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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 196 for “"small molecule inhibitors"”.
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Small Molecule Inhibitors of HPV16 E6
… between HPV E6 and its partners using small molecules had the potential to re-sensitize HPV+ cells to apoptosis. To test this prediction, we screened libraries of small molecules for candidates that could block E6/caspase 8 binding, and identified several candidates from different …
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Small molecule inhibitors of parasitic enzymes
… is threefold:-(i) development of potential novel inhibitors of cysteine proteases from the causative agents of Malaria, African sleeping sickness and Chagas disease, (ii) development of potential new and novel anti-trypanosomal inhibitors of trypanosome alternative oxidase, and (ii) synthetic and …
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Small molecule inhibitors against enteric bacterial glycosyltransferases
… C. rodentium virulence, we aimed to find small molecular inhibitors which specifically bind to NleB. Therefore, we performed high-throughput screening (HTS) assays to identify NleB/SseK inhibitors. We identified two compounds (100066N and 102644N) that significantly inhibited NleB1, SseK1, …
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Investigating small-molecule inhibitors of platelet aggregation
… tools were used to virtually screen over 440,000 molecules to identify novel scaffolds possessing reasonable similarities in 3D shape and electrostatic properties in reference to the experimental P2Y12 antagonist, AZD1283. Docking of the best hits was performed against the recently solved crystal …
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The search for small molecule inhibitors of histone acetylation
… for example cancer and HIV. The<br/>search for small molecule inhibitors of histone acetylation focuses on anacardic acid and the<br/>azumamides. Anacardic acid is a natural compound found in cashew nut shell liquid. Its structure<br/>consists of salicylic acid and a long hydrophobic alkyl tail, …
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Approaches to Study Small Molecule Inhibitors and Their Targets
<p>Bioactive small molecules are valuable tools to understand and manipulate biological pathways. In order to be effective as either probes for understanding cell biology or as clinical drugs, the small molecule's mechanism of action must be characterized. However, identifying a small molecule's …
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Analysis of Small Molecule Inhibitors Aimed at Bacterial Virulence
… host cells by Gram-negative bacterial pathogens. Small molecules that target type III protein secretion may therefore represent a new class of antibacterial agents and provide a platform for evaluating an anti-virulence approach. The salicylidene acylhydrazides (SAHs) are a class of compounds that …
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Small molecule inhibitors: novel probes of progesterone receptor action
… and breast cancer. We have identified a set of small molecules that uniquely act outside of PR’s ligand-binding pocket and selectively inhibit PR activity in intact cells. These small molecules inhibit PR-mediated induction of the mouse mammary tumor virus (MMTV)-luciferase reporter and …
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The development of small molecule inhibitors for fibrosis drug discovery
… detailed in this report were aimed to develop small molecule inhibitors with drug like physicochemical properties for fibrosis drugdiscovery.;Chapter 1 focusses on the secreted enzyme ATX, which is responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic …
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Identification of small molecule inhibitors targeting Plasmodium falciparum Hsp70-Hop pathway
… Both PfHsp70-1 and PfHsp90 are essential molecules that could be specifically inhibited by potential antimalarial drugs. Therefore, this study evaluated the inhibition of the functional partnership between PfHop and PfHsp70-1 by colistin sulfate and pifithrin µ. In order to carry out in …
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Hdm2 Small-Molecule Inhibitors For Therapeutic Intervention In B-Cell Lymphoma
… value of disrupting HDM2-p53 association by small-molecule inhibitors (SMIs). HDM2 SMIs have been developed and are currently under various stages of preclinical and clinical investigation. This study examined various molecular mechanisms associated and biological effects of two different …
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Structure-based Design of Small Molecule Inhibitors of HIV-1 Entry
… and replication. One of the targets of HIV entry inhibitors is the interaction between CD4 and gp120. A large percentage of CD4-gp120 contacts revolved around a cavity in gp120 in which the PHE43 residue of CD4 caps. We were able to design and synthesize a progression of small molecule compounds …
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Small molecule inhibitors of lactate dehydrogenase A as an anticancer strategy
Embargo set by: Seth Robbins for item 73141 Lift date: 2017-01-21T19:56:18Z Reason: Author requested U of Illinois access only (OA after 2yrs) in Vireo ETD system
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Small molecule inhibitors of steroid receptors for breast and prostate cancer
… prostate cancer treatment. Reported here are two inhibitors that antagonize androgen receptor (AR) function and one that suppresses estrogen receptor (ER) signaling. Moderate-to-high throughput screens of chemical libraries were designed and implemented to identify these inhibitors. The most …
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The Identification and Development of Small Molecule Inhibitors of Amyloid β Aggregation
… and spectral interference from the test molecules, can limit efforts to identify new small molecule inhibitors. Furthermore, the lack of robust, time- and cost-efficient methods for screening compounds in cellular or in vivo models limits the throughput with which seemingly active small …
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Isoform Selective Regulation of Adenylyl Cyclase By Small Molecule Inhibitors and Gbetagamma Protein
… cyclase (AC), via synthesis of the signaling molecule cyclic AMP (cAMP), are involved in many isoform specific physiological functions. All nine isoforms share a similar structural organization; thus, AC isoform differences in physiological function are due to different regulatory profiles. A …
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Discovery and Characterization of Small Molecule Inhibitors of Biofilm Formation in Pseudomonas Aeruginosa
… patients. Unfortunately, no clinically effective inhibitors of biofilm formation are available. Through the development and application of convenient high-throughput screening methods for non-antibiotic biofilm inhibitors, it was discovered that simple iron salts are potent inhibitors of biofilm …
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The discovery of small molecule inhibitors of poly(ADP-ribose) mediated cell death
… (PARP-1), the enzyme that synthesizes PAR, inhibitors are currently in clinical trials as chemopotentiators, and as personalized treatments for patients with the BRCA-1/-2 mutation. However, there is a lack of small molecule inhibitors of other important enzymes and proteins in this pathway. …
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Strategies to Sensitize Bladder Cancer Cells to Small Molecule Inhibitors Targeting The Pi3K Pathway
… in this particular type of cancer. Several small molecule inhibitors have been developed to target this pathway, but their efficacy has been shown to be heterogeneous among different cell lines and mostly cytostatic but not cytotoxic in the case of bladder cancer. Understanding the genetic …
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Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents
… describe the design, synthesis and evaluation of small-molecule inhibitors of two different biological targets: <em>Plasmodium falciparium</em>, the most virulent malarial parasite in humans, and plasminogen activator inhibitor-1 (PAI-1), an endogenous serine proteases inhibitor implicated in a …
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