Kinase inhibitor screening
| Kinases . | Inhibitors . | . | . | . | . | . | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|
. | 100 μM Genistein . | 10 μM PP2 . | 1 μM SU6656 . | 10 μM Imatinib . | 200 μM LFM-A13 . | 1 μM VEGFR kinase inhibitor . | |||||
| ABL | + | + | − | + | |||||||
| ABL1 E255K | + | + | |||||||||
| ABL1 G250E | + | + | |||||||||
| ABL1 Y253F | + | + | |||||||||
| ABL2 (ARG) | + | + | |||||||||
| BMX | + | − | + | ||||||||
| CSK | + | − | − | ||||||||
| EGFR | + | + | − | − | − | ||||||
| ERBB4 (HER4) | + | + | |||||||||
| FGR | + | + | |||||||||
| FLT4 (VEGFR3) | + | − | + | ||||||||
| FYN | + | + | + | − | |||||||
| KDR (VEGFR2) | + | − | + | ||||||||
| PDGFRA D842V | + | + | |||||||||
| PDGFRB | + | − | + | + | |||||||
| SRC | + | + | + | − | − | ||||||
| YES | + | + | + | − | |||||||
| Kinases . | Inhibitors . | . | . | . | . | . | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|
. | 100 μM Genistein . | 10 μM PP2 . | 1 μM SU6656 . | 10 μM Imatinib . | 200 μM LFM-A13 . | 1 μM VEGFR kinase inhibitor . | |||||
| ABL | + | + | − | + | |||||||
| ABL1 E255K | + | + | |||||||||
| ABL1 G250E | + | + | |||||||||
| ABL1 Y253F | + | + | |||||||||
| ABL2 (ARG) | + | + | |||||||||
| BMX | + | − | + | ||||||||
| CSK | + | − | − | ||||||||
| EGFR | + | + | − | − | − | ||||||
| ERBB4 (HER4) | + | + | |||||||||
| FGR | + | + | |||||||||
| FLT4 (VEGFR3) | + | − | + | ||||||||
| FYN | + | + | + | − | |||||||
| KDR (VEGFR2) | + | − | + | ||||||||
| PDGFRA D842V | + | + | |||||||||
| PDGFRB | + | − | + | + | |||||||
| SRC | + | + | + | − | − | ||||||
| YES | + | + | + | − | |||||||
Listed are tyrosine kinases that are PP2 sensitive, expressed in arterial ECs, and likely localized to cell–cell contacts. Their susceptibility to other inhibitors is indicated. −, inhibition by <60% ; +, inhibition by >60%; blank, no data available. PECAM-1 response was inhibited by Genistein, PP2, and SU6656 and was not inhibited by Imatinib, LFM-A13, and VEGFR kinase inhibitor (Fig. 5, A and B). Kinase susceptibility is obtained from the following sources: Genistein, Akiyama and Ogawara (1991); PP2 and Imatinib, http://www.invitrogen.com/downloads/SelectScreen_Data_193.pdf; SU6656, Blake et al. (2000); LFM-A13, Chau et al. (2002) and Mahajan et al. (1999); and VEGFR kinase inhibitor, Cools et al. (2004) and Fraley et al. (2002).