title: Small Molecules for Active Targeting in Cancer.
abstract: For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?
authors.affiliation: Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.
authors.forename: Chin S
authors.initials: CS
authors.lastname: Kue
authors.affiliation: Department of Chemistry, Texas A & M University, Box 30012, College Station, TX, 77842.
authors.forename: Anyanee
authors.initials: A
authors.lastname: Kamkaew
authors.affiliation: Department of Chemistry, Texas A & M University, Box 30012, College Station, TX, 77842.
authors.forename: Kevin
authors.initials: K
authors.lastname: Burgess
authors.affiliation: Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.
authors.forename: Lik V
authors.initials: LV
authors.lastname: Kiew
authors.affiliation: Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.
authors.forename: Lip Y
authors.initials: LY
authors.lastname: Chung
authors.affiliation: Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.
authors.forename: Hong B
authors.initials: HB
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D008024:Ligands; D009369:Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands
keywords: active targeting; cancer imaging; cancer therapeutics; drug delivery; small-molecule ligands