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Synthesis and Biological Evaluation of Cyclobutane-Based ß3 Integrin Antagonists: A Novel Approach to Targeting Integrins for Cancer Therapy.
Sutherland, Mark; Gordon, Andrew; Al-Shammari, Fatemah O F O; Throup, Adam; Cilia La Corte, Amy; Philippou, Helen; Shnyder, Steven D; Patterson, Laurence H; Sheldrake, Helen M.
Afiliação
  • Sutherland M; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Gordon A; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Al-Shammari FOFO; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Throup A; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Cilia La Corte A; Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UK.
  • Philippou H; Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UK.
  • Shnyder SD; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Patterson LH; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
  • Sheldrake HM; Institute of Cancer Therapeutics, University of Bradford, Bradford BD7 1DP, UK.
Cancers (Basel) ; 15(16)2023 Aug 08.
Article em En | MEDLINE | ID: mdl-37627051
The Arg-Gly-Asp (RGD)-binding family of integrin receptors, and notably the ß3 subfamily, are key to multiple physiological processes involved in tissue development, cancer proliferation, and metastatic dissemination. While there is compelling preclinical evidence that both αvß3 and αIIbß3 are important anticancer targets, most integrin antagonists developed to target the ß3 integrins are highly selective for αvß3 or αIIbß3. We report the design, synthesis, and biological evaluation of a new structural class of ligand-mimetic ß3 integrin antagonist. These new antagonists combine a high activity against αvß3 with a moderate affinity for αIIbß3, providing the first evidence for a new approach to integrin targeting in cancer.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2023 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2023 Tipo de documento: Article