Navigation Links
Data: ATSP-7041 as first-in-class p53 pathway re-activator for solid/ hematologic cancers
Date:8/15/2013

CAMBRIDGE, Mass., August 15, 2013 Aileron Therapeutics, Inc., a clinical stage biopharmaceutical company that is developing first-in-class therapeutics based on its proprietary Stapled Peptide drug platform, announced today the publication of preclinical data on ATSP-7041, a potent and selective stapled peptide re-activator of the wild type p53 tumor suppressor protein. P53, known as "the guardian of the genome" because it repairs damaged DNA or triggers cell death in pre-cancerous cells, is one of the most important known tumor suppressors, as it is shown to be inactivated in virtually all human cancers. As 50% of all cancers circumvent P53's protective mechanisms by the over-expression of the inhibitory proteins MDM2 and MDMX, Aileron's stapled peptide is novel in that it can selectively bind to and inhibit both proteins equally and, thereby, restore the P53 function. The research, published in Proceedings of the National Academy of Sciences (PNAS), provides the first detailed publication by Aileron of one of its cell penetrating peptides that is a precursor molecule to one that the company is developing for the treatment of both liquid and solid tumors. The paper, entitled "Stapled α−Helical Peptide Drug Development: A Potent Dual Inhibitor of MDM2 and MDMX for p53-Dependent Cancer Therapy," expands on data reported by the company in poster presentations at the 2012 EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics and the 2013 International MDM2 workshop in Cambridge, England.

"As evidenced by the multitude of research and clinical efforts, the full activation of p53 has been the goal of cancer researchers for decades given its [ubiquitous] role in all human cancers" said Joseph A. Yanchik III, president and chief executive officer of Aileron Therapeutics. "Our stapled peptide drug will be the first full-activator of wild type p53 of its kind to our knowledge to enter clinical trials. Our unique approach to restore p53 activity through direct inhibition of both MDM2 and MDMX has the potential to deliver greater efficacy and safety than existing small molecule approaches, which are primarily limited to inhibition of just MDM2. We look forward to advancing the p53 program into clinical trials next year that will represent our second stapled peptide drug to enter human clinical trials."

Key findings from the paper showed that ATSP 7041:

  • suppressed tumor growth in animal models of multiple human xenograft models, including breast cancer and bone cancer

  • is an equipotent dual inhibitor of MDM2 and MDMX that restores p53 specific activity

  • is a peptide that efficiently penetrated cell membranes and exhibited a more durable on mechanism effect on p53 signaling than small-molecule MDM2-selective inhibitors

  • exhibited favorable drug-like and pharmacokinetic properties that can support convenient clinical dosing regimens [including the potential for once-weekly dosing]


'/>"/>

Contact: Kathryn Morris
kathryn@theyatesnetwork.com
914-204-6412
The Yates Network
Source:Eurekalert

Related medicine news :

1. New concussion data: 2 biomarkers better than 1
2. Cellular pathway linked to diabetes, heart disease
3. Unusual protein helps regulate key cell communication pathway
4. Mutant Kras drives pancreatic cancer maintenance via metabolic pathways
5. Breast stem-cell research: Receptor teamwork is required and a new pathway may be involved
6. VCU researchers identify changes in cholesterol metabolic pathways
7. Researchers determine pathway for origin of most common form of brain and spinal cord tumor
8. Inhibiting Hedgehog signaling pathway may improve pancreatic cancer treatment
9. Global Energy Assessment identifies pathways to a sustainable energy future
10. Grb2 holds powerful molecular signaling pathway in check
11. Researchers block pathway to cancer cell replication
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/24/2017)... McLean, Virginia (PRWEB) , ... April 24, 2017 ... ... have announced that they are seeking public support to bring their novel lifesaving ... in appearance, wearable device packed with medical-grade sensors, specially designed to read a ...
(Date:4/24/2017)... ... April 24, 2017 , ... symplrTM, a leading provider of ... that Kyle Allain has joined the company as Vice President and General Manager ... provider, payor and managed care solutions. , A seasoned executive with more ...
(Date:4/24/2017)... ... April 24, 2017 , ... MAP Health ... anxiety levels in people with addiction who are served by MAP’s patient engagement ... wearable device that monitors heart and breath rates to identify anxiety levels and ...
(Date:4/24/2017)... ... April 24, 2017 , ... As a former supermodel ... thousand words. The good news for single women is that she put all the ... available on April 25th. Joan's insight, personal experiences and sparkling sense of humor have ...
(Date:4/24/2017)... ... April 24, 2017 , ... Donna Parker, L. Ac. reads all sorts of ... of them to be very practical. She wanted to write a guide/workbook that would ... their health. It prompted her in writing “ A Clear Path to a Vibrant ...
Breaking Medicine News(10 mins):
(Date:4/20/2017)... , April 20, 2017  Zimmer Biomet Holdings, ... musculoskeletal healthcare, today announced that it will be participating ... Conference at the InterContinental Hotel in Boston, ... Biomet will present at 11:20 a.m. Eastern Time. ... accessed via Zimmer Biomet,s Investor Relations website at ...
(Date:4/20/2017)... April 20, 2017  CVS Pharmacy, the retail ... a new store design to enhance the retail ... food, health-focused products and expanded beauty selections paired ... customers discover new offerings. Together with its innovative ... of the customer experience at CVS Pharmacy.  ...
(Date:4/20/2017)... , April 20, 2017 ... platform, the first non-viral gene expression technology that enables ... the eye to address a wide range of ophthalmic ... Medicines and Healthcare products Regulatory Agency (MHRA) to advance ... ...
Breaking Medicine Technology: