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Showing 1 to 20 of 22 for “"chemical probe"”.

  1. VHL inhibitors as chemical probes of the hypoxia signalling pathway

    Frost, JuliantyUniversity of Dundee2018

    … α remain to be elucidated. The development of a chemical probe that unambiguously blocks the VHL:HIF α interaction downstream of HIF α hydroxylation by prolyl hydroxylase domain (PHD) enzymes, would address biological questions about VHL molecular targets and functional consequences of disrupting …

    dundee Repository record

  2. Small-molecule approaches to interrogate the druggability of the VHL E3 Cullin RING Ubiquitin Ligase

    Soares, PedroUniversity of Dundee2018

    … in Nature and so are attractive targets for chemical biology and drug discovery. Modulating PPIs is challenging because of the nature of their interacting surfaces. Nevertheless, recent progress has led to the discovery of small molecule modulators of PPIs as chemical probes or lead compounds …

    dundee Repository record

  3. Roles of singlet oxygen and triplet excited state of dissolved organic matter formed by different organic matters in bacteriophage MS2 inactivation

    Rosado, SahidUniversity of Illinois at Urbana-Champaign2013

    … rate constants of 2,4,6-trimethylphenol (TMP), a probe compound that previously had been shown to react mainly with 3DOM*. Linear correlations between MS2 kobs and 1O2 concentrations were also found for both purified DOM isolates and natural water samples. These correlations, along with data from …

    uiuc Repository record

  4. High Throughput Screening for Small Molecule Interactions with Nucleic Acid Binding Proteins

    Wilson, Robert M.Massachusetts Institute of Technology2022

    … not only several starting points for chemical probe development, but also the fundamental chemical tractability of protein domains involved in RNA binding. Together, this work generates new chemical matter for inhibiting previously intractable targets and identifies a strategy for …

    mit Repository record

  5. Multiscale chemomechanics of polymer deformation under contact : predicting structure-property correlations from the bulk to the interphase

    Tweedie, Catherine AnneMassachusetts Institute of Technology2008

    … formation of a structural interphase region. Chemical probe functionalization experiments are developed to explore the effects of probe surface charge on the probe-polymer interface and contribute to the understanding of the interphase that dominates nanocomposite material response. A …

    mit Repository record

  6. Synthesis and evaluation of β-fluoro-γ-aminobutyric acid enantiomers

    Deniau, GildasUniversity of St Andrews2007

    … demonstrates that the C-F bond can be used as a chemical probe to reveal the binding conformation of a bioactive amine and this offers exciting prospects for future research. The synthesis of 3-fluoro-GABA from phenylalanine indicated that amino acids are practical starting materials for the …

    st-andrews Repository record

  7. Synthesis, Characterization, And Rna Reactivity Of Amino-Acid-Linked Cisplatin Analogues

    Bao, Xun2015

    … drug cisplatin was previously applied as a chemical probe of rRNA structure to determine solvent accessible purines (guanosine) in vivo and in vitro. Cisplatin accumulates faster on RNA than DNA, with less chance of repair. As such, designing new RNA-targeting Pt compounds is not only a …

    wayne-thes Repository record

  8. Modular synthesis-enabled mechanistic characterization of the potent antilipoperoxidant activity of peridinin

    Haley, Hannah M.University of Illinois at Urbana-Champaign2018

    … the utility of peridinin as a small molecule probe of the role of lipid peroxidation in pathogenesis, the mechanistic underpinnings of its antilipoperoxidant activity were investigated. Solid-state NMR experiments with a site-selectively 13C-labeled peridinin isotopologue revealed that the …

    uiuc Repository record

  9. Identification and Optimization of Small Molecule Binders for ALK2, USP5, and DCAF1

    Gonzalez Alvarez, Hector2024

    … compound 19 with the intent of generating a chemical probe to investigate the biology of DCAF1 in cells. Lastly, we outlined the optimization of an alternative chemical scaffold targeting the WDR domain of DCAF1. This thesis has enabled major advances in developing high quality binders for …

    toronto-retro Repository record

  10. Thermo-analytical and spectroscopic characterisation of pore lining minerals in reservoir rocks.

    Clegg, Francis.Sheffield Hallam University (United Kingdom).1998

    … The second method uses organic molecules as chemical probes to elucidate the surface mineralogy of reservoir rocks. Clay mineral standards which have been exposed to certain chemical probes and subsequently heated show desorption profiles (monitored by thermogravimetric analysis (TGA)) that …

    sheffield-hallam Repository record

  11. Dopamine Transporter (DAT) and Metabotropic Glutamate Receptor 5 (MGLU5) Irreversible Probes for Identifying Anti-Psychostimulant Therapeutics

    Velagaleti, Ranganadh2018

    … of this research was to develop irreversible chemical probes based on select DAT inhibitors and mGlu5 NAMs in order to map the corresponding binding sites and poses of these compounds within their major drug targets. The central hypothesis was that these compounds could be derivatized, without …

    duquesne Repository record

  12. Dopamine Transporter (DAT), Nicotinic Acetylcholine Receptor (nAChR), and Metabotropic Glutamate Receptor 2 (mGlu2) Irreversible Probes For Identifying Anti-Psychostimulant Therapeutics

    Aggarwal, Shaili2018

    … of this research was to develop irreversible chemical probes based on promising anti-addiction lead compounds (i.e., pyrovalerone, bupropion, BINA, etc) to map their binding sites and poses within the DAT, select nAChR subtypes, or mGlu2. The central hypothesis was that these compounds could …

    duquesne Repository record

  13. Exploring Potential Drug Target Sites In The Ribosome Using Cisplatin And Its Analogues

    Rijal, Keshab2011

    … sites of interaction with RNA and its use as a chemical probe to gain accessibility information, were explored.</p> <p>To understand the site-selectivity of cisplatin with RNA, model RNA constructs and full-length 16S rRNA were employed. The binding studies revealed a cisplatin preference for …

    wayne-thes Repository record

  14. Approaches Towards the Inhibition of Anti-Apoptotic Proteins

    iegre, jessicaUniversity of Cambridge2019

    … affinity (Kd 150 nM), and that can act as a chemical probe for targeting the PPI of CK2. 2) Inhibition of the anti-apoptotic Bcl-2 proteins to dissect their role in platelet activation and apoptosis. Bcl-2 proteins regulate cell lifespan; however, their role in non-nucleated platelets is not …

    cambridge Repository record

  15. Analyzing Resistance to Design Chemical Inhibitors of AAA Proteins

    Pisa, Rudolf

    … alleles can thus reveal and suggest the biochemical determinants of the drug's selectivity and potency. In this thesis, I explore how mutations in active sites of proteins can be leveraged to understand inhibitor binding and to design selective chemical inhibitors. In my thesis work I focus …

    rockefeller Repository record

  16. Hinokitiol restores hemoglobinization and mitigates neurodegeneration in animals by re-establishing iron homeostasis

    Ekaputri, StellaUniversity of Illinois Urbana-Champaign2023

    … mice, a mouse model of FD, as well as various biochemical and cell-based assays, we show that hinokitiol redistributes iron from liver macrophages to serum transferrin and promotes hemoglobinization in transferrin-dependent manner. We also show that hinokitiol interfaces with endogenous proteins …

    uiuc Repository record

  17. Chemical Biology of Dynein

    Santarossa, Cristina C

    … of dynein action. Fast-acting small molecule probes can be powerful tools to study dynein's many cellular mechanisms, but the design of potent and selective inhibitors of dynein remains challenging. Inhibitors of dynein's motor domain have been reported, such as ciliobrevins, dynapyrazoles and …

    rockefeller Repository record

  18. IN VITRO SUSCEPTIBILITY OF CHLAMYDIA TRACHOMATIS TO LPS-BINDING POLYAMINES AND CELLULOSE ETHER POLYMERS: TOWARDS THE DEVELOPMENT OF A MICROBICIDE AGAINST CHLAMYDIA INFECTION

    Osaka, IchieUniversity of Kansas2013

    … small molecule DS-96 targeting lipid A as a chemical probe. DS-96 effectively blocked chlamydial attachment and entry steps, suggesting that chlamydial LOS plays a role in these steps. These data were supported by the observation that a high level of inhibition by DS-96 was maintained through …

    ku Repository record

  19. DEVELOPING CHEMICAL TOOLS TO MAP MOLECULAR MECHANISMS THAT DRIVE DISEASE

    Hurben, Alexander2023

    … and neurodegenerative diseases. Often, small chemical changes to our DNA and proteins can be the culprits of such dysregulation. These seemingly minuscule modifications can impair the cell’s proper functions, which can lead to cell death or uncontrolled growth, and ultimately manifest as …

    umn Repository record

  20. Synthesis of Structurally Diverse N-Substituted Quaternary Carbon Containing Small Molecules and Their Application as Novel Starting Points for Drug Discovery

    Kidd, Sarah LouiseUniversity of Cambridge2019

    … required to seed both medicinal chemistry and chemical biology research. Within the two last decades, however, organic synthesis has been identified as a limiting factor in this regard owing to the historically uneven exploration of chemical space. Whilst fragment-based screening has proven a …

    cambridge Repository record

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