1196449-87-2Relevant academic research and scientific papers
Preparation and Evaluation of Radiolabeled Antibody Recruiting Small Molecules That Target Prostate-Specific Membrane Antigen for Combined Radiotherapy and Immunotherapy
Genady, Afaf R.,Janzen, Nancy,Banevicius, Laura,El-Gamal, Mahmoud,El-Zaria, Mohamed E.,Valliant, John F.
, p. 2660 - 2673 (2016/04/10)
The feasibility of developing a single agent that can deliver radioactive iodine and also direct cellular immune function by engaging endogenous antibodies as an antibody-recruiting small molecule (ARM) was determined. A library of new prostate-specific membrane antigen (PSMA)-binding ligands that contained antibody-recruiting 2,4-dinitrophenyl (DNP) groups and iodine were synthesized and screened in vitro and in vivo. A lead compound (9b) showed high affinity for PSMA and the ability to bind anti-DNP antibodies. Biodistribution studies of the iodine-125 analogue showed 3% ID/g in LNCaP xenograft tumors at 1 h postinjection with tumor-to-blood and tumor-to-muscle ratios of 10:1 and 44:1, respectively. The radiolabeled analogue was bound and internalized by LNCaP cells, with both functions blocked using a known PSMA inhibitor. A second candidate showed high tumor uptake (>10% ID/g) but had minimal binding to anti-DNP antibodies. The compounds reported represent the first examples of small molecules developed specifically for combination immunotherapy and radiotherapy for prostate cancer.
BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS
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, (2012/11/07)
The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H′ function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and b
Chemical control over immune recognition: A class of antibody-recruiting small molecules that target prostate cancer
Murelli, Ryan P.,Zhang, Andrew X.,Michel, Julien,Jorgensen, William L.,Spiegel, David A.
supporting information; experimental part, p. 17090 - 17092 (2010/03/25)
(Figure Presented) Prostate cancer is the second leading cause of cancer-related death among the American male population, and society is in dire need of new approaches to treat this disease. Here we report the design, synthesis, and biological evaluation
An antibody-recruiting small molecule that targets HIV gp120
Parker, Christopher G.,Domaoal, Robert A.,Anderson, Karen S.,Spiegel, David A.
supporting information; experimental part, p. 16392 - 16394 (2010/02/16)
(Chemical Equation Presented) HIV/AIDS is a global pandemic for which new treatment strategies are desperately needed. We have designed a novel small molecule, designated as ARM-H, that has the potential to interfere with HIV survival through two mechanis
