Search Results - "Klumpp, Martin"

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach by Chen, Chao, Zhu, Hugh, Stauffer, Frédéric, Caravatti, Giorgio, Vollmer, Susanne, Machauer, Rainer, Holzer, Philipp, Möbitz, Henrik, Scheufler, Clemens, Klumpp, Martin, Tiedt, Ralph, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Zhang, Jeff, Gaul, Christoph

“…Oncogenic MLL fusion proteins aberrantly recruit Dot1L, a histone methyltransferase, to ectopic loci, leading to local hypermethylation of H3K79 and…”
Get full text

Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor by Graf, Christine, Klumpp, Martin, Habig, Michael, Rovina, Philipp, Billich, Andreas, Baumruker, Thomas, Oberhauser, Berndt, Bornancin, Frédéric

“…Ceramide kinase (CerK) produces the bioactive lipid ceramide-1-phosphate (C1P) and appears as a key enzyme for controlling ceramide levels. In this study, we…”
Get more information

Development and validation of a generic fluorescent methyltransferase activity assay based on the transcreener AMP/GMP assay by Klink, Tony A, Staeben, Matt, Twesten, Kim, Kopp, Andrew L, Kumar, Meera, Dunn, Rebecca Schall, Pinchard, Cori A, Kleman-Leyer, Karen M, Klumpp, Martin, Lowery, Robert G

“…Methylation is a ubiquitous covalent modification used to control the function of diverse biomolecules including hormones, neurotransmitters, xenobiotics,…”
Get more information

Structure of the Substrate Binding Domain of the Thermosome, an Archaeal Group II Chaperonin by Klumpp, Martin, Baumeister, Wolfgang, Essen, Lars-Oliver

“…The crystal structure of the substrate binding domain of the thermosome, the archaeal group II chaperonin, has been determined at 2.3 Å resolution. The core…”
Get full text

Non-stoichiometric inhibition in integrated lead finding - a literature review by Klumpp, Martin

“…Non-stoichiometric inhibition summarizes different mechanisms by which low-molecular weight compounds can reproducibly inhibit high-throughput screening (HTS)…”
Get more information

Screening for Inhibitors of Kinase Autophosphorylation by Heedmann, Bianca, Klumpp, Martin

“…Autophosphorylation of kinases influences their conformational state and can also regulate enzymatic activity. Recently, this has become an area of interest…”
Get more information

Analysis of p53 “Latency” and “Activation” by Fluorescence Correlation Spectroscopy by Wölcke, Julian, Reimann, Maurice, Klumpp, Martin, Göhler, Thomas, Kim, Ella, Deppert, Wolfgang

“…The concept that the tumor suppressor p53 is a latent DNA-binding protein that must become activated for sequence-specific DNA binding recently has been…”
Get full text

Group II chaperonin in an open conformation examined by electron tomography by Baumeister, Wolfgang, Nitsch, Michael, Walz, Jochen, Typke, Dieter, Klumpp, Martin, Essen, Lars-Oliver

Get full text

Expression of an archaeal chaperonin in E. coli: formation of homo- (α, β) and hetero-oligomeric (α + β) thermosome complexes by Waldmann, Thomas, Nitsch, Michael, Klumpp, Martin, Baumeister, Wolfgang

“…Co-expression of the two genes encoding the α- and β-subunit of the Thermoplasma acidophilum thermosome in Escherichia coli yielded fully assembled…”
Get full text

A Screening Pattern Recognition Method Finds New and Divergent Targets for Drugs and Natural Products by Wassermann, Anne Mai, Lounkine, Eugen, Urban, Laszlo, Whitebread, Steven, Chen, Shanni, Hughes, Kevin, Guo, Hongqiu, Kutlina, Elena, Fekete, Alexander, Klumpp, Martin, Glick, Meir

“…Computational target prediction methods using chemical descriptors have been applied exhaustively in drug discovery to elucidate the mechanisms-of-action…”
Get full text

Light it up: Highly efficient multigene delivery in mammalian cells by Trowitzsch, Simon, Klumpp, Martin, Thoma, Ralf, Carralot, Jean-Philippe, Berger, Imre

“…Multigene delivery and expression systems are emerging as key technologies for many applications in contemporary biology. We have developed new methods for…”
Get full text

A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P 3 – P 1 Pharmacophore by Ostermann, Nils, Ruedisser, Simon, Ehrhardt, Claus, Breitenstein, Werner, Marzinzik, Andreas, Jacoby, Edgar, Vangrevelinghe, Eric, Ottl, Johannes, Klumpp, Martin, Hartwieg, J. Constanze D., Cumin, Frederic, Hassiepen, Ulrich, Trappe, Jörg, Sedrani, Richard, Geisse, Sabine, Gerhartz, Bernd, Richert, Paul, Francotte, Eric, Wagner, Trixie, Krömer, Markus, Kosaka, Takatoshi, Webb, Randy L., Rigel, Dean F., Maibaum, Jürgen, Baeschlin, Daniel K.

Get full text

A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3 –P1 Pharmacophore by Ostermann, Nils, Ruedisser, Simon, Ehrhardt, Claus, Breitenstein, Werner, Marzinzik, Andreas, Jacoby, Edgar, Vangrevelinghe, Eric, Ottl, Johannes, Klumpp, Martin, Hartwieg, J. Constanze D, Cumin, Frederic, Hassiepen, Ulrich, Trappe, Jörg, Sedrani, Richard, Geisse, Sabine, Gerhartz, Bernd, Richert, Paul, Francotte, Eric, Wagner, Trixie, Krömer, Markus, Kosaka, Takatoshi, Webb, Randy L, Rigel, Dean F, Maibaum, Jürgen, Baeschlin, Daniel K

“…A small library of fragments comprising putative recognition motifs for the catalytic dyad of aspartic proteases was generated by in silico similarity searches…”
Get full text

Efficient elimination of nonstoichiometric enzyme inhibitors from HTS hit lists by Habig, Michael, Blechschmidt, Anke, Dressler, Sigmar, Hess, Barbara, Patel, Viral, Billich, Andreas, Ostermeier, Christian, Beer, David, Klumpp, Martin

“…High-throughput screening often identifies not only specific, stoichiometrically binding inhibitors but also undesired compounds that unspecifically interfere…”
Get more information

Measurement of enzyme kinetics and inhibitor constants using enthalpy arrays by Recht, Michael I., Torres, Frank E., Bruyker, Dirk De, Bell, Alan G., Klumpp, Martin, Bruce, Richard H.

“…Enthalpy arrays enable label-free, solution-based calorimetric detection of molecular interactions in a 96-detector array format. Compared with conventional…”
Get full text

Measurement of enzyme kinetics and inhibitor constants using enthalpy arrays1 by Recht, Michael I., Torres, Frank E., De Bruyker, Dirk, Bell, Alan G., Klumpp, Martin, Bruce, Richard H.

“…Enthalpy arrays enable label-free, solution-based calorimetric detection of molecular interactions in a 96-detector array format. Compared with conventional…”
Get full text

Readout technologies for highly miniaturized kinase assays applicable to high-throughput screening in a 1536-well format by Klumpp, Martin, Boettcher, Andreas, Becker, Damaris, Meder, Gabriele, Blank, Jutta, Leder, Lukas, Forstner, Michael, Ottl, Johannes, Mayr, Lorenz M

“…This article discusses the development of homogeneous, miniaturized assays for the identification of novel kinase inhibitors from very large compound…”
Get more information

The thermosome: archetype of group II chaperonins by Klumpp, Martin, Baumeister, Wolfgang

“…The thermosome, the chaperonin of the archaea, and its homologue from the cytosol of eukaryotes, known as TRiC or CCT, form a distinct subfamily of the…”
Get full text

Analysis of p53 "latency" and "activation" by fluorescence correlation spectroscopy. Evidence for different modes of high affinity DNA binding by Wölcke, Julian, Reimann, Maurice, Klumpp, Martin, Göhler, Thomas, Kim, Ella, Deppert, Wolfgang

“…The concept that the tumor suppressor p53 is a latent DNA-binding protein that must become activated for sequence-specific DNA binding recently has been…”
Get full text

The thermosome: alternating α and β-subunits within the chaperonin of the archaeon Thermoplasma acidophilum by Nitsch, Michael, Klumpp, Martin, Lupas, Andrei, Baumeister, Wolfgang

“…The thermosome of the archaeon Thermoplasma acidophilum is composed of two subunits, α and β, which are arranged in two stacked, eight-membered rings. Electron…”
Get full text