Tumour vasculature targeting agents in hybrid/conjugate drugs.
Citation:Prokopiou EM, Ryder SA, Walsh JJ, Tumour vasculature targeting agents in hybrid/conjugate drugs., Angiogenesis, 16, 3, 2013, 503 - 524
Prokopiou_Ryder_Walsh_2013_Tumour_vasculature_targeting_agents_in_hybrid_conjugate_drugs.pdf (Published (author's copy) - Peer Reviewed) 973.6Kb
Tumour vasculature targeting has been a very active area of cancer drug discovery over the last decade. Growth of solid tumours beyond a certain point requires a sufficient blood supply in order for them to develop and metastasise. While novel anti-angiogenic and vascular disrupting agents represent an important contribution to the armoury of anti-cancer agents, they nevertheless usually require combination with standard cytotoxic therapy in order to demonstrate positive clinical outcomes. In line with this consensus, a new concept has arisen, namely the design of functional hybrids where at least one component of the design targets a tumour angiogenic/vasculature pathway. This review will outline examples of such hybrid/conjugate-based approaches. Emphasis will be placed on their preclinical evaluation with particular focus on the arginine-glycine-aspartic acid/asparagine-glycine-arginine (RGD/NGR) conjugates, heparin-related hybrids and antibody-drug conjugates. In conclusion, the benefits and shortcomings of hybrids under development will be discussed in the context of future directions and applications.
Type of material:Journal Article
Availability:Full text available
Keywords:Angiogenesis, Combination therapy, Conjugates, Hybrids, Tumour vasculature, Vascular disrupting agents