Method for determining modulation of p110δ activity

Details Method for determining modulation of p110δ activity Method for determining modulation of p110δ activity

2005-02-01

2005-02-01

Rao, Manjunath N. (Department: 1652)

Chemistry: molecular biology and microbiology

Measuring or testing process involving enzymes or...

Involving hydrolase

C435S004000, C435S006120, C435S018000, C435S069100, C435S183000, C435S195000, C435S196000, C435S252300, C435S348000, C435S320100, C536S023200, C536S023400, C536S023500, C530S350000

Reexamination Certificate

active

06849420

ABSTRACT:
The invention relates to a novel lipid kinase which is part of the PI3 Kinase family. PI3 Kinases catalyze the addition of phosphate to inositol generating inositol mono, di and triphosphate. Inositol phosphates have been implicated in regulating intracellular signaling cascades resulting in alternations in gene expression which, amongst other effects, can result in cytoskeletal remodeling and modulation of cellular motility. More particularly the invention relates to a novel human PI3 Kinase, p110Δ which interacts with p85, has a broad phosphinositide specificity and is sensitive to the same kinase inhibitors as PI3 Kinase p110A. However, in contrast to previously identified PI3 Kinases which show a ubiquitous pattern of expression, p110Δ is selectively expressed in leucocytes. Importantly, p110Δ shows enhanced expression in most melanomas tested and therefore may play a crucial role in regulating the metastatic property exhibited by melanomas. The identification of agents that enhance or reduce p110Δ activity may therefore prevent cancer metastatis.

REFERENCES:
Hu et al. (Mol. Cell. Biol., 1993, vol. 13(12):7677-7688).*
Stephens et al. (Cell, 1994, vol. 77, 83-93).*
Vanhaesebroeck et al. (FASEB Journal, Apr. 30, 1996, vol. 10(6):p1380).

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