A5010306517- Chemical Synthesis and Analysis
- Receptor Mechanisms and Signaling
- Monoclonal and Polyclonal Antibodies Research
- Click Chemistry and Applications
- HIV/AIDS drug development and treatment
- Silk-based biomaterials and applications
- RNA Interference and Gene Delivery
- Antimicrobial Peptides and Activities
- HIV Research and Treatment
- Regulation of Appetite and Obesity
- Biochemical Analysis and Sensing Techniques
- Molecular Junctions and Nanostructures
- Neuropeptides and Animal Physiology
- Peptidase Inhibition and Analysis
- Mass Spectrometry Techniques and Applications
- Analytical Chemistry and Chromatography
- Innovative Microfluidic and Catalytic Techniques Innovation
- Biochemical and Structural Characterization
Kyoto Pharmaceutical University
2018
University of Arizona
2007-2011
Current cancer therapies exploit either differential metabolism or targeting to specific individual gene products that are overexpressed in aberrant cells. The work described herein proposes an alternative approach--to specifically target combinations of cell-surface receptors using heteromultivalent ligands ("receptor combination approach"). As a proof-of-concept functionally unrelated can be noncovalently cross-linked with high avidity and specificity, series heterobivalent (htBVLs) were...
We demonstrate the potential utility of multivalent ligands as targeting agents for cancer imaging or therapy by determining binding homobivalent to their corresponding receptors. This manuscript details synthesis and evaluation a series bivalent containing two copies truncated heptapeptide version [Nle4-d-Phe7]-α-melanocyte stimulating hormone (NDP-α-MSH), referred MSH(7). These were connected with various semirigid linkers Pro-Gly repeats, without flexible poly(ethylene glycol) (PEGO)...
The emergence of drug-resistant HIV from a widespread antiviral chemotherapy targeting protease in the past decades is unavoidable and provides challenge to develop alternative inhibitors. We synthesized series allophenylnorstatine-based peptidomimetics with various P3, P2, P2́ moieties. derivatives P2 tetrahydrofuranylglycine (Thfg) were found be potent against wild type HIV-1 virus, leading highly compound 21f (KNI-1657) lopinavir/ritonavir- or darunavir-resistant strains. Co-crystal...
A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used to connect two high affinity NDP-α-MSH ligands or low MSH(4) ligands. The incorporated into the conjugate by solid-phase synthesis. In vitro biological evaluations showed potency of binding human melanocortin 4 receptor not diminished for linker−ligand combinations relative corresponding ligand alone.
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionORIGINAL ARTICLEThis notice is a correctionDesign, Synthesis, and Validation of Branched Flexible Linker for Bioactive Peptides.Martina E. Bowen, Yasunari Monguchi, Rajesh Sankaranarayanan, Josef Vagner, Lucinda J. Begay, Liping Xu, Bhumasamudram Jagadish, Victor Hruby, Robert Gillies, Eugene A. MashCite this: Org. Chem. 2007, 72, 9, 3608Publication Date (Web):March 27, 2007Publication History Published online27 March 2007Published inissue...