Anti-angiogenic mechanism of IPS-05002, a novel antagonist against integrin a5β1, determined by ProteoChip-based antibody array

Kim, Mina; Kang, In‐Cheol

doi:10.1007/s13206-016-0303-8

Cited by 1 publication

(2 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…More recently, another non-RGD-mimetic inhibitor of α 5 β 1 was reported by Kang and Kim . Termed IPS-05002, compound 25 was identified by a screen of a phytochemical compound library using a ProteoChip-based protein–protein interaction assay for α 5 β 1 antagonists. This compound showed micromolar inhibition of α 5 β 1 in a cell proliferation assay and a cell migration assay, Figure .…”

Section: α5β1 Non-rgd-mimetic Inhibitorsmentioning

confidence: 99%

“…More recently, another non-RGD-mimetic inhibitor of α 5 β 1 was reported by Kang and Kim. 68 Termed IPS-05002, compound 25 68 was identified by a screen of a phytochemical compound library using a ProteoChip-based protein−protein interaction assay for α 5 β 1 antagonists. This compound showed micromolar inhibition of α 5 β 1 in a cell proliferation assay and a cell migration assay, Figure 14.…”

Section: Journal Of Medicinal Chemistrymentioning

confidence: 99%

See 1 more Smart Citation

Emergence of Small-Molecule Non-RGD-Mimetic Inhibitors for RGD Integrins

et al. 2017

View full text Add to dashboard Cite

The RGD integrins are recognized therapeutic targets for thrombosis, fibrosis, and cancer, amongst others. Current inhibitors are designed to mimic the tripeptide sequence (arginineglycine-aspartic acid) of the natural ligands; however, the RGD-mimetic antagonists for α IIb β 3 have been shown to cause partial agonism, leading to the opposite pharmacological effect. The challenge of obtaining oral activity and synthetic tractability with RGD-mimetic molecules, along with the issues relating to pharmacology, has left integrin-therapeutics in need of a new strategy. Recently, a new generation of inhibitor has emerged that lacks the RGD-mimetic. This 2 perspective will discuss the discovery of these non-RGD-mimetic inhibitors, and the progress that has been made in this promising new chemotype.

show abstract

Section: α5β1 Non-rgd-mimetic Inhibitorsmentioning

confidence: 99%

Section: Journal Of Medicinal Chemistrymentioning

confidence: 99%