Chemical probes
Progress in the development of non-BET bromodomain chemical probes
... Homologous bromodomains BAZ2A/B belong to the BAZ family of proteins, which are ubiquitously expressed. Little is known about the biological roles of the BAZ family, therefore, the development of chemical ...
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Insights into 6 methylsalicylic acid bio assembly by using chemical probes
... Abstract: Chemical probes capable of reacting with KS (ketosynthase)-bound biosynthetic intermediates were utilized for the investigation of the model type I iterative polyketide synthase 6-methylsalicylic ...
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Novel chemical probes for the investigation of nonribosomal peptide assembly
... An overview of echinomycin putative intermediates captured from S. lasaliensis ACP12 (S970A) via the newly devised chemical probes is given in Table 1 and Fig. 2. A whole range of captured species spanning ...
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Donated chemical probes for open science.
... generate chemical probes, but to develop new drugs, not all donated probes have been profiled to the same depth that is required of a high-quality chemical ...pharma-donated probes have ...
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Target Abundance-Based Fitness Screening (TAFiS) Facilitates Rapid Identification of Target-Specific and Physiologically Active Chemical Probes
... relevant chemical- target ...relevant chemical probes that functionally interact with the selected target protein from a single primary ...on-target chemical probes (6, 23, 24), each ...
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Labelled chemical probes for demonstrating direct target engagement in living systems.
... labelled chemical probes have a major place in drug discovery, there are differences regarding their design and ...the chemical biology ...The Chemical Probes Portal [12] and Probe ...
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Chemical probes for the functionalization of polyketide intermediates
... functionalized chemical probes 3–13 constitute first-hand chemical biology tools for exploring novel polyketide diversification by providing direct informa- tion on PKSs tolerance and processing of ...
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Objective, Quantitative, Data-Driven Assessment of Chemical Probes.
... This work was primarily supported through the People Programme (Marie Curie Actions) of the 7th Framework Programme of the European Union (FP7/2007-2013) under REA grant agreement no. 600388 (TECNIOspring programme); the ...
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Computational Design and Fabrication of Optical Fibre Fluorescent Chemical Probes for the Detection of Cocaine
... In the evaluation of the probes produced, fluorescence emis- sion spectra were obtained and recorded. Light from a LED (375 nm centre wavelength) was coupled through a multimode fibre with good UV/visible spectral ...
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Recent advances in the development of synthetic chemical probes for glycosidase enzymes
... of chemical substrates that have been developed for the detection of glycosidase ...develop probes suitable as tools for medical diagnostics and drug ...
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Design and synthesis of chemical probes for the protein kinase B PH domain
... (-)-70 (Scheme 4.13). The 1-phosphonate (-)-133 was synthesised using the same conditions as outlined above. As with the synthesis of the racemic phosphonate, purification of the intermediate again proved difficult. Pure ...
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Design and synthesis of chemical probes for the plekstrin homology domain
... Another important example of this recognition is of phosphotyrosine pTyr residues with Src homology 2 SH2 and pTyr binding PTB domains, and is the target of a many inhibitors bearing iso[r] ...
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canSAR: update to the cancer translational research and drug discovery knowledgebase.
... objective chemical probe assessment plat- form which applies assessment of probe fitness factors to all compounds in canSAR, and ranks these compounds for their suitability to be used as chemical ...
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Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology.
... concerning chemical probes are usu- ally published in specialist chemical biology journals for which the readership mainly comprises experts already well aware of the issues and current best practice ...
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Second generation probes for biosynthetic intermediate capture : towards a comprehensive profiling of polyketide assembly
... of chemical probes ...by chemical probes 5–8: these interfere with the normal biosynthetic pathway (A) and undergo compe- titive decarboxylative Claisen condensation with KS-bound ...
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The pharmacological regulation of cellular mitophagy
... We are therefore optimistic that the review of the pharmacological modulation of mitophagy provided here may draw attention to the need for new, specific modulators of mitophagy and facilitate discussion within the field ...
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Rational design of small molecule probes for investigating the mechanism of action of the chemotherapeutic agents CDDO and artemisinin
... A chemical synthesis of tetraoxane probes that contain a UV chromophore was performed and analogues were subsequently screened for antimalarial ...as chemical probes and standards for ...
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Small molecules and their roles in effective pre-clinical target validation
... As demonstrated in multiple historical analyses, there are two main causes of clinical attrition; firstly drugs are not efficacious, and secondly they cause unacceptable toxicity, both of which can be the result of poor ...
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How Probes Work
... of Probes involving serious, effortful accomplishment, rather than being a mere distribution and collection exercise, resonates with other methodological issues concerning how we go about tapping into other ...
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Molecular Probes in Tandem Electrospray Ionization Mass Spectrometry: Application to Tracing Chemical Changes of Specific Phospholipid Molecular Species
... molecular probes, M1 and M2 (such as 3 and 4), give different product ion mass-to-charge ratio (m/z), p1 and p2, respectively, the parent ion scan mode at p1 should give a signal of M1 at m/z p1 with strict ...
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