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Biological Relevance of RGD‐Integrin Subtype‐Specific Ligands in Cancer
Author(s) -
Sani Saidu,
Messe Mélissa,
Fuchs Quentin,
Pierrevelcin Marina,
Laquerriere Patrice,
EntzWerle Natacha,
Reita Damien,
EtienneSelloum Nelly,
Bruban Véronique,
Choulier Laurence,
Martin Sophie,
Dontenwill Monique
Publication year - 2021
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.202000626
Subject(s) - integrin , peptidomimetic , extracellular matrix , transmembrane protein , chemistry , cancer research , microbiology and biotechnology , computational biology , receptor , peptide , biology , biochemistry
Integrins are heterodimeric transmembrane proteins able to connect cells with the micro‐environment. They represent a family of receptors involved in almost all the hallmarks of cancer. Integrins recognizing the Arg‐Gly‐Asp (RGD) peptide in their natural extracellular matrix ligands have been particularly investigated as tumoral therapeutic targets. In the last 30 years, intense research has been dedicated to designing specific RGD‐like ligands able to discriminate selectively the different RGD‐recognizing integrins. Chemists′ efforts have led to the proposition of modified peptide or peptidomimetic libraries to be used for tumor targeting and/or tumor imaging. Here we review, from the biological point of view, the rationale underlying the need to clearly delineate each RGD‐integrin subtype by selective tools. We describe the complex roles of RGD‐integrins (mainly the most studied αvβ3 and α5β1 integrins) in tumors, the steps towards selective ligands and the current usefulness of such ligands. Although the impact of integrins in cancer is well acknowledged, the biological characteristics of each integrin subtype in a specific tumor are far from being completely resolved. Selective ligands might help us to reconsider integrins as therapeutic targets in specific clinical settings.