Bioconjugate Chemistry
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#1Marco BassettoH-Index: 1
#2Merve Sen (University of Tübingen)H-Index: 2
Last. Olivier ZelphatiH-Index: 14
view all 8 authors...
The prevalence of retinal disorders associated with visual impairment and blindness is increasing worldwide, while most of them remain without effective treatment. Pharmacological and molecular therapy development is hampered by the lack of effective drug delivery into the posterior segment of the eye. Among molecular approaches, RNA-interference (RNAi) features strong advantages, yet delivering it to the inner layer of the retina appears extremely challenging. To address this, we developed an o...
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#1Rodell C. Barrientos (WRAIR: Walter Reed Army Institute of Research)H-Index: 5
#2Connor Whalen (WRAIR: Walter Reed Army Institute of Research)H-Index: 1
Last. Gary R. Matyas (WRAIR: Walter Reed Army Institute of Research)H-Index: 31
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Opioid use disorders and fatal overdose due to consumption of fentanyl-laced heroin remain a major public health menace in the United States. Vaccination may serve as a promising potential remedy to combat accidental overdose and to mitigate the abuse potential of opioids. We previously reported the heroin and fentanyl monovalent vaccines carrying, respectively, a heroin hapten, 6-AmHap, and a fentanyl hapten, para-AmFenHap, conjugated to tetanus toxoid (TT). Herein, we describe the mixing of th...
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#1Mareile Boschanski (Bielefeld University)H-Index: 3
#2Tobias Krüger (Bielefeld University)H-Index: 3
Last. Thomas Dierks (Bielefeld University)H-Index: 45
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Multiple, site-specific protein conjugation is increasingly attractive for the generation of antibody-drug conjugates (ADCs). As it is important to control the number and position of cargoes in an ADC, position-selective generation of reactive sites in the protein of interest is required. Formylglycine (FGly) residues are generated by enzymatic conversion of cysteine residues embedded in a certain amino acid sequence motif with a formylglycine-generating enzyme (FGE). The addition of copper ions...
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#1Amaury Guillou (UZH: University of Zurich)H-Index: 2
#2Daniel F. Earley (UZH: University of Zurich)H-Index: 1
Last. Jason P. Holland (UZH: University of Zurich)H-Index: 30
view all 7 authors...
Most experimental work in the space of bioconjugation chemistry focuses on using new methods to construct covalent bonds between a cargo molecule and a protein of interest such as a monoclonal antibody (mAb). Bond formation is important for generating new diagnostic tools, yet when these compounds advance to preclinical in vitro and in vivo studies, and later for translation to the clinic, understanding the fate of potential metabolites that arise from chemical or enzymatic degradation of the co...
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#1Gyudong Lee (POSTECH: Pohang University of Science and Technology)H-Index: 1
#2Jaejung Song (POSTECH: Pohang University of Science and Technology)H-Index: 12
Last. Sungjee Kim (POSTECH: Pohang University of Science and Technology)H-Index: 48
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This paper demonstrates fabrication of silica-shell-coated magnetic nanoparticle clusters (SMNCs) and subsequent surface engineering of SMNCs to produce surface-modified SMNCs that have zwitterionic and primary amine ligands (SMNC-ZW/Am). SMNC-ZW/Am was passivated by zwitterionic ligands for improved colloidal stability and reduced nonspecific adsorption and by primary amine ligands for facilitated conjugation with biomolecules. Hydrodynamic (HD) size and zeta potential of SMNC-ZW/Am could be fl...
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#1Sam J. Moons (Radboud University Nijmegen)H-Index: 5
#2Emiel Rossing (Radboud University Nijmegen)H-Index: 2
Last. Thomas J. Boltje (Radboud University Nijmegen)H-Index: 17
view all 9 authors...
Bacterial pathogens such as Nontypeable Haemophilus influenzae (NTHi) can evade the immune system by taking up and presenting host-derived sialic acids. Herein, we report a detailed structure-activity relationship of sialic acid-based inhibitors that prevent the transfer of host sialic acids to NTHi. We report the synthesis and biological evaluation of C-5, C-8, and C-9 derivatives of the parent compound 3-fluorosialic acid (SiaNFAc). Small modifications are tolerated at the C-5 and C-9 position...
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#1Diogo A. Mendonça (IMM: Instituto de Medicina Molecular)H-Index: 2
#2Mariët Bakker (Avans University of Applied Sciences)
Last. Toni Todorovski (UPF: Pompeu Fabra University)H-Index: 2
view all 12 authors...
Passing through the blood-brain barrier (BBB) to treat neurological conditions is one of the main hurdles in modern medicine. Many drugs with promising in vitro profiles become ineffective in vivo due to BBB restrictive permeability. In particular, this includes drugs such as antiviral porphyrins, with the ability to fight brain-resident viruses causing diseases such as HIV-associated neurocognitive disorders (HAND). In the last two decades, BBB shuttles, particularly peptide-based ones, have sh...
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#1Asma Rahali (UAM: Autonomous University of Madrid)
#2Ahmed Shaukat (Aalto University)H-Index: 3
Last. Eduardo Anaya-Plaza (Aalto University)H-Index: 7
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Design and synthesis of novel photosensitizer architectures is a key step toward new multifunctional molecular materials. Photoactive Janus-type molecules provide interesting building blocks for such systems by presenting two well-defined chemical functionalities that can be utilized orthogonally. Herein a multifunctional phthalocyanine is reported, bearing a bulky and positively charged moiety that hinders their aggregation while providing the ability to adhere on DNA origami nanostructures via...
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#1Pan Liu (SUES: Shanghai University of Engineering Sciences)
#2Le Wang (SUES: Shanghai University of Engineering Sciences)H-Index: 4
Last. Xiangyang Shi (Donghua University)H-Index: 87
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A cyclotriphosphazene-based "butterfly" fluorescence probe HCCP-MNI bearing two naphthalimide and morpholine units were developed for lysosome targeting. The synthesized HCCP-MNI exhibited stable fluorescence signals and was cytocompatible in the given concentration range. Co-localization experimental results showed that cells treated with the HCCP-MNI and a commercial dye (Lyso-Tracker Red DND-99) had overlapped fluorescence signals, demonstrating its targeting specificity to lysosomes. The dev...
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#1Wendy Yu (UPenn: University of Pennsylvania)
#2Kevin P. Gillespie (UPenn: University of Pennsylvania)H-Index: 4
Last. Andrew Tsourkas (UPenn: University of Pennsylvania)H-Index: 44
view all 8 authors...
Antibody-drug conjugates (ADCs) have demonstrated great therapeutic potential due to their ability to target the delivery of potent cytotoxins. However, the heterogeneous nature of conventional drug conjugation strategies can affect the safety, efficacy, and stability of ADCs. Site-specific conjugations can resolve these issues, but often require genetic modification of Immunoglobulin G (IgG), which can impact yield or cost of production, or require undesirable chemical linkages. Here, we descri...
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Top fields of study
Molecular biology
Chemistry
Conjugate
Combinatorial chemistry
Peptide
Biochemistry
Stereochemistry