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VANCOUVER, BC--(Marketwired - November 29, 2016) - Advanced Proteome Therapeutics Corporation ("APC" or the "Company") (TSX VENTURE: APC) ( : 0E8) is pleased to announce that it has invented a measurable basis for evaluating antibody labeling that provides key information on the pattern of labeling. The technology provides a means of sorting labeling entities according to the degree of selective labeling resulting from modification of a target antibody for conjugation. The methodology produces a rank order of candidate antibodies carrying antibody connectors for linkage to payloads such as drugs or toxins which should aid decision-making in ADC development. Immense growth is expected for the therapeutic antibody market which is estimated to reach nearly $125 Billion USD by the year 2020 (The therapeutic monoclonal antibody market: Ecker et al. MAbs 2015, Volume 7, ppgs 9-14.). This invention was developed to fulfil the Company's recently announced partnering initiatives with Wilex AG's subsidiary, Heidelberg Pharma GmbH and the Toronto Recombinant Antibody Centre (TRAC) at the University of Toronto. The method has been applied to measurements of the selectivity pattern that emerges from APC's experimental conditions for labeling commercially marketed antibody targets. Despite being prerequisites for a reliable assessment of performance of labeling technology, quantitative methods for the rapid determination of the purity of antibody-drug conjugates, and an analysis of the labeling pattern which produces them, have been lacking. APC's approach to impacting the field of antibody-drug conjugates is to design a labeling entity that places a handle on the antibody to which virtually any payload such as a drug or toxin can be attached. Since the Company is targeting "universal" sites on antibodies, the type that all IgG antibodies possess, it is important to emphasize that our approach could ultimately enable attaching drugs or toxins to any target antibody selectively, for which quantitative measurements are essential. (IgGs are the principal antibody carriers of ADCs.) Apropos of the above, APC is focusing on enabling technology, designed to link antibodies to drugs or toxins to produce pure and homogeneous antibody-drug conjugates. The field of antibody-drug conjugates affords numerous opportunities for improving the properties of therapeutic antibodies, but reliable methods for site-specifically attaching drugs or toxins to antibodies to give ADCs of high purity are needed to avoid the heterogeneity that currently limits applications of ADCs. The number of therapeutic antibodies and the companies producing them are legion, and growing, but comparatively few companies have capabilities for chemical modification of such antibodies aimed at producing "kinder and gentler" agents than classical chemotherapeutics. Advanced Proteome Therapeutics Corporation (APC) is advancing a site-specific protein modification technology platform to enable the development of superior protein therapeutics. Using this technology, APC has generated numerous and diverse modifications of annexin proteins with superior binding and stability properties, which are amenable to further labeling and conjugation for use in therapeutic applications. APC is now vigorously applying its technologies to achieve the site-specific labeling of therapeutic antibodies and provide the next generation of antibody-drug conjugates. Neither the TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts responsibility for the adequacy or accuracy of this release. The forward-looking statements contained in this news release involve risks and uncertainties, and are subject to change based on various important factors including timely development and acceptance of new products, gaining product approval, successful entry into new markets, changes in financing conditions, and changes in FDA regulations.

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.

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

For more information about Advanced Proteome Therapeutics, please contact: Dr. Allen (Alexander) Krantz President & CEO Advanced Proteome Therapeutics Corporation ...

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 ...

Advanced Proteome Therapeutics | Entity website

Immunotherapy Stimulating the immune system to unleash the bodys natural defenses against cancerous cells. Learn More

PubMed | Optivia Biotechnology, Thermo Fisher Scientific, Advanced Proteome Therapeutics, ConjuChem and Bruker Daltonics Inc.
Type: | Journal: Computational and structural biotechnology journal | Year: 2014

The first example of a kinetic labeling library designed to enable the discovery of affinity labels is presented. Each library component (1) consists of a variable peptidyl component linked to a biotinyl moiety by a 4-mercaptobenzoyl linker in thioester format. We demonstrate that an affinity label can be uncovered by measuring reaction rates between library pools and the protein target, human serum albumin (HSA) and identifying significant outliers. By choosing peptide functionality compatible with a potentially reactive thioester labeling entity, libraries can be screened in pools. It is noteworthy that a limited subset of amino acids (R, S, E, F, Y, l, M, W, and Q) that compose the affinity moiety is sufficient to produce rate variances that guide the discovery process. After two rounds of deconvolution, J-FLYEE-NH2 (7-E) emerges as a bona fide affinity label of HSA. Unlike known affinity labels, the affinity moiety is not retained in the protein product, but is extruded upon acylation of the protein. This feature affords a method of introducing various payloads, without extraneous elements, onto protein frameworks.

The present invention relates to the formation of conjugates (e.g., protein-protein dimers) using a-halo-acetophenones, benzylic halides, quinones, and related compounds as a conjugating system. The invention also features compositions that include the conjugates described herein, as well as uses of these conjugates in methods of medical treatment.

Advanced Proteome Therapeutics | Entity website

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