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Integrins as Therapeutic Targets: Successes and Cancers.


ABSTRACT: Integrins are transmembrane receptors that are central to the biology of many human pathologies. Classically mediating cell-extracellular matrix and cell-cell interaction, and with an emerging role as local activators of TGF?, they influence cancer, fibrosis, thrombosis and inflammation. Their ligand binding and some regulatory sites are extracellular and sensitive to pharmacological intervention, as proven by the clinical success of seven drugs targeting them. The six drugs on the market in 2016 generated revenues of some US$3.5 billion, mainly from inhibitors of ?4-series integrins. In this review we examine the current developments in integrin therapeutics, especially in cancer, and comment on the health economic implications of these developments.

SUBMITTER: Raab-Westphal S 

PROVIDER: S-EPMC5615325 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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Integrins as Therapeutic Targets: Successes and Cancers.

Raab-Westphal Sabine S   Marshall John F JF   Goodman Simon L SL  

Cancers 20170823 9


Integrins are transmembrane receptors that are central to the biology of many human pathologies. Classically mediating cell-extracellular matrix and cell-cell interaction, and with an emerging role as local activators of TGFβ, they influence cancer, fibrosis, thrombosis and inflammation. Their ligand binding and some regulatory sites are extracellular and sensitive to pharmacological intervention, as proven by the clinical success of seven drugs targeting them. The six drugs on the market in 201  ...[more]

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