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2. BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma

Author

Weisberg, Ellen, Chowdhury, Basudev, Meng, Chengcheng, Case, Abigail E., Ni, Wei, Garg, Swati, Sattler, Martin, Azab, Abdel Kareem, Sun, Jennifer, Muz, Barbara, Sanchez, Dana, Toure, Anthia, Stone, Richard M., Galinsky, Ilene, Winer, Eric, Gleim, Scott, Gkountela, Sofia, Kedves, Alexia, Harrington, Edmund, Abrams, Tinya, Zoller, Thomas, Vaupel, Andrea, Manley, Paul, Faller, Michael, Chung, BoYee, Chen, Xin, Busenhart, Philipp, Stephan, Christine, Calkins, Keith, Bonenfant, Debora, Thoma, Claudio R., Forrester, William, and Griffin, James D.

Published
2022
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3. BET bromodomain inhibitors regulate keratinocyte plasticity

Author

Schutzius, Gabi, Kolter, Christian, Bergling, Sebastian, Tortelli, Federico, Fuchs, Florian, Renner, Steffen, Guagnano, Vito, Cotesta, Simona, Rueeger, Heinrich, Faller, Michael, Bouchez, Laure, Salathe, Adrian, Nigsch, Florian, Richards, Shola M., Louis, Malvina, Gruber, Viktoria, Aebi, Alexandra, Turner, Jonathan, Grandjean, Frederic, Li, Jun, Dimitri, Chris, Thomas, Jason R., Schirle, Markus, Blank, Jutta, Drueckes, Peter, Vaupel, Andrea, Tiedt, Ralph, Manley, Paul W., Klopp, Julia, Hemmig, Rene, Zink, Florence, Leroy, Nelly, Carbone, Walter, Roma, Guglielmo, Keller, Caroline Gubser, Dales, Natalie, Beyerbach, Armin, Zimmerlin, Alfred, Bonenfant, Debora, Terranova, Remi, Berwick, Amy, Sahambi, Sukhdeep, Reynolds, Aimee, Jennings, Lori L., Ruffner, Heinz, Tarsa, Peter, Bouwmeester, Tewis, Driver, Vickie, Frederiksen, Mathias, Lohmann, Felix, and Kirkland, Susan

Published
2021
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12. Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist.

Author

Betschart, Claudia, Faller, Michael, Zink, Florence, Hemmig, René, Blank, Jutta, Vangrevelinghe, Eric, Bourrel, Marjorie, Glatthar, Ralf, Behnke, Dirk, Barker, Kerstin, Heizmann, Andreas, Angst, Daniela, Nimsgern, Pierre, Jacquier, Sébastien, Junt, Tobias, Zipfel, Géraldine, Ruzzante, Giulia, Loetscher, Pius, Limonta, Sarah, and Hawtin, Stuart

Published
2022
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14. Target-Based Identification and Optimization of 5‑Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.

Author

Knoepfel, Thomas, Nimsgern, Pierre, Jacquier, Sébastien, Bourrel, Marjorie, Vangrevelinghe, Eric, Glatthar, Ralf, Behnke, Dirk, Alper, Phil B., Michellys, Pierre-Yves, Deane, Jonathan, Junt, Tobias, Zipfel, Géraldine, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric, Boulay, Thomas, Loetscher, Pius, Faller, Michael, Blank, Jutta, and Feifel, Roland

Published
2020
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15. Operational optimization of a 4th generation district heating network with mixed integer quadratically constrained programming.

Author

Hering, Dominik, Faller, Michael R., Xhonneux, André, and Müller, Dirk

Subjects
*WASTE heat, *HEATING from central stations, *HEAT pumps, *LOW temperatures, *INTEGERS, *OPERATING costs
Abstract

Decreasing CO 2 -Emissions is a common goal for efficient energy system design and operation. An efficient design for the heating sector are 4th-generation district heating networks with waste heat integration. This paper focuses on operational optimization of a 4th-generation district heating network with regards to temperatures and use of thermal inertia in the network and in thermal energy storages. A case study is presented, where the system is formulated as a Mixed-Integer Quadratically Constrained Program. The quadratic formulations allow to simultaneously optimize energy balances and temperatures, with regards to efficiency correlations and temperature thresholds of components. The case study consists of seven consumers with heat pumps and thermal energy storages, which are supplied by waste heat from a nearby high-performance computer. The case study is solved for eight representative days. The results show, that savings in operational costs up to 18.2% compared to a reference system with constant temperatures are possible. All in all, this paper demonstrates the use and limitations of quadratic formulations in an operational optimization and emphasizes the possibility of temperature optimizations in operation of 4th-generation district heating. • An MIQCP is presented for optimization of load shifting and operating temperatures. • The method is applied to a low temperature district heating network. • Results are compared to fixed temperature reference scenarios. • Including temperatures in the optimization improves the objective. [ABSTRACT FROM AUTHOR]

Published
2022
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16. Heme is involved in microRNA processing.

Author

Faller, Michael, Matsunaga, Michio, Yin, Sheng, Loo, Joseph A., and Guo, Feng

Subjects
*HEME, *RNA, *CELLULAR signal transduction, *GENE expression, *GENETIC regulation, *PROTEIN binding
Abstract

MicroRNAs (miRNAs) regulate the expression of a large number of protein-coding genes. Their primary transcripts (pri-miRNAs) have to undergo multiple processing steps to reach the functional form. Little is known about how the processing of miRNAs is modulated. Here we show that the RNA-binding protein DiGeorge critical region-8 (DGCR8), which is essential for the first processing step, is a heme-binding protein. The association with heme promotes dimerization of DGCR8. The heme-bound DGCR8 dimer seems to trimerize upon binding pri-miRNAs and is active in triggering pri-miRNA cleavage, whereas the heme-free monomer is much less active. A heme-binding region of DGCR8 inhibits the pri-miRNA–processing activity of the monomer. This putative autoinhibition is overcome by heme. Our finding that heme is involved in pri-miRNA processing suggests that the gene-regulation network of miRNAs and signal-transduction pathways involving heme might be connected. [ABSTRACT FROM AUTHOR]

Published
2007
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17. Microstructure and vacancy-type defects of high-pressure torsion deformed Al-3 wt%Cu alloy.

Author

Parz, Peter, Faller, Michael, Pippan, Reinhard, Reingruber, Herbert, Puff, Werner, and Würschum, Roland

Subjects
*ALUMINUM-copper alloys, *TORSION, *MICROSTRUCTURE, *POSITRON annihilation, *PRECIPITATION (Chemistry)
Abstract

The influence of high-pressure torsion (HPT) on the microstructure and free-volume type defects of supersaturated Al-3 wt%Cu was studied. By means of HPT, grain refinement down to sizes of 100 nm could be achieved. Positron annihilation spectroscopy was applied for the characterization of deformation-induced defects and of vacancy-solute interaction. The chemical sensitive method of two-dimensional Doppler broadening spectroscopy reveals predominantly deformation-induced defects. In comparison to undeformed supersaturated Al-3 wt%Cu, the fraction of Cu-decorated free-volume type defects is strongly reduced and Al2Cu-precipitates with equilibrium structure occur rather than metastable semi-coherent Al-Cu precipitates. These precipitates stabilize the nanocrystalline structure and give rise to a rather different aging behaviour compared to the undeformed state. [ABSTRACT FROM AUTHOR]

Published
2012
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18. Development of autotaxin inhibitors: A series of zinc binding triazoles.

Author

Thomson, Christopher G., Le Grand, Darren, Dowling, Mark, Brocklehurst, Cara E., Chinn, Colin, Elphick, Lucy, Faller, Michael, Freeman, Mark, Furminger, Vikki, Gasser, Cornelia, Hamadi, Ahmed, Hardaker, Elizabeth, Head, Victoria, Hill, Johan C., Janus, Diana I., Pearce, David, Poulaud, Anne-Sophie, Stanley, Emily, and Sviridenko, Lilya

Subjects
*AUTOTAXIN, *ENZYME inhibitors, *TRIAZOLES synthesis, *ZINC analysis, *CRYSTALLINITY
Abstract

A series of inhibitors of Autotaxin (ATX) has been developed using the binding mode of known inhibitor, PF-8380, as a template. Replacement of the benzoxazolone with a triazole zinc-binding motif reduced crystallinity and improved solubility relative to PF-8380. Modification of the linker region removed hERG activity and led to compound 12 – a selective, high affinity, orally-bioavailable inhibitor of ATX. Compound 12 concentration-dependently inhibits autotaxin and formation of LPA in vivo , as shown in pharmacokinetic-pharmacodynamic experiments. [ABSTRACT FROM AUTHOR]

Published
2018
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19. Development of autotaxin inhibitors: A series of tetrazole cinnamides.

Author

Thomson, Christopher G., Le Grand, Darren, Dowling, Mark, Beattie, David, Elphick, Lucy, Faller, Michael, Freeman, Mark, Hardaker, Elizabeth, Head, Victoria, Hemmig, Rene, Hill, Johan, Lister, Andrew, Pascoe, David, Rieffel, Sebastien, Shrestha, Binesh, Steward, Oliver, and Zink, Florence

Subjects
*AUTOTAXIN, *TETRAZOLES, *IDIOPATHIC pulmonary fibrosis
Abstract

A series of inhibitors of Autotaxin (ATX) have been developed from a high throughput screening hit, 1a , which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were dependent on the lipophilicity of the compounds, and this was optimised by reduction of clogD whilst maintaining high affinity ATX inhibition. Compound 15a shows good oral exposure, and concentration dependent inhibition of formation of LPA in vivo , as shown in pharmacokinetic-pharmacodynamic (PK/PD) experiments. [ABSTRACT FROM AUTHOR]

Published
2021
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