Emerging therapeutic opportunities for integrin inhibitors

RJ Slack, SJF Macdonald, JA Roper… - Nature Reviews Drug …, 2022 - nature.com
Integrins are cell adhesion and signalling proteins crucial to a wide range of biological
functions. Effective marketed treatments have successfully targeted integrins αIIbβ3 …

Integrin signaling in cancer: bidirectional mechanisms and therapeutic opportunities

S Li, C Sampson, C Liu, H Piao, HX Liu - Cell Communication and …, 2023 - Springer
Integrins are transmembrane receptors that possess distinct ligand-binding specificities in
the extracellular domain and signaling properties in the cytoplasmic domain. While most …

An αv‐RGD integrin inhibitor toolbox: drug discovery insight, challenges and opportunities

RJD Hatley, SJF Macdonald, RJ Slack… - Angewandte Chemie …, 2018 - Wiley Online Library
There is a requirement for efficacious and safe medicines to treat diseases with high unmet
need. The resurgence in αv‐RGD integrin inhibitor drug discovery is poised to contribute to …

Cancer stem cells in prostate cancer radioresistance

T Tsao, J Beretov, J Ni, X Bai, J Bucci, P Graham, Y Li - Cancer letters, 2019 - Elsevier
Cancer stem cells (CSCs) in prostate cancer (CaP) are regarded as major contributors to
radioresistance due to complex mechanisms including enhanced DNA repair, increased …

New strategies using antibody combinations to increase cancer treatment effectiveness

I Corraliza-Gorjón, B Somovilla-Crespo… - Frontiers in …, 2017 - frontiersin.org
Antibodies have proven their high value in antitumor therapy over the last two decades.
They are currently being used as the first-choice to treat some of the most frequent …

[HTML][HTML] Targeting the “sweet spot” in septic shock–A perspective on the endothelial glycocalyx regulating proteins Heparanase-1 and-2

T Pape, AM Hunkemöller, P Kümpers, H Haller… - Matrix biology plus, 2021 - Elsevier
Sepsis is a life-threatening syndrome caused by a pathological host response to an infection
that eventually, if uncontrolled, leads to septic shock and ultimately, death. In sepsis, a …

αvβ3 and α5β1 integrin-specific ligands: From tumor angiogenesis inhibitors to vascularization promoters in regenerative medicine?

LA Rocha, DA Learmonth, RA Sousa… - Biotechnology advances, 2018 - Elsevier
Integrins are cell adhesion receptors predominantly important during normal and tumor
angiogenesis. A sequence present on several extracellular matrix proteins composed of Arg …

Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists: miniperspective

HM Sheldrake, LH Patterson - Journal of medicinal chemistry, 2014 - ACS Publications
The integrins are a family of 24 heterodimeric transmembrane cell surface receptors.
Involvement in cell attachment to the extracellular matrix, motility, and proliferation identifies …

[HTML][HTML] A randomized, double-blind, multicenter, phase 2 study of a human monoclonal antibody to human αν integrins (intetumumab) in combination with docetaxel …

A Heidenreich, SK Rawal, K Szkarlat, N Bogdanova… - Annals of oncology, 2013 - Elsevier
Background Intetumumab is a fully human mAb with antiangiogenic, antitumor properties
which has shown potential therapeutic effect in castration-resistant prostate cancer (CRPC) …

RGD-binding integrins in prostate cancer: expression patterns and therapeutic prospects against bone metastasis

M Sutherland, A Gordon, SD Shnyder, LH Patterson… - Cancers, 2012 - mdpi.com
Prostate cancer is the third leading cause of male cancer deaths in the developed world.
The current lack of highly specific detection methods and efficient therapeutic agents for …