87450-10-0Relevant academic research and scientific papers
Synthesis of Two-Photon Active Tricomponent Fluorescent Probe for Distinguishment of Biotin Receptor Positive and Negative Cells and Imaging 3D-Spheroid
Pal, Kaushik,Sharma, Aman,Koner, Apurba L.
, p. 6425 - 6429 (2018)
A fluorescence microscopy-based distinguishment between biotin receptor (BiR) positive and negative cell lines via receptor-mediated endocytosis has been demonstrated. A water-soluble, three-component, two-photon (2P) active solvatofluorochromic probe has been designed and synthesized. The applicability of the probe for 2P microscopy and 3D-spheroid was also assessed.
Designing Molecular Printboards: A Photolithographic Platform for Recodable Surfaces
Abt, Doris,Schmidt, Bernhard V. K. J.,Pop-Georgievski, Ognen,Quick, Alexander S.,Danilov, Denis,Kostina, Nina Yu.,Bruns, Michael,Wenzel, Wolfgang,Wegener, Martin,Rodriguez-Emmenegger, Cesar,Barner-Kowollik, Christopher
, p. 13186 - 13190 (2015)
A light induced strategy for the design of β-cyclodextrin (CD) based supramolecular devices is introduced, presenting a novel tool to fabricate multifunctional biointerfaces. Precision photolithography of a modified β-CD was established on a light sensiti
Development of PDT/PET Theranostics: Synthesis and Biological Evaluation of an 18F-Radiolabeled Water-Soluble Porphyrin
Entract, Guy M.,Bryden, Francesca,Domarkas, Juozas,Savoie, Huguette,Allott, Louis,Archibald, Stephen J.,Cawthorne, Chris,Boyle, Ross W.
, p. 4414 - 4423 (2015)
Synthesis of the first water-soluble porphyrin radiolabeled with fluorine-18 is described: a new molecular theranostic agent which integrates the therapeutic selectivity of photodynamic therapy (PDT) with the imaging efficacy of positron emission tomograp
Clustering of PK-trisaccharides on amphiphilic cyclodextrin reveals unprecedented affinity for the Shiga-like toxin Stx2
Zhang, Ping,Paszkiewicz, Eugenia,Wang, Qifang,Sadowska, Joanna M.,Kitov, Pavel I.,Bundle, David R.,Ling, Chang-Chun
, p. 10528 - 10531 (2017)
Using amphiphilic cyclodextrin as a scaffold, the first class of PK-glycoconjugates capable of high avidity binding to both Stx1 and Stx2 toxins in solid-phase assay formats is reported. The generated glycomicroarray effectively mimics the plas
A bioorthogonal turn-on fluorescent strategy for the detection of lysine acetyltransferase activity
He, Maomao,Han, Zhen,Qiao, Jing,Ngo, Liza,Xiong, May P.,Zheng, Y. George
, p. 5594 - 5597 (2018)
Lysine acetylation plays vital roles in the regulation of fundamental cellular processes, which is mediated by lysine acetyltransferases (KATs). Developing chemical biology probes for KAT activity detection is of important value in providing improved understanding of their biological functions. We reported a panel of "turn-on" fluorescent probes for sensitive and selective detection of KAT enzymatic activity through a simple mix-and-read format. Combined with bioorthogonal substrate labelling and click chemistry, these probes produced strong "turn-on" fluorescent signals in response to KAT-mediated acylation process. This chemical biology strategy diversifies the assay toolboxes to investigate functions and mechanisms of acetyltransferase enzymes.
Facial Synthesis and Bioevaluation of Well‐Defined OEGylated Betulinic Acid‐Cyclodextrin Conjugates for Inhibition of Influenza Infection
Chen, Yingying,Gao, Qianqian,Liang, Shuobin,Ma, Xinyuan,Tretyakova, Elena V.,Wang, Xinchen,Xiao, Sulong,Zhang, Yongmin,Zhou, Demin
, (2022/02/19)
Betulinic acid (BA) and its derivatives exhibit a variety of biological activities, especially their anti‐HIV‐1 activity, but generally have only modest inhibitory potency against influenza virus. The entry of influenza virus into host cells can be competitively inhibited by multivalent derivatives targeting hemagglutinin. In this study, a series of hexa‐, hepta‐ and octavalent BA derivatives based on α-, β-and γ-cyclodextrin scaffolds, respectively, with varying lengths of flexible oligo(ethylene glycol) linkers was designed and synthesized using a microwave‐assisted copper‐catalyzed 1,3‐di-polar cycloaddition reaction. The generated BA‐cyclodextrin conjugates were tested for their in vitro activity against influenza A/WSN/33 (H1N1) virus and cytotoxicity. Among the tested com-pounds, 58, 80 and 82 showed slight cytotoxicity to Madin‐Darby canine kidney cells with viabilities ranging from 64 to 68% at a high concentration of 100 μM. Four conjugates 51 and 69–71 showed significant inhibitory effects on influenza infection with half maximal inhibitory concentration val-ues of 5.20, 9.82, 7.48 and 7.59 μM, respectively. The structure‐activity relationships of multivalent BA‐cyclodextrin conjugates were discussed, highlighting that multivalent BA derivatives may be potential antiviral agents against influenza infection.
Functionalized 2-Hydroxybenzaldehyde-PEG Modules as Portable Tags for the Engagement of Protein Lysine ?-Amino Groups
Sacco, Giovanni,Stammwitz, Simon,Belvisi, Laura,Pignataro, Luca,Dal Corso, Alberto,Gennari, Cesare
supporting information, p. 1763 - 1767 (2021/03/24)
The formation of reversible-covalent interactions between a small-molecule ligand and its protein target is emerging as a general strategy to design binders with increased affinity. In this context, 2-hydroxybenzaldehyde (2HB) has been recently proposed a
On-Nanoparticle Gating Units Render an Ordinary Catalyst Substrate- And Site-Selective
Kim, Minju,Dygas, Miroslaw,Sobolev, Yaroslav I.,Beker, Wiktor,Zhuang, Qiang,Klucznik, Tomasz,Ahumada, Guillermo,Ahumada, Juan Carlos,Grzybowski, Bartosz A.
supporting information, p. 1807 - 1815 (2021/02/05)
When an organometallic catalyst is tethered onto a nanoparticle and is embedded in a monolayer of longer ligands terminated in "gating"end-groups, these groups can control the access and orientation of the incoming substrates. In this way, a nonspecific catalyst can become enzyme-like: it can select only certain substrates from substrate mixtures and, quite remarkably, can also preorganize these substrates such that only some of their otherwise equivalent sites react. For a simple, copper-based click reaction catalyst and for gating ligands terminated in charged groups, both substrate- and site-selectivities are on the order of 100, which is all the more notable given the relative simplicity of the on-particle monolayers compared to the intricacy of enzymes' active sites. The strategy of self-assembling macromolecular, on-nanoparticle environments to enhance selectivities of "ordinary"catalysts presented here is extendable to other types of catalysts and gating based on electrostatics, hydrophobicity, and chirality, or the combinations of these effects. Rational design of such systems should be guided by theoretical models we also describe.
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INIDBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0151; 0152, (2021/02/05)
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
ANTIBODY-DRUG CONJUGATES COMPRISING ANTI-B7-H3 ANTIBODIES
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Page/Page column 106; 111-112, (2022/01/04)
The present disclosure relates to antibody-drug conjugates (ADCs) wherein one or more active agents are conjugated to an anti-B7-H3 antibody through a linker. The linker may comprise a unit that covalently links active agents to the antibody. The disclosure further relates to monoclonal antibodies and antigen binding fragments, variants, multimeric versions, or bispecifics thereof that specifically bind B7-H3, as well as methods of making and using these anti-B7-H3 antibodies and antigen-binding fragments thereof in a variety of therapeutic, diagnostic and prophylactic indications
