Integrin modulators: a patent review.
BACKGROUND
Integrins are heterodimeric cell surface receptors, which enable adhesion, proliferation, and migration of cells by recognizing binding motifs in extracellular matrix (ECM) proteins. As transmembrane linkers between the cytoskeleton and the ECM, they are able to recruit a huge variety of proteins and to influence signaling pathways bidirectionally, thereby regulating gene expression and cell survival. Hence, integrins play a key role in various physiological as well as pathological processes, which has turned them into an attractive target for pharmaceutical research.


METHODS
In this review, the latest therapeutic developments of drug candidates and recently patented integrin ligands are summarized.


CONCLUSIONS
Integrins have been proven to be valuable therapeutic targets in the treatment of several inflammatory and autoimmune diseases, where leukocyte adhesion processes are regulated by them. Furthermore, they play an important role in pathological angiogenesis and tumor metastasis, being a promising target for cancer therapy.
Institute for Advanced Study (IAS) and Center for Integrated Protein Science (CIPSM), Department Chemie, Technische Universität München , Lichtenbergstrasse 4, 85747 Garching , Germany kessler@tum.de.
Tobias G
TG
Kapp
Florian
F
Rechenmacher
Tariq R
TR
Sobahi
Horst
H
Kessler
D000818:Animals; D006801:Humans; D016023:Integrins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000378:metabolism; D009389:Neovascularization, Pathologic; D010330:Patents as Topic; D011485:Protein Binding; D013329:Structure-Activity Relationship
D016023:Integrins