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Medicinal Chemistry Scholarly Works: Recent submissions
Now showing items 241-255 of 255
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Development and characterization of a novel C-terminal inhibitor of Hsp90 in androgen dependent and independent prostate cancer cells
(BioMed Central, 2011-10-31)Background: The molecular chaperone, heat shock protein 90 (Hsp90) has been shown to be overexpressed in a number of cancers, including prostate cancer, making it an important target for drug discovery. Unfortunately, results ... -
A filter-based feature selection approach for identifying potential biomarkers for lung cancer
(BioMed Central, 2011-03-21)Background: Lung cancer is the leading cause of death from cancer in the world and its treatment is dependant on the type and stage of cancer detected in the patient. Molecular biomarkers that can characterize the cancer ... -
Cyclopropylamine inactivation of cytochromes P450: Role of metabolic intermediate complexes
(Elsevier, 2005-04-15)The inactivation of cytochrome P450 enzymes by cyclopropylamines has been attributed to a mechanism involving initial one-electron oxidation at nitrogen followed by scission of the cyclopropane ring leading to covalent ... -
Molecular Basis for the High Affinity Binding and Stabilization of Firefly Luciferase by PTC124
(National Academy of Sciences, 2010-03-16)Firefly luciferase (FLuc), an ATP-dependent bioluminescent reporter enzyme, is broadly used in chemical biology and drug discovery assays. PTC124 (Ataluren; (3-[5-(2-fluorophenyl)-1,2,4-oxadiazol-3-yl]benzoic acid) discovered ... -
Ocular and Systemic Safety Evaluation of Calcium Formate as a Dietary Supplement
(Mary Ann Liebert, 2009-05-20)Purpose: The objective of this study was to perform a preliminary evaluation of the ocular and systemic safety of calcium formate, a dietary calcium supplement for prevention and management of osteoporosis. Although formate ... -
Enzymic transformation of an acyclic sesterterpene terminal epoxide into a lanosterol analogue
(Royal Society of Chemistry, 1969) -
Cobalt complexes: correlation of redox potential with effectivity as oxygenation catalysts
(Royal Society of Chemistry, 1974)The redox potential of a series of cobalt(II) chelates correlates with their properties as either oxygen carriers or phosphine oxidation catalysts. -
Metal-Catalyzed Hydration of 2-Pyridyloxirane
(Royal Society of Chemistry, 1975)In the presence of CuII the hydration of 2-pyridyloxiran is accelerated 18,000-fold, and its reaction with Cl–, Br–, and MeO– becomes 100% regiospecific for β-attack. -
Roles of key active-site residues in flavocytochrome P450 BM3
(Portland Press, 1999)The effects of mutation of key active-site residues (Arg-47, Tyr-51, Phe-42 and Phe-87) in Bacillus megaterium flavocytochrome P450 BM3 were investigated. Kinetic studies on the oxidation of laurate and arachidonate showed ... -
Structural analysis of metalloform-selective inhibition of methionine aminopeptidase
(International Union of Crystallography, 2006-04)One of the challenges in the development of methionine aminopeptidase (MetAP) inhibitors as antibacterial and anticancer agents is to define the metal ion actually used by MetAP in vivo and to discover MetAP inhibitors ... -
The reactive metabolite target protein database (TPDB) – a web-accessible resource
(BioMed Central, 2007-03-16)Background The toxic effects of many simple organic compounds stem from their biotransformation to chemically reactive metabolites which bind covalently to cellular proteins. To understand the mechanisms of cytotoxic ... -
Bioinformatic analysis of xenobiotic reactive metabolite target proteins and their interacting partners
(BioMed Central, 2009-06-12)Background Protein covalent binding by reactive metabolites of drugs, chemicals and natural products can lead to acute cytotoxicity. Recent rapid progress in reactive metabolite target protein identification has shown ... -
Absorption and elimination of formate following oral administration of calcium formate in female human subjects
(American Society for Pharmacology and Experimental Therapeutics, 2005-02)Published abstract: Calcium formate is a water-soluble salt of an essential mineral nutrient with potential for use as a dietary calcium supplement. Formate ion is a product of endogenous and xenobiotic metabolism, but ... -
Relative bioavailability of calcium from calcium formate, calcium citrate, and calcium carbonate
(American Society for Pharmacology and Experimental Therapeutics, 2005-06)Published Abstract: Calcium is an essential nutrient required in substantial amounts, but many diets are deficient in calcium making supplementation necessary or desirable. The objective of this study was to compare the ... -
A combined intramolecular Diels-Alder/intramolecular Schmidt reaction: Formal synthesis of (+/-)-stenine
(WILEY-V C H VERLAG GMBH, 2002)