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Boston, MA, United States

Yu P.,Alcon | Strug I.,Millipore | Cafarella T.R.,Boston University | Seaton B.A.,Boston University | Krantz A.,Advanced Proteome Therapeutics
Organic and Biomolecular Chemistry | Year: 2012

Annexin V (1) specifically binds to phosphatidylserine on apoptotic and necrotic cells as well as certain cancer cells, making it an attractive vehicle for the delivery of therapeutically-relevant conjugates to such sites. The wild-type protein possesses a single thiol at Cys316, which is difficultly accessible to site-specific labeling by simple maleimides. By contrast, 1,4-benzoquinone site-specifically labels annexin V in minutes. The resulting conjugate (5) serves as an intermediate for crosslinking annexin molecules, which can be accomplished within hours either directly for linking annexin V-128 (19), or via an extended sequence involving the crosslinking of two units of (5) by the symmetrical α,ω-dithiol (20). Besides its ability to mediate protein dimer formation while retaining annexin V's ability to bind phosphatidylserine, (5) possesses classic 1,4-benzoquinone reactivity. Various nucleophiles and Diels-Alder dienes form adducts with (5) in reactions that may have general utility for the synthesis of novel biologically active entities. The present work presents the first example of thiol-specific crosslinking of proteins by 1,4-quinone-based methodology designed to exploit the reactivity of this versatile chemical entity. © 2012 The Royal Society of Chemistry. Source


Patent
Advanced Proteome Therapeutics | Date: 2013-05-13

The present invention relates to the formation of protein conjugates from proteins chemically modified for linkage to (1) anticancer drug pharmacophores, (2) ligands to biomarkers on cancer cell surfaces, (3) and/or another protein molecule. It provides and specifies new compositions, methods and combinations for tumor, and tumor vasculature targeting and cancer treatment.


Advanced Proteome Therapeutics | Entity website

Investor Information We are a reporting company in Canada and file with the Canadian Securities Administrators our annual reports with annual financial statements, interim reports, management information, circulars (proxy statements), press releases, and other items, which are publicly available on SEDAR at www.sedar ...


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In the News Advanced Proteome Therapeutics will provide the latest stories as the media reports our progress, as well as other articles of interest about our technology and industry


Advanced Proteome Therapeutics | Entity website

The Foundation Trinity Technology: Combining Anti-Cancer Therapies in a Single Agent for Targeted Delivery to Tumors Cancer is a complex disease, and for therapies to be maximally effective and tolerable, they must distinguish between normal and cancerous cells. Advanced Proteome Therapeutics Corporation, through its subsidiary, Advanced Proteome Therapeutics Inc ...

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