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 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.
%0 Journal Article
%1 noKey
%A Prokopiou, E.M.
%A Ryder, S.A.
%A Walsh, J.J.
%D 2013
%I Springer Netherlands
%J Angiogenesis
%K Angiogenesis Combination Conjugates Hybrids Tumour Vascular agents disrupting myown therapy vasculature
%N 3
%P 503-524
%R 10.1007/s10456-013-9347-8
%T Tumour vasculature targeting agents in hybrid/conjugate drugs
%U http://dx.doi.org/10.1007/s10456-013-9347-8
%V 16
%X 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 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.
@article{noKey,
abstract = {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 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.},
added-at = {2013-07-31T21:54:28.000+0200},
author = {Prokopiou, E.M. and Ryder, S.A. and Walsh, J.J.},
biburl = {https://www.bibsonomy.org/bibtex/2c0854fca60dcfbadd2dae42825264d33/sryder},
doi = {10.1007/s10456-013-9347-8},
interhash = {0febe750780aa1bbf91d4b874a9745b3},
intrahash = {c0854fca60dcfbadd2dae42825264d33},
issn = {0969-6970},
journal = {Angiogenesis},
keywords = {Angiogenesis Combination Conjugates Hybrids Tumour Vascular agents disrupting myown therapy vasculature},
language = {English},
number = 3,
pages = {503-524},
publisher = {Springer Netherlands},
timestamp = {2013-07-31T21:54:28.000+0200},
title = {Tumour vasculature targeting agents in hybrid/conjugate drugs},
url = {http://dx.doi.org/10.1007/s10456-013-9347-8},
volume = 16,
year = 2013
}