Curis Hedgehog and Beyond --plus multi-targeting cancer inhibitors

Novel Anti-Cancer therapies

Skip to content

It is currently Tue Feb 07, 2012 5:11 pm

  • CUDC-101 (HDAC/EGFR/Her2 inhibitor)
    Topics surrounding a novel approach to fighting cancers
    News of CUDC-101 (HDAC/EGFR/Her2 inhibitor) News  Site map of CUDC-101 (HDAC/EGFR/Her2 inhibitor) Site map  RSS Feed of CUDC-101 (HDAC/EGFR/Her2 inhibitor) RSS Feed  Sitemap of CUDC-101 (HDAC/EGFR/Her2 inhibitor) Sitemap 
    2 Topics
    2 Posts
    Last postCUDC-101 Medicinal ...
    by hedgehog View the latest post
    Sat Feb 27, 2010 4:12 pm
  • No new posts HSP90 Debio-0932 (CUDC-305)
    Debio 0932 (formerly CUDC-305) is a small molecule inhibitor of Heat Shock Protein 90 (Hsp90). Debio0932 is expected to enter Phase I clinical testing in early Q1 2010.
    News of HSP90 Debio-0932 (CUDC-305) News  Site map of HSP90 Debio-0932 (CUDC-305) Site map  RSS Feed of HSP90 Debio-0932 (CUDC-305) RSS Feed  Sitemap of HSP90 Debio-0932 (CUDC-305) Sitemap 
    2 Topics
    3 Posts
    Last postAbout Debio-0932 ...
    by hedgehog View the latest post
    Fri Feb 19, 2010 2:27 pm
  • CU-201 (an Inhibitor of HDAC, SFK and Abl Kinases)
    CU-201 is a network-targeted molecule that is designed to simultaneously inhibit HDAC, Abl and Src family kinases, the combination of which Curis scientists believe have synergistic interaction against cancer cells. Src family kinases are critical components of multiple signaling pathways that regulate cancer cell proliferation, survival, angiogenesis and metastasis. Thus, as a network disrupting agent that directly targets multiple nodes of genetic and epigenetic dysregulation, CU-201 is expected to impact processes as diverse as proliferation, survival, metastasis and angiogenesis in cancer. In vitro studies demonstrate that CU-201 is able to potently inhibit class I and class II HDACs, Src and Bcr-Abl. It has been shown to outperform single target agents in proliferation assays of hematologic and solid tumor lines and to inhibit migration and invasion of cancer cell lines in vitro. In vivo, it displays potent anti-tumor activity in a variety of hematologic and solid tumor models, including subcutaneous, metastatic and orthotopic models.
    News of CU-201 (an Inhibitor of HDAC, SFK and Abl Kinases) News  Site map of CU-201 (an Inhibitor of HDAC, SFK and Abl Kinases) Site map  RSS Feed of CU-201 (an Inhibitor of HDAC, SFK and Abl Kinases) RSS Feed  Sitemap of CU-201 (an Inhibitor of HDAC, SFK and Abl Kinases) Sitemap 
    1 Topics
    1 Posts
    Last postCU-201 Preclinical Data
    by hedgehog View the latest post
    Mon Dec 06, 2010 10:20 am
  • CU-906 (Inhibitor HDAC and PI3K/mTOR)
    CU-906 is a multi-targeted molecule that is designed to inhibit HDAC and PI3K and mTOR kinases, the combination of which Curis scientists believe have synergistic interaction against cancer cells. In vitro mechanism of action studies demonstrated that CU-906 is able to inhibit Class I PI3K and mTOR kinases, suppress multiple nodes of other survival pathways including the RAF-MEK-ERK pathway, and upregulate P21, which is a cyclin-dependent kinase inhibitor that can promote cancer cell death when upregulated. The suppression of non-PI3K-AKT-mTOR survival pathways occurs via epigenetic modification as a result of the inhibition of HDAC, the non-kinase target of CU-906. By contrast, single-target PI3K inhibitors and PI3K/mTor dual inhibitors that only target the primary PI3K and/or mTOR kinase survival pathways, have only been shown to have limited effects on tumors with disregulation of other signaling pathways.

    CU-906 exhibits anti-proliferation activity against a broad range of cancer cell types in in vitro studies, including cell lines that are insensitive to PI3K inhibitors. CU-906's anti-proliferation activity is up to 100 times more potent than that of two leading PI3K inhibitors in development. Efficacy studies in various K-RAS mutant tumor xenograft models indicate that this compound has more potent antitumor activity than a leading PI3K inhibitor that is currently in clinical development, at doses causing no obvious side effects to the tumor-bearing animals.

    Importantly, CU-906 displays high exposure and long half-life in tumor tissue after IV administration and is orally bioavailable in preclinical models. CU-906 has a half-life of more than 10 hours in xenograft tumors, induces apoptosis and inhibits cell proliferation up to 48 hours following a single dose of the compound to tumor-bearing animals.
    News of CU-906 (Inhibitor HDAC and PI3K/mTOR) News  Site map of CU-906 (Inhibitor HDAC and PI3K/mTOR) Site map  RSS Feed of CU-906 (Inhibitor HDAC and PI3K/mTOR) RSS Feed  Sitemap of CU-906 (Inhibitor HDAC and PI3K/mTOR) Sitemap 
    1 Topics
    2 Posts
    Last postCU-906 Preclinical ...
    by hedgehog View the latest post
    Thu Dec 09, 2010 5:54 pm
  • CU-907 (Inhibitor HDAC and PI3K/mTOR)
    CUDC-907 is an orally bioavailable, multi-targeted small molecule that is designed to inhibit HDAC and PI3K, the combination of which Curis scientists believe have synergistic interaction against cancer cells. In vitro mechanism of action studies demonstrate that CUDC-907 is able to inhibit Class I PI3K and upregulate molecules involved in cancer cell death. CUDC-907 has also demonstrated the ability to suppress multiple nodes of other survival pathways as a result of the epigenetic modification resulting from the inhibition of its non-kinase HDAC target. By contrast, single-target PI3K inhibitors only target the primary PI3K survival pathway and reportedly have only limited effects on tumors with disregulation of other signaling pathways.
    News of CU-907 (Inhibitor HDAC and PI3K/mTOR) News  Site map of CU-907 (Inhibitor HDAC and PI3K/mTOR) Site map  RSS Feed of CU-907 (Inhibitor HDAC and PI3K/mTOR) RSS Feed  Sitemap of CU-907 (Inhibitor HDAC and PI3K/mTOR) Sitemap 
    1 Topics
    1 Posts
    Last postAbout CUDC-907
    by hedgehog View the latest post
    Mon Jan 10, 2011 5:45 pm

Login  •  Register

Who is online

In total there are 2 users online :: 0 registered, 0 hidden and 2 guests (based on users active over the past 5 minutes)
Most users ever online was 39 on Sun Apr 04, 2010 7:45 am

Registered users: No registered users
Legend: Administrators, Global moderators

Statistics

Total posts 46 • Total topics 32 • Total members 44 • Our newest member JPZaragoza

Powered by phpBB © 2000, 2002, 2005, 2007 phpBB Group

phpBB SEO
cron