small molecule drug discovery
Patient derived lymphoblastoid cell lines harboring mitochondrial DNA mutations as tool for small molecule drug discovery
... of small molecules in ...the discovery of broadly-applicable small molecule therapeutics for mitochondrial disease, and/or identify genetic mutations that may confer resist- ance to such ...of ...
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Small Molecule Inhibitors of PTP1B and TCPTP
... range owing to their low molecular weights. These molecules can be taken as a starting pharmacophore for developing a selective potent inhibitor by exploring sites in the vicinity of binding pockets. The compound AU-008 ...
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Discovery of Small-Molecule Human Immunodeficiency Virus Type 1 Entry Inhibitors That Target the gp120-Binding Domain of CD4
... for drug de- velopment, T20, a fusion inhibitor (36, 42, 43), is the only HIV entry inhibitor approved by the ...and Drug Admin- istration for the treatment of HIV/AIDS at the present ...
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The Who, Why, and How of Small-Molecule Production in Invertebrate Microbiomes: Basic Insights Fueling Drug Discovery
... defensive small molecules is strong in symbionts (13, 15), pressure to maintain basic metabolic functions needed for independent growth is weakened because of the hospitable and stable host environment ...where ...
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Discovery of Novel Small Molecule Activators of beta-Catenin Signaling
... Integrative approaches coupling protein interaction maps to siRNA screening data have suggested that the components that constitute the Wnt/b-catenin signaling machinery in a given cell type are highly variable [21]. Our ...
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Discovery, in vivo activity, and mechanism of action of a small molecule p53 activator
... 30,000 drug-like small molecules from the Chembridge DIVERSet for their ability to activate p53 in a robust, simple, and cheap primary cell-based screening ...
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Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1
... Given the critical role of LIMK in regulating cell migration, chemotaxis, and T cell activation, long-term suppression of LIMK may inhibit immune responses. Nevertheless, the possibility of developing future clinical ...
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Realisation of small molecule libraries based on frameworks distantly related to natural products
... scaffolds were developed from two common cycloadducts. The robust and scalable synthetic methods enabled the scaffolds 3-6 to be prepared on a scale that was suitable for the production of large numbers of screening ...
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Toxins and drug discovery
... for drug discovery and ...conventional small molecules appear to be gaining favour with development companies and with regulatory author- ...than small-molecule NMEs: ...approved ...
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Molecular dynamics simulations and drug discovery
... In some rare cases, protein motions are limited, and the ligand may fit into a fairly static binding pocket like a key fits into a lock [2]. More typically, the ligand may bind and stabilize only a subset of the many ...
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Discovery of a small molecule targeting SET-PP2A interaction to overcome BCR-ABL T315I mutation of chronic myeloid leukemia
... Given the decisive role of BCR-ABL in the development of CML, TKI-based therapy has been regarded as the gold standard for the treatment of CML since the excellent clinical performance of the first TKI, imatinib. The ...
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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes
... of drug resistance and the lack of effective drugs are well exemplified by malaria and Chagas disease, ...of small-molecule probes that act against these infectious agents through new ...
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Discovery and Application of Small Molecule Regulators of MicroRNA Function.
... are small non-coding RNAs that act as post-transcriptional gene regulators and have been shown to control many biological processes including embryonal development, cell differentiation, apoptosis, and ...
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Implications of the Business Strategies of Pharmaceutical Companies for Industry Developments in Australia
... new drug is launched with a comprehensive and expensive global marketing campaign that involves the full range of marketing tools including media advertising, comprehensive information packs, special events for ...
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Small Molecule Inhibitors of CXCR4
... The identification and development of CXCR4 antagonists have been described in several recent studies [57-61]. In 2008, we published a comprehen- sive review covering publications and patent applica- tions describing ...
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Small Molecule Acetylation Controls the Degradation of Benzoate and Photosynthesis in Rhodopseudomonas palustris
... BadL is required for the expression of the genes encoding enzymes that dearomatize the benzene ring. As shown by in vivo data (Fig. 2A and B), R. palustris requires BadL function to grow on benzoate as the source of ...
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Discovery and Development of Small Molecule Modulators for the Sulfation of Glycosaminoglycans and Studying the Role of O GlcNAc on CREB through Semisynthesis
... cell-permeable small molecule that can selectively inhibit GAG sulfotransferases and modify the fine structure of ...This small molecule may serve as a useful lead compound or chemical tool ...
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Small molecule screening in zebrafish: an in vivo approach to identifying new chemical tools and drug leads
... for drug toxicity and teratogenisity, as well as for testing direct chemical targets in ...valuable drug for multiple myeloma and leprosy, but caused severe developmental birth defects when taken by ...
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Drug discovery in jeopardy
... of drug companies. Reduced pro- ductivity in the drug industry is caused mainly by corporate policies that discourage ...for drug discovery are ...
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Moga_unc_0153D_15304.pdf
... To optimize microneedles for the delivery of chemotherapeutics to skin-invading breast cancers, tumor-bearing animal studies must be performed on optimized PRINT microneedle devices with docetaxel. Quantitative assays ...
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