Re: PI3K Alpha isoform suggested target

[Guest guest]

The problem with targeting the alpha isoenzyme is that it is

also expressed in most cells in the body. Thus, toxicities

are expected with such an agent. That is why delta is an

ideal target, it is only expressed in hematopoietic cells.

There are several delta targeting drugs in development, so

stayed tuned...

Rick Furman

>

> CAL101 is a PI3-K delta inhibitor.

>

> A paper to be presented at the EHA Congress looks at PI3-K-

> isoform 'alpha'.

>

> CLL cells express all four PI3-K-p110 isoforms (alpha, beta,

> gamma and delta) at the mRNA and protein at higher levels

> than samples of healthy individuals.

>

> Targeting the PI3K pathway with alpha isoform-specific

> inhibitors significantly induces apoptosis in CLL cells and

> overcome the supportive effect of bone marrow stromal cells.

>

> Source:

http://www.eventure-online.com/eventure/publicAbstractView.do?id=163060 & congress\

Id=4634

>

> or

>

> http://tinyurl.com/4xu3nhy

>