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....
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 ....
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....
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....
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....
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....
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....
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....
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....
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....
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 ....
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....
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<....
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 ....
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....
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
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....
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....