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Technology ID
TAB-4191

Renal Selective Unsaturated Englerin Analogues

E-Numbers
E-072-2014-0
Lead Inventors
Beutler, John
Co-Inventors
Ransom, Tanya
Echavarren, Antonio
Ratel, Frederic
Applications
Therapeutics
Therapeutic Areas
Oncology
Infectious Disease
Endocrinology
Development Stages
Discovery
Lead IC
NCI
ICs
NCI

Englerin A, a natural product, has shown growth-inhibiting activity against renal cancer cell lines. The compound is an agonist of protein kinase C (PCK) theta, which results in cell cytotoxicity, insulin inhibition, and selective activation of viral replication in T cells.  Englerin A derivatives are promising treatment strategies for any diseases associated with PKC theta and/or ion channel proteins.

Researchers at the National Cancer Institute have developed a series of Englerin A analogs for the treatment of renal cancer. The new derivatives are less toxic than the parent compound and have shown effective inhibition of growth in vitro.

Competitive Advantages:

  • PKC theta associated with a number of immune disorders, cancers, and HIV
  • Reduced toxicity compared to parent Englerin A compounds

Commercial Applications:

  • Renal cancer therapeutic
  • HIV therapeutic

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Licensing Contacts
Dick, Taryn
taryn.dick@nih.gov

Related Inventions

  • E-064-2008           TAB-4262
    Cancer Inhibitors Isolated from an African Plant
  • E-090-2014           TAB-4340
    Natural product-based anti-cancer agents: aza-Englerin analogues
  • E-140-2017

Patents

  • US
    Provisional (PRV) 62/146,805
    Filed on 2015-04-13
    Status: Abandoned
  • Patent Cooperation Treaty
    (PCT) PCT/US2016/027262
    Filed on 2016-04-13
    Status: Expired
  • Australia
    National Stage 2016247920
    Filed on 2016-04-13
    Status: Issued
  • Canada
    National Stage 2982564
    Filed on 2016-04-13
    Status: Issued
  • European Patent
    National Stage 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Japan
    National Stage 2017-554513
    Filed on 2016-04-13
    Status: Issued
  • US Patent 10,287,297
    Filed on 2016-04-13
    Status: Issued
  • Belgium
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Switzerland
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Germany
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Denmark
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Spain
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • France
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • United Kingdom
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Italy
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Norway
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued
  • Sweden
    European patent (EP) 16718144.5
    Filed on 2016-04-13
    Status: Issued

Publications

Collaborations

  • Licensing
  • Collaboration
Date Published