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(6-Maleimidocaproyl)hydrazone of doxorubicin--a new derivative for the preparation of immunoconjugates of doxorubicin.
TLDR
DTT reduction of disulfides present in the mAb was a reliable and general method for generating a consistent number of reactive SH groups and BR96 conjugates showed antigen-specific cytotoxicity. Expand
Site-specific covalent modification of monoclonal antibodies: in vitro and in vivo evaluations.
TLDR
In vivo results suggest that oligosaccharide modification of monoclonal antibodies is a preferred method of preparing conjugates, compared to more conventional methods. Expand
Monoclonal antibody conjugates of doxorubicin prepared with branched peptide linkers: inhibition of aggregation by methoxytriethyleneglycol chains.
TLDR
The data suggest that the methoxytriethylene glycol chain hydrolyzes as designed upon antigen-specific internalization into tumor lysosomes in vitro, where enzymatic degradation of the peptide linker releases free doxorubicin. Expand
Monoclonal antibody conjugates of doxorubicin prepared with branched linkers: A novel method for increasing the potency of doxorubicin immunoconjugates.
TLDR
The results suggest that, by using the branched linker methodology, it is possible to significantly reduce the amount of mAb required to achieve antigen-specific cytotoxic activity. Expand
Effect of linker variation on the stability, potency, and efficacy of carcinoma-reactive BR64-doxorubicin immunoconjugates.
TLDR
The increased stability of theBR64-S-DOX conjugates resulted in the delivery of more biologically active DOX to tumors with a concomitant increase in potency and efficacy over that which could be achieved with either unconjugated DOX or BR64-SS-DOx conjugate. Expand
Monoclonal antibody mediated intracellular targeting of tallysomycin S(10b).
TLDR
This method provides a novel approach for increasing the potency and therapeutic index of nominally moderately-active cytotoxic agents by conjugated to the internalizing antibody BR96. Expand
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] as α7 Nicotinic Receptor Agonists.
TLDR
Two potent and selective α7 nAChR partial agonists improved cognition in a preclinical rodent model of learning and memory and suggested the presence of a steric site that when engaged led to significant loss of affinity at that receptor. Expand
BR96 conjugates of highly potent anthracyclines.
TLDR
The 6-maleimidocaproylhydrazone derivatives of highly potent antitumor agents 5-Diacetoxypentyldoxorubicin and MorpholinodoxorubICin were synthesized and conjugated to monoclonal antibody BR96 and control IgG and demonstrated highly potent and antigen specific in vitro. Expand
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
TLDR
A series of conformationally restricted homotryptamines has been synthesized and shown to be potent inhibitors of hSERT, and preferred cyclopentane ring stereochemistry in both series was cis. Expand
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.
TLDR
The present studies have identified a series of diaminopyrimidines and diam inopyridines as novel 5-HT(7) receptor ligands and show clearly the structure-activity relationship with position of ring nitrogens. Expand
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