Chemistry

Functional Studies of Plasmodium falciparum Dipeptidyl Aminopeptidase I Using Small Molecule Inhibitors and Active Site Probes

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Edgar Deu, Melissa J. Leyva, Victoria E. Albrow, Mark J. Rice, Jonathan A. Ellman, Matthew Bogyo. The widespread resistance of malaria parasites to all affordable drugs has made the identification of new targets urgent. Dipeptidyl aminopeptidases (DPAPs) represent potentially valuable new targ....
Categories: Biology, Chemistry, Journals

Application of Fragment-Based Drug Discovery to Membrane Proteins: Identification of Ligands of the Integral Membrane Enzyme DsbB

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Virginie Früh, Yunpeng Zhou, Dan Chen, Caroline Loch, Eiso AB, Yelena N. Grinkova, Herman Verheij, Stephen G. Sligar, John H. Bushweller, Gregg Siegal. Membrane proteins are important pharmaceutical targets, but they pose significant challenges for fragment-based drug discovery approaches. Here, we present the first successful use of biophysical ....
Categories: Biology, Chemistry, Journals

Nitric Oxide-Mediated Histone Hyperacetylation in Oral Cancer: Target for a Water-Soluble HAT Inhibitor, CTK7A

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Mohammed Arif, Bhusainahalli M. Vedamurthy, Ramesh Choudhari, Yogesh B. Ostwal, Kempegowda Mantelingu, Gopinath S. Kodaganur, Tapas K. Kundu. Altered histone acetylation is associated with several diseases, including cancer. We report here that, unlike in most cancers, histones are found to be highly hyperacetylated in oral squamous cel....
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A Metabolomic View of Staphylococcus aureus and Its Ser/Thr Kinase and Phosphatase Deletion Mutants: Involvement in Cell Wall Biosynthesis

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Manuel Liebeke, Hanna Meyer, Stefanie Donat, Knut Ohlsen, Michael Lalk. Little is known about intracellular metabolite pools in pathogens such as Staphylococcus aureus. We have studied a particular metabolome by means of the presented LC-MS method. By investiga....
Categories: Biology, Chemistry, Journals

The Awesome Power of Synergy from Chemical-Chemical Profiling

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Jeff S. Piotrowski, Chuek Hei Ho, Charles Boone. Chemical-chemical profiling, as described in Farha and Brown (2010), delivers all the power of chemical-genomic profiling while untethering researchers from model systems and thereby enabling us t....
Categories: Biology, Chemistry, Journals

Expanding the Biological Periodic Table

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Javier Seravalli, Stephen W. Ragsdale. Metal ions play an indispensable role in biology, enabling enzymes to perform their functions and lending support to the structures of numerous macromolecules. Despite their prevalence and importa....
Categories: Biology, Chemistry, Journals

Chemical Probes of Escherichia coli Uncovered through Chemical-Chemical Interaction Profiling with Compounds of Known Biological Activity

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Maya A. Farha, Eric D. Brown. While cell-based screens have considerable power in identifying new chemical probes of biological systems and leads for new drugs, a major challenge to the utility of such compounds is in connecti....
Categories: Biology, Chemistry, Journals

The Glycerophospho Metabolome and Its Influence on Amino Acid Homeostasis Revealed by Brain Metabolomics of GDE1(−/−) Mice

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Florian Kopp, Toru Komatsu, Daniel K. Nomura, Sunia A. Trauger, Jason R. Thomas, Gary Siuzdak, Gabriel M. Simon, Benjamin F. Cravatt. GDE1 is a mammalian glycerophosphodiesterase (GDE) implicated by in vitro studies in the regulation of glycerophophoinositol (GroPIns) and possibly other glycerophospho (GroP) metabolites. Here, w....
Categories: Biology, Chemistry, Journals

Recognition of Intermediate Functionality by Acyl Carrier Protein over a Complete Cycle of Fatty Acid Biosynthesis

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Eliza Płoskoń, Christopher J. Arthur, Amelia L.P. Kanari, Pakorn Wattana-amorn, Christopher Williams, John Crosby, Thomas J. Simpson, Christine L. Willis, Matthew P. Crump. It remains unclear whether in a bacterial fatty acid synthase (FAS) acyl chain transfer is a programmed or diffusion controlled and random action. Acyl carrier protein (ACP), which delivers all in....
Categories: Biology, Chemistry, Journals

Bioactive Cell-Penetrating Peptides: Kill Two Birds with One Stone

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Gilles Divita. Jones et al. (2010) propose an innovative strategy for the development of bioactive cell-penetrating peptides. They combine computer-based design with specific targeting to elaborate a potent cell....
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A Eubacterial Riboswitch Class That Senses the Coenzyme Tetrahydrofolate

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Tyler D. Ames, Dmitry A. Rodionov, Zasha Weinberg, Ronald R. Breaker. Comparative sequence analyses of bacterial genomes are revealing many structured RNA motifs that function as metabolite-binding riboswitches. We have identified an RNA motif frequently positioned ....
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Red Fluorescent Protein with Reversibly Photoswitchable Absorbance for Photochromic FRET

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Fedor V. Subach, Lijuan Zhang, Theodorus W.J. Gadella, Nadya G. Gurskaya, Konstantin A. Lukyanov, Vladislav V. Verkhusha. We have developed the first red fluorescent protein, named rsTagRFP, which possesses reversibly photoswitchable absorbance spectra. Illumination with blue and yellow light switches rsTagRFP into a....
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Characterization of Bioactive Cell Penetrating Peptides from Human Cytochrome c: Protein Mimicry and the Development of a Novel Apoptogenic Agent

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Sarah Jones, Tina Holm, Imre Mäger, Ülo Langel, John Howl. Cell penetrating peptides (CPPs) with intrinsic biological activities offer a novel strategy for the modulation of intracellular events. QSAR analysis identified CPPs within human cytochrome c<....
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Microfluidic Compartmentalized Directed Evolution

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Brian M. Paegel, Gerald F. Joyce. Directed evolution studies often make use of water-in-oil compartments, which conventionally are prepared by bulk emulsification, a crude process that generates nonuniform droplets and can damage ....
Categories: Biology, Chemistry, Journals

Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Tim J. Wigle, Laurel M. Provencher, Jacqueline L. Norris, Jian Jin, Peter J. Brown, Stephen V. Frye, William P. Janzen. The discovery of small molecules targeting the >80 enzymes that add (methyltransferases) or remove (demethylases) methyl marks from lysine and arginine residues, most notably present in histone....
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Dihydrosphingomyelin Impairs HIV-1 Infection by Rigidifying Liquid-Ordered Membrane Domains

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Catarina R. Vieira, Jose M. Munoz-Olaya, Jesús Sot, Sonia Jiménez-Baranda, Nuria Izquierdo-Useros, Jose Luis Abad, Beatriz Apellániz, Rafael Delgado, Javier Martinez-Picado, Alicia Alonso, Josefina Casas, José L. Nieva, Gemma Fabriás, Santos Mañes, Félix M. Goñi. The lateral organization of lipids in cell membranes is thought to regulate numerous cell processes. Most studies focus on the coexistence of two fluid phases, the liquid crystalline (l
Categories: Biology, Chemistry, Journals

Insights into Protein-Protein and Enzyme-Substrate Interactions in Modular Polyketide Synthases

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Lucky Tran, R. William Broadhurst, Manuela Tosin, Andrea Cavalli, Kira J. Weissman. Numerous natural products of clinical value are biosynthesized by polyketide synthases (PKSs) and nonribosomal peptide synthetases (NRPSs), which are multienzymes comprising modules of catalytic d....
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Application of Chemoproteomics to Drug Discovery: Identification of a Clinical Candidate Targeting Hsp90

Chemistry and Biology (most read) - Thu, 2010-09-09 06:30
Patrick Fadden, Kenneth H. Huang, James M. Veal, Paul M. Steed, Amy F. Barabasz, Briana Foley, Mei Hu, Jeffrey M. Partridge, John Rice, Anisa Scott, Laura G. Dubois, Tiffany A. Freed, Melanie A. Rehder Silinski, Thomas E. Barta, Philip F. Hughes, Andy Ommen, Wei Ma, Emilie D. Smith, Angela Woodward Spangenberg, Jeron Eaves, Gunnar J. Hanson, Lindsay Hinkley, Matthew Jenks, Meredith Lewis, James Otto, Gijsbertus J. Pronk, Katleen Verleysen, Timothy A. Haystead, Steven E. Hall. A chemoproteomics-based drug discovery strategy is presented that utilizes a highly parallel screening platform, encompassing more than 1000 targets, with a focused chemical library prior t....
Categories: Biology, Chemistry, Journals