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PI-88 and Related Heparan Sulfate Mimetics.
Chhabra, Mohit; Ferro, Vito.
Afiliação
  • Chhabra M; School of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, Australia.
  • Ferro V; Australian Infectious Diseases Research Centre, The University of Queensland, Brisbane, Australia.
Adv Exp Med Biol ; 1221: 473-491, 2020.
Article em En | MEDLINE | ID: mdl-32274723
The heparan sulfate mimetic PI-88 (muparfostat) is a complex mixture of sulfated oligosaccharides that was identified in the late 1990s as a potent inhibitor of heparanase. In preclinical animal models it was shown to block angiogenesis, metastasis and tumor growth, and subsequently became the first heparanase inhibitor to enter clinical trials for cancer. It progressed to Phase III trials but ultimately was not approved for use. Herein we summarize the preparation, physicochemical and biological properties of PI-88, and discuss preclinical/clinical and structure-activity relationship studies. In addition, we discuss the PI-88-inspired development of related HS mimetic heparanase inhibitors with improved properties, ultimately leading to the discovery of PG545 (pixatimod) which is currently in clinical trials.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oligossacarídeos / Heparitina Sulfato / Neoplasias / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oligossacarídeos / Heparitina Sulfato / Neoplasias / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article