Integrin Function and Signalling as Pharmacological Targets
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".
Deadline for manuscript submissions: closed (8 June 2023) | Viewed by 349
Special Issue Editor
Special Issue Information
Dear Colleagues,
Cells grow and survive more on a culture plate coated with an extracellular matrix protein. It has been, therefore, assumed that cells must have a signalling receptor for matrix proteins. In 1985, the receptor was caught in a gel as a heterodimer from a fibronectin affinity column, eluted by Arg-Gly-Asp (RGD) peptide. The vitronectin receptor was found right after the fibronectin receptor. In addition, several unanticipated proteins were found to have a similar structure to the matrix receptors, such as GPIIb/IIIa and LFA-1. This class of heterodimers with diverse functions on cell surfaces was termed integrin in 1987.
In 2022, the integrin family has been recognized as an appealing therapeutic target. Four integrins, αIIbβ3, α4β1, αLβ2, and α4β7, have been introduced into the clinical market, with anti-α4β7 monoclonal antibody (mAb) for inflammatory bowel diseases as one of the blockbusters. To date, all the above are non-RGD-recognizing and -circulating cell integrins. In contrast, currently, small molecules targeting RGD-recognizing integrins on fibroblasts or epithelial cells are in or close to clinical trials concerning pulmonary and hepatic fibrosis. Whether RGD-recognizing or non-RGD, constitutively expressed or induced, small molecule or mAb, there are many areas open for discussion. In addition, an essential task of integrins, signaling, may be considered from a pharmacological point of view. All of these and other ideas related to drug discovery must be integrated into this Special Issue to shed light on the future of drug discovery. The remaining 20 untargeted heterodimers must be reasonable therapeutic targets since integrin research has, to some extent, advanced and matured in the past 37 years to understand many of their functions and signaling pathways. What is the next disease to control and which will be the first non-circulating cell integrin to be a successful therapeutic target?
Prof. Dr. Yasuyuki Yokosaki
Guest Editor
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Keywords
- integrin
- extra cellular matrix
- RGD
- cell signal
- drug discovery
- monoclonal antibody
- pharmacophore
- fibrosis
- cancer
- macular degeneration
