Document Detail


The autophilic anti-CD20 antibody DXL625 displays enhanced potency due to lipid raft-dependent induction of apoptosis.
MedLine Citation:
PMID:  20216307     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Despite widespread use of anti-CD20 antibodies as therapeutic agents for oncologic and autoimmune indications, precise descriptions of killing mechanisms remain incomplete. Complement-dependent cytolysis and antibody-dependent cell-mediated cytotoxicity are indicated as modes of target cell depletion; however, the importance of apoptosis induction is controversial. Studies showing that the therapeutic anti-CD20 antibody rituximab (Rituxan) mediates apoptosis of tumor cell targets in vitro after cross-linking by anti-Fc reagents suggest that enhancement strategies applied to Fc-independent activities for anti-CD20 antibodies could improve therapeutic efficacy. An anti-CD20 antibody designated DXL625, with autophilic properties such as increased binding avidity, is shown here to independently induce caspase-mediated apoptosis of an established B-cell lymphoma line in vitro. Depletion of membrane cholesterol or chelation of extracellular calcium abrogated the pro-apoptotic activity of DXL625, indicating that intact lipid rafts and calcium are required for this activity. The Fc-mediated complement-dependent and antibody-dependent cellular killing mechanisms are maintained by DXL625 despite conjugation of the parental Rituxan antibody to the autophilic DXL peptide sequence. This study shows a strategy for improving anti-CD20 immunotherapy by endowing therapeutic antibodies with self-interacting properties.
Authors:
Marc G Bingaman; Gargi D Basu; Tiana C Golding; Samuel K Chong; Andrew J Lassen; Thomas J Kindt; Christopher A Lipinski
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Anti-cancer drugs     Volume:  21     ISSN:  1473-5741     ISO Abbreviation:  Anticancer Drugs     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-04-14     Completed Date:  2010-05-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9100823     Medline TA:  Anticancer Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  532-42     Citation Subset:  IM    
Affiliation:
InNexus Biotechnology Inc, Scottsdale, Arizona, USA.
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MeSH Terms
Descriptor/Qualifier:
Antibodies, Monoclonal / pharmacology*
Antigens, CD20 / immunology
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects*
Calcium / metabolism
Cell Line, Tumor
Cell Proliferation / drug effects
Humans
Membrane Microdomains / drug effects*
Chemical
Reg. No./Substance:
0/Antibodies, Monoclonal; 0/Antigens, CD20; 0/Antineoplastic Agents; 0/rituximab; 7440-70-2/Calcium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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