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RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences

“RGD” is frequently pictured as a ligand for αvβ3-integrin and useful for molecular targeting of angiogenesis—which is about as simplistic as the idea that laser beams are green or red and particularly useful for arming spaceships. There is, however, much more to RGD. In particular, targeting angiog...

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Autor principal: Notni, Johannes
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9866491/
https://www.ncbi.nlm.nih.gov/pubmed/36678553
http://dx.doi.org/10.3390/ph16010056
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author Notni, Johannes
author_facet Notni, Johannes
author_sort Notni, Johannes
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description “RGD” is frequently pictured as a ligand for αvβ3-integrin and useful for molecular targeting of angiogenesis—which is about as simplistic as the idea that laser beams are green or red and particularly useful for arming spaceships. There is, however, much more to RGD. In particular, targeting angiogenesis is likely not the most significant stronghold of RGD-comprising constructs. RGD is the one-letter code of a very short peptide sequence, arginine-lysine-aspartate, which is recognized by eight different integrins, namely, α(IIb)β3, α5β1, α8β1, and the five dimers that αv forms with β1, β3, β5, β6, and β8. These 8 RGD receptors form an own subset among the entire class of 24 known integrins, which furthermore comprises another three distinct groups (4 collagen receptors, 4 laminin receptors, and 8 leukocyte receptors). However, the 8 RGD-recognizing integrins are far from being alike. They do not even share the same tissue prevalences and functions, but are expressed on fundamentally different cell types and fulfill the most diverse biological tasks. For example, α(IIb)β3 is found on platelets and mediates thrombus formation, whereas αvβ6- and αvβ8-integrin are expressed on epithelial cells, activate TFG-β, and thus may promote cancer progression and invasion as well as fibrosis. Recent non-clinical experiments and clinical findings suggest that the highly specific expression of αvβ6-integrin by some carcinoma types, in combination with the availability of the corresponding small-molecule ligands, may open a multitude of new and promising avenues for improved cancer diagnosis and therapy, including, but not limited to, radiopharmaceutical approaches.
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spelling pubmed-98664912023-01-22 RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences Notni, Johannes Pharmaceuticals (Basel) Opinion “RGD” is frequently pictured as a ligand for αvβ3-integrin and useful for molecular targeting of angiogenesis—which is about as simplistic as the idea that laser beams are green or red and particularly useful for arming spaceships. There is, however, much more to RGD. In particular, targeting angiogenesis is likely not the most significant stronghold of RGD-comprising constructs. RGD is the one-letter code of a very short peptide sequence, arginine-lysine-aspartate, which is recognized by eight different integrins, namely, α(IIb)β3, α5β1, α8β1, and the five dimers that αv forms with β1, β3, β5, β6, and β8. These 8 RGD receptors form an own subset among the entire class of 24 known integrins, which furthermore comprises another three distinct groups (4 collagen receptors, 4 laminin receptors, and 8 leukocyte receptors). However, the 8 RGD-recognizing integrins are far from being alike. They do not even share the same tissue prevalences and functions, but are expressed on fundamentally different cell types and fulfill the most diverse biological tasks. For example, α(IIb)β3 is found on platelets and mediates thrombus formation, whereas αvβ6- and αvβ8-integrin are expressed on epithelial cells, activate TFG-β, and thus may promote cancer progression and invasion as well as fibrosis. Recent non-clinical experiments and clinical findings suggest that the highly specific expression of αvβ6-integrin by some carcinoma types, in combination with the availability of the corresponding small-molecule ligands, may open a multitude of new and promising avenues for improved cancer diagnosis and therapy, including, but not limited to, radiopharmaceutical approaches. MDPI 2022-12-30 /pmc/articles/PMC9866491/ /pubmed/36678553 http://dx.doi.org/10.3390/ph16010056 Text en © 2022 by the author. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Opinion
Notni, Johannes
RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title_full RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title_fullStr RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title_full_unstemmed RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title_short RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
title_sort rgd forever!—past, present, and future of a 3-letter-code in radiopharmacy and life sciences
topic Opinion
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9866491/
https://www.ncbi.nlm.nih.gov/pubmed/36678553
http://dx.doi.org/10.3390/ph16010056
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