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Showing 1 to 19 of 19 for “"photoaffinity labeling"”.
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Azido Auxins: Synthesis and Use as Photoaffinity Labeling Agents
… synthesized by Dr. Lee Melhado to be used as photoaffinity labeling agents in plants. The analogs, 4-, 5-, and 6-azidoindole-3-acetic acid, were prepared in seven steps with overall yields of 2-20%. The nonfluorescent analogs are stable in the dark but degrade to fluorescent products upon …
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Estrogens Containing Conjugated Ketones: Synthesis and Photoaffinity Labeling Studies
Made available in DSpace on 2014-12-13T20:10:16Z (GMT). No. of bitstreams: 1 7804096.pdf: 5550891 bytes, checksum: 09fff2caaefbe40c404b4257e219d6f1 (MD5) Previous issue date: 1977
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Photoaffinity Labeling of the Estrogen Binding Protein From Immature Rat Uterus
Made available in DSpace on 2014-12-10T23:01:57Z (GMT). No. of bitstreams: 1 7500380.pdf: 4995188 bytes, checksum: 4d2ab07238c52d71ecfe79c5614c0304 (MD5) Previous issue date: 1974
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Photoaffinity labeling the nucleotide sites of the sarcoplasmic reticulum Ca²⁺-ATPase
We have synthesized a new class of photoaffinity analogs, 2',3'-O-(2,4,6-trinitrophenyl)-8-azido-ATP, -ADP and -AMP (TNP- 8N₃ATP, -ADP and -AMP), and their radiolabeled derivatives, and characterized their interaction with the sarcoplasmic reticulum Ca²⁺-ATPase. The TNP-8N₃-nucleotides were …
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Exploring The Ligand Binding Site On The Dopamine Transporter By Photoaffinity Labeling And Site-Directed Mutagenesis
<p>The dopamine transporter (DAT) is a neuronal presynaptic transmembrane protein that clears released dopamine (DA) from the synaptic space, regulating the neurotransmitter concentration and availability, DAT and the related serotonin (SERT) and norepinephrine (NET) transporters belong to the SLC6 …
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Design, synthesis, and biochemical evaluation of novel photoaffinity labeling reagents for the estrogen and progesterone receptors
… (TFAA) 1 and its protio analogue (PAA) 2, both photoaffinity labeling (PAL) reagents for the estrogen receptor (ER), have been prepared by direct coupling of the appropriately substituted 4-azidobenzoyl chloride with the electron rich C-3 of 2-(4-methoxyphenyl)-6-methoxybenzo (b) thiophene 6. …
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Monoamine Transporter Photoaffinity Ligands Based On Methylphenidate and Citalopram: Rational Design, Chemical Synthesis, and Biochemical Application
… of a "Binding Ensemble Profiling with (f)Photoaffinity Labeling (BEProFL)" experimental approach. Specifically, BEProFL rationally couples photoaffinity labeling, chemical proteomics, and computational molecular modeling in order to map the binding sites and poses of ligands within their …
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Part One: Iodinated Estrogens - Potential Photoaffinity Labeling and Tumor Localizing Agents for Estrogen Responsive Tissues. Part Two: Synthesis of a Hexestrol Derivative for Potential Use in Affinity Chromatography to Purify Estrogen Receptors
Made available in DSpace on 2014-12-13T20:09:38Z (GMT). No. of bitstreams: 1 7606804.pdf: 4754811 bytes, checksum: 5e28e9583b4f5a10e05d7cff564649b7 (MD5) Previous issue date: 1975
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Dopamine Transporter (DAT), Nicotinic Acetylcholine Receptor (nAChR), and Metabotropic Glutamate Receptor 2 (mGlu2) Irreversible Probes For Identifying Anti-Psychostimulant Therapeutics
… of a "Binding Ensemble Profiling with (f)Photoaffinity Labeling (BEProFL)" experimental approach. BEProFL rationally couples photoaffinity labeling, chemical proteomics, and computational molecular modeling to allow structure-function studies of the target proteins. This central hypothesis …
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Synthesis of Functional Analogs of Non-Steroidal Estrogens
… achieved for estrogens bearing aryl iodides. For photoaffinity labeling studies of the estrogen receptor, a new photoreactive ligand, 1-(4'-hydroxyphenyl)-2-(2'-nitro-4'-methoxyphenyl)butane, was prepared by total synthesis (nine steps). This compound exhibited a low relative binding affinity for …
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Toward High-throughput, Quantitative Platforms to Identify the Targets of Small Molecules
… chemical method can be used to quickly generate photoaffinity labeling analogs of small molecules that can be used in a covalent ELISA and mass spectrometry workflow to determine whether small molecules bind to a target of interest and identify off-target binders. Additionally, we created a …
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Photochemistry of 5-Membered Heteroaryl(trifluoromethyl)carbenes in Low Temperature Matrices
… diazirines might add to the possibility of new photoaffinity labeling agents.
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Shedding Light On General Anesthesia: Uncovering The Molecular Mechanisms For Propofol And Volatile Anesthetics
… in chemical and molecular biology, including photoaffinity labeling, have allowed enhanced appreciation of the complex interactions anesthetic’s have with their macromolecular substrates. This work is dedicated to further define the protein interactions of the frequently administered volatile …
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Characterization of resistance to halogenated aromatic hydrocarbons in a population of Fundulus heteroclitus from a marine superfund site
… NBH F1 fish. Hepatic AhR content, as measured by photoaffinity labeling with 125I-N3Br2DD, was lower in NBH fish than in SC fish and lower in males than in females. After 90 days in captivity, the sex difference persisted, but the site difference did not. TCDF induced hepatic AIIR content in NBH …
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Structural Determinants for Inhibitor Recognition by the Dopamine Transporter
The dissertation will give an introduction, background and our research progress in the areas of dopamine transporter (DAT). A 3-D DAT computer model was generated in our laboratory based on the X-ray crystal structure of the bacterial leucine transporter LeuT, a distant homolog of DAT. The ability …
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Attempted Synthesis of a Photoreactive Geranylcysteine Derivative.
<p>In an attempt to synthesize a photoreactive geranylcysteine derivative, <b>A</b>, with an appropriate photoprobe to be studied as a mimic for farnesylated protein, <b>B</b>, the following syntheses were carried out. The hydroxyl group of geraniol was protected with DHP/PPTs to generate <b>1</b> …
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Purification and characterisation of plasmodium falciparum Hypoxanthine phosphoribosyltransferase
Malaria remains the most important parasitic disease worldwide. It is estimated that over 500 million infections and more that 2.7 million deaths arising from malaria occur each year. Most (90%) of the infections occur in Africa with the most affected groups being children of less than five years …