Academic literature on the topic 'Click-chemistry based activity probe'

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Journal articles on the topic "Click-chemistry based activity probe"

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Luijkx, Yvette M. C. A., Seino Jongkees, Karin Strijbis, and Tom Wennekes. "Development of a 1,2-difluorofucoside activity-based probe for profiling GH29 fucosidases." Organic & Biomolecular Chemistry 19, no. 13 (2021): 2968–77. http://dx.doi.org/10.1039/d1ob00054c.

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Bell, Jessica L., Andrew J. Haak, Susan M. Wade, Yihan Sun, Richard R. Neubig, and Scott D. Larsen. "Design and synthesis of tag-free photoprobes for the identification of the molecular target for CCG-1423, a novel inhibitor of the Rho/MKL1/SRF signaling pathway." Beilstein Journal of Organic Chemistry 9 (May 21, 2013): 966–73. http://dx.doi.org/10.3762/bjoc.9.111.

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CCG-1423 and related analogues represent a new class of inhibitors of Rho/MKL1/SRF-mediated gene transcription, a pathway that has been implicated in both cancer and fibrosis. The molecular target for these compounds is unknown. To facilitate its identification, a series of tag-free photoaffinity probes was designed and synthesized, each one containing a photoactivatable group and an acetylenic end group for subsequent attachment to a fluorescent tag using click chemistry. All were confirmed to maintain biological activity in a cell-based assay for inhibition of SRE-Luc expression. The functio
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Ismail, Hanafy M., Victoria Barton, Matthew Phanchana, et al. "Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7." Proceedings of the National Academy of Sciences 113, no. 8 (2016): 2080–85. http://dx.doi.org/10.1073/pnas.1600459113.

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The artemisinin (ART)-based antimalarials have contributed significantly to reducing global malaria deaths over the past decade, but we still do not know how they kill parasites. To gain greater insight into the potential mechanisms of ART drug action, we developed a suite of ART activity-based protein profiling probes to identify parasite protein drug targets in situ. Probes were designed to retain biological activity and alkylate the molecular target(s) of Plasmodium falciparum 3D7 parasites in situ. Proteins tagged with the ART probe can then be isolated using click chemistry before identif
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Chen, Guilin, Hui Feng, Wenbin Xi, Jing Xu, Saifei Pan, and Zhaosheng Qian. "Thiol–ene click reaction-induced fluorescence enhancement by altering the radiative rate for assaying butyrylcholinesterase activity." Analyst 144, no. 2 (2019): 559–66. http://dx.doi.org/10.1039/c8an01808a.

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Yan, Xiaowen, Yacui Luo, Zhubao Zhang, et al. "Europium-Labeled Activity-Based Probe through Click Chemistry: Absolute Serine Protease Quantification Using 153Eu Isotope Dilution ICP/MS." Angewandte Chemie 124, no. 14 (2012): 3414–19. http://dx.doi.org/10.1002/ange.201108277.

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Yan, Xiaowen, Yacui Luo, Zhubao Zhang, et al. "Europium-Labeled Activity-Based Probe through Click Chemistry: Absolute Serine Protease Quantification Using 153Eu Isotope Dilution ICP/MS." Angewandte Chemie International Edition 51, no. 14 (2012): 3358–63. http://dx.doi.org/10.1002/anie.201108277.

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Yao, Tingting, Xiaowei Xu, and Rong Huang. "Recent Advances about the Applications of Click Reaction in Chemical Proteomics." Molecules 26, no. 17 (2021): 5368. http://dx.doi.org/10.3390/molecules26175368.

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Despite significant advances in biological and analytical approaches, a comprehensive portrait of the proteome and its dynamic interactions and modifications remains a challenging goal. Chemical proteomics is a growing area of chemical biology that seeks to design small molecule probes to elucidate protein composition, distribution, and relevant physiological and pharmacological functions. Click chemistry focuses on the development of new combinatorial chemical methods for carbon heteroatom bond (C-X-C) synthesis, which have been utilized extensively in the field of chemical proteomics. Click
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Lin, Vivian S. "Interrogating Plant-Microbe Interactions with Chemical Tools: Click Chemistry Reagents for Metabolic Labeling and Activity-Based Probes." Molecules 26, no. 1 (2021): 243. http://dx.doi.org/10.3390/molecules26010243.

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Continued expansion of the chemical biology toolbox presents many new and diverse opportunities to interrogate the fundamental molecular mechanisms driving complex plant–microbe interactions. This review will examine metabolic labeling with click chemistry reagents and activity-based probes for investigating the impacts of plant-associated microbes on plant growth, metabolism, and immune responses. While the majority of the studies reviewed here used chemical biology approaches to examine the effects of pathogens on plants, chemical biology will also be invaluable in future efforts to investig
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Tyler, Dean S., Johanna Vappiani, Tatiana Cañeque, et al. "Click chemistry enables preclinical evaluation of targeted epigenetic therapies." Science 356, no. 6345 (2017): 1397–401. http://dx.doi.org/10.1126/science.aal2066.

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The success of new therapies hinges on our ability to understand their molecular and cellular mechanisms of action. We modified BET bromodomain inhibitors, an epigenetic-based therapy, to create functionally conserved compounds that are amenable to click chemistry and can be used as molecular probes in vitro and in vivo. We used click proteomics and click sequencing to explore the gene regulatory function of BRD4 (bromodomain containing protein 4) and the transcriptional changes induced by BET inhibitors. In our studies of mouse models of acute leukemia, we used high-resolution microscopy and
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Serim, Sevnur, Susanne V. Mayer, and Steven H. L. Verhelst. "Tuning activity-based probe selectivity for serine proteases by on-resin ‘click’ construction of peptide diphenyl phosphonates." Organic & Biomolecular Chemistry 11, no. 34 (2013): 5714. http://dx.doi.org/10.1039/c3ob40907d.

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Dissertations / Theses on the topic "Click-chemistry based activity probe"

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Couvertier, Shalise Monique. "Chemical-proteomic strategies to study cysteine posttranslational modifications." Thesis, Boston College, 2016. http://hdl.handle.net/2345/bc-ir:107200.

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Thesis advisor: Eranthie Weerapana<br>Cysteine residues on proteins play important catalytic and regulatory roles in complex proteomes. These functional residues can be modified under physiological conditions by posttranslational modifications (PTMs) to regulate protein activities and modulate cysteine reactivity. Many PTMs are highly labile and dynamic, rendering it difficult to detect modified proteins within complex systems. To contribute to the chemical-proteomic methods currently available, chemical probe-Mass Spectrometry (MS) platforms were developed to study oxidative cysteine modifica
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Kumar, Lalit. "DEVELOPMENT OF NOVEL CHEMICAL TOOLS FOR PROTEASOME BIOLOGY & A NEW APPROACH TO 1-AZASPIROCYCLIC RING SYSTEM." UKnowledge, 2012. http://uknowledge.uky.edu/chemistry_etds/14.

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The proteasome, a multiprotease complex, is clinically validated as an anticancer target by the FDA approval of bortezomib and carfilzomib for the treatment of multiple myeloma. The emergence of resistance to proteasome inhibitors however remains a major clinical challenge. Recently, distinct types of proteasomes termed ‘intermediate proteasomes’, which contain unconventional mixtures of catalytic subunits, have been implicated with drug resistance of tumor cells. In elucidating the role of intermediate proteasomes in drug resistance, a crucial step is to unequivocally determine the subunit co
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Coover, Robert A. "Development of Irreversible Substrate Competitive Probes for PKA Activity." VCU Scholars Compass, 2015. http://scholarscompass.vcu.edu/etd/3907.

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The current environment for drug discovery and disease treatment relies heavily on genomic analysis, structural biology and chemical biology techniques. With the enormous advances in genomic analysis and structural biology, the use of and desire for targeted therapies has increased. However, as more genomic data for cancer disease state pathology becomes available we must ask increasingly difficult questions and even produce new technologies, such as activity-based probes, to answer these questions. In particular, targeted kinase inhibitors for the treatment of cancer has become a mainstay for
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O'Byrne, Sean. "Adaptation of BODIPY dyes to investigate drug delivery and develop 'self-reporting' activity-based probes." Thesis, University of Glasgow, 2018. http://theses.gla.ac.uk/9035/.

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The work presented within adapts BODIPY fluorescent dyes for two distinct purposes: to investigate drug delivery into parasites and to develop ‘self-reporting’ activity-based probes for protein profiling. Methods for the treatment of parasitic diseases (human, animal and plant) have recently focussed on techniques for improving the delivery of a drug into the host infected cell, followed by its subsequent uptake into the parasite. In an effort to develop new anti-parasitic agents, a new system was developed, that is able to deliver low molecular weight units, as well as larger biomolecules (13
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Charoensutthivarakul, Sitthivut. "From medicinal chemistry optimisation of antimalarial 2-aryl quinolones to synthesis and application of endoperoxide activity-based protein profiling probes." Thesis, University of Liverpool, 2014. http://livrepository.liverpool.ac.uk/2006416/.

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Malaria is one of the most prevalent and deadliest parasitic diseases affecting various systems of the body and leading to death. Resistance against antimalarial treatment is a major threat in controlling and eliminating malaria. New drugs are urgently needed especially when artemisinin resistance has emerged. The mitochondrial electron transport chain of Plasmodium falciparum is an attractive target for chemotherapy. Two enzymes in the pathway - Pfbc1 and PfNDH2 - are druggable target enzymes. The dual inhibition of both enzymes can be seen in 2-aryl quinolone pharmacophore giving added thera
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Kambafwile, Henry Kunda. "Synthesis of activity-based protein profiling probes for malaria and hypertension disease models & potential novel ACE inhibitors with an attenuated zinc binding group." Doctoral thesis, University of Cape Town, 2012. http://hdl.handle.net/11427/11736.

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Includes bibliographical references.<br>Angiotensin-converting enzyme (ACE) and P. falciparum A M1 (PfA-M1) are both zinc metalloproteases implicated in hypertension and malaria, respectively. Hypertension affects approximately 26 % of the world’s population while each year over 300 million cases of malaria occur worldwide resulting in between 1.5 and 2.7 million deaths annually. Hypertension treatment with current ACE inhibitors is marred by unpleasant side effects, such as cough and angioedema. In malaria, the parasites continuously develop resistance to anti-malarial drugs where the disease
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Trabbic, Christopher J. "Chemoenzymatic Synthesis of NAADP Derivatives: Probing the Unknown NAADP Receptor." University of Toledo Health Science Campus / OhioLINK, 2012. http://rave.ohiolink.edu/etdc/view?acc_num=mco1333749803.

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Salaam, Jeremy. "Sondes magnetogènes à base de Fe(II) répondantes à un analyte chimique par changement de spin électronique." Thesis, Lyon, 2020. http://www.theses.fr/2020LYSEN075.

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Cette thèse traite de molécules à base de Fe(II) capables d’un passage de spin sous l’action d’un analyte en solution, utilisées dans le domaine de l’imagerie moléculaire, notamment l’IRM (Imagerie par Résonance Magnétique). Depuis plusieurs années, la communauté scientifique autour de l’IRM a pris conscience de deux problématiques importantes : la faible sensibilité de l’IRM et la toxicité des agents de contrastes utilisés pour l’améliorer. Notre équipe répond à ces deux problématiques en développant des sondes magnétogènes spécifiques à un analyte biologique et supposées moins toxiques. Dans
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Wang, Yun 1981. "Controlling nitric oxide (NO) overproduction : N[omega], N[omega]-dimethylarginine dimethylaminohydrolase (DDAH) as a novel drug target." 2010. http://hdl.handle.net/2152/14048.

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Nitric oxide (NO) overproduction is correlated with numerous human diseases, such as arthritis, asthma, diabetes, inflammation and septic shock. The enzyme activities of both NO synthase (NOS) and dimethylarginine dimethylaminohydrolase-1 (DDAH-1) promote NO production. DDAH-1 mainly colocalizes in the same tissues as the neuronal isoform of NOS and catabolizes the endogenously-produced competitive inhibitors of NOS, N[omega]-monomethyl-L-arginine (NMMA) and asymmetric N[omega], N[omega]-dimethyl-L-arginine (ADMA). Inhibition of DDAH-1 leads to elevated concentrations of NMMA and ADMA, which s
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Book chapters on the topic "Click-chemistry based activity probe"

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Willetts, David. "The Research-Intensive University." In A University Education. Oxford University Press, 2017. http://dx.doi.org/10.1093/oso/9780198767268.003.0009.

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Professor Liebig of Giessen University is looking back with pride on his career in organic chemistry and his keen young team of researchers in their lab ‘almost exclusively devoted to the improvement of organic analysis . . . The only complaints were those of the attendant who in the evenings, when he had to clean, could not get the workers to leave the laboratory.’ All quite typical—except that he is describing a laboratory he created in 1826. It was the first research laboratory based in a university. There were a few other laboratories but they were usually sponsored by learned societies (you can still see Michael Faraday’s laboratory at the Royal Institution) and were nothing to do with universities. Professor Liebig knew the significance of what he was doing: ‘there began at the small university an activity such as the world had not yet seen’. It was the birth of one of the most important institutions of the modern world—the research-based university systematically creating new knowledge—and it was conceived in Germany, as we saw in Chapter One. Wilhelm von Humboldt wrote a short policy paper which proved to be one of the seminal documents in the emergence of the modern university, proposing that the university should become a centre of research. Underneath the idealist Hegelian prose he wrestles with issues which are still live today. He argues that research based in the university is enhanced by teaching, compared with the alternative model of research in a separate academy: . . . If one declares the university as destined only for the teaching and dissemination of science, but the academy to its expansion, one clearly does the former an injustice. Surely, the sciences have been just as much—and in Germany more so—expanded by university professors as by the academy members, and these men have arrived at their advances in their field precisely through their teaching. For the free oral lecture before listeners, among whom there is always a significant number of minds that think along for themselves, surely spurs on the person who has become used to this kind of study as much as the solitary leisure of the writer’s life or the loose association of an academic fellowship. . . .
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Conference papers on the topic "Click-chemistry based activity probe"

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Mangold, Martin, Michael Gütschow, and Marit Stirnberg. "A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2." In 3rd International Electronic Conference on Medicinal Chemistry. MDPI, 2017. http://dx.doi.org/10.3390/ecmc-3-04705.

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Gütschow, Michael, and Daniela Häußler. "Aminophosphonates as Novel Activity-Based Probes for Matriptase-2 ." In 1st International Electronic Conference on Medicinal Chemistry. MDPI, 2015. http://dx.doi.org/10.3390/ecmc-1-a041.

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