Navigation Links
SF1126, Semafore's PI3 Kinase Inhibitor, Found to Block Angiogenic Signaling From Both VEGF and Bv8 in Multiple Cell Lines
Date:8/26/2008

INDIANAPOLIS, Aug. 26 /PRNewswire/ -- Semafore Pharmaceuticals Inc. announced data presented at the Seventh International Congress on Targeted Therapies in Cancer in Washington, D.C., showing additional antiangiogenic activity of vascular-targeted PI3 kinase (PI3K) inhibitor SF1126, by blocking both VEGF and Bv8 signaling.

PI3K is part of a very powerful pathway, the PI3/AKT /mTOR pathway that has been shown to play a major role in cancer. Studies have shown that by inhibiting this pathway, tumor growth can be suppressed.

SF1126, a vascular targeted pan-PI3K inhibitor conjugate currently in Phase I clinical trials, was shown to block the pAKT pathway through which the angiogenic factors VEGF and Bv8 are involved. Bv8 is a recently identified protein that, like VEGF, plays a role in the angiogenic process and can significantly upregulate pAKT levels thereby supporting tumor growth.

In vitro inhibition of the PI3K/AKT/mTOR pathway by SF1126 was demonstrated to impede the ability of angiogenic stimulants VEGF and Bv8 to activate AKT in a dose dependant manner in two cancer cell lines (786-0 -- renal cell and PC3 prostate) and one endothelial cell line (HBEC -- human brain endothelial cells). Inhibiting Bv8 with antibodies has also been shown by others to have antitumor effects in mouse xenograft models.

"SF1126 could have additional impact in treating cancer where Bv8 is an important component of angiogenesis," said Dr. Dennis McKeever, Semafore's Chief Executive Officer. "In addition to targeting angiogenesis, SF1126 blocks key targets involved in tumor growth including mTOR, DNA-PK, PIM-1 and PLK-1. This adds another layer of versatility to what SF1126 can do as an antitumor agent."

About Semafore

Semafore is a clinical stage drug discovery and development company focused on small molecule modulators of the PI3 kinase and PTEN cell signaling pathway, a promising target pathway for multiple disorders, including the comp
'/>"/>

SOURCE Semafore Pharmaceuticals Inc.
Copyright©2008 PR Newswire.
All rights reserved

1

GOOD

Page: 1 2 3

Related medicine technology :

1. Semafore Pharmaceuticals Reports Positive Interim Results from a Phase I Study of SF1126, a Targeted Pan-PI3K Inhibitor, in Patients with Advanced Solid Tumors
2. Telik Announces Presentation of Preclinical Data on Dual Inhibitors of Aurora Kinases and VEGFR2
3. Telik Announces Preclinical Data Demonstrating Anti-Cancer Activity of Dual Inhibitors of Aurora Kinase and VEGFR2
4. Semafores PI3 Kinase Inhibitor SF1126 is Active Against Tumor and Tumor Cells and Synergizes with Standard Chemotherapy Agents
5. SuperGen Reports Initiation of Multi-arm Phase 1b Trial of Novel Tyrosine Kinase Inhibitor
6. EntreMed to Highlight ENMD-2076 Kinase Inhibitor at 2008 AACR Annual Meeting
7. Semafores PI3 Kinase Inhibitor SF1126 is a Vascular Targeted Conjugate in Phase I Clinical Trials in Solid Tumors and Multiple Myeloma
8. Ardea Biosciences Presents Data Demonstrating Favorable Pharmacokinetics and Efficacy for Mitogen-Activated ERK Kinase (MEK) Inhibitors
9. SuperGen Identifies Lead PIM Kinase Inhibitor, SGI-1776, That Causes Tumor Regression in AML Xenograft Models
10. Latest Cell Publication Describes the Novel Kinase Regulators Using OriGenes Functional Kinome Collection
11. Poniard Pharmaceuticals Licenses Kinase Inhibitors From The Scripps Research Institute
Post Your Comments:
*Name:
*Comment:
*Email: