides have been explored as trafficking moiety due to ease of synthesis, structural simplicity, and low probability of undesirable immunogenicity. Peptides derived from sequence of cell surface proteins, such as intercellular adhesion moleculeโ1 (ICAMโ1), LHRH, Bombesin, and LFAโ1, have shown potent binding affinity to the target cell surface receptors. Moreover, peptides derived from ICAMโ1 receptor can be internalized by the leukemic Tโcells along with the conjugated moiety offering the promise to selectively treat cancers and autoimmune diseases. Systematic analyses have revealed that physicochemical properties of the drugโpeptide conjugates and their mechanism of receptorโmediated cellular internalization are important controlling factors for developing a successful targeting system. This review is focused on understanding the factors involved in the development of an effective drugโpeptide conjugate with an emphasis on the chemistry and biology of the conjugates. Reported results on several promising drugโpeptide conjugates have been critically evaluated. The approaches and results presented here will serve as a guide to systematically approach targeted delivery of cytotoxic drug molecules using peptides for treatment of several diseases. ยฉ 2010 Wiley Periodicals, Inc. Med Res Rev, 32, No. 3, 637โ658, 2012