Search Results - "LUNDBÄCK, Thomas"

The cellular thermal shift assay for evaluating drug target interactions in cells by Jafari, Rozbeh, Almqvist, Helena, Axelsson, Hanna, Ignatushchenko, Marina, Lundbäck, Thomas, Nordlund, Pär, Molina, Daniel Martinez

“…Interaction between a drug and its protein target results in a shift in thermal stability of that protein. The cellular thermal shift assay–CETSA–exploits this…”
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CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil by Almqvist, Helena, Axelsson, Hanna, Jafari, Rozbeh, Dan, Chen, Mateus, André, Haraldsson, Martin, Larsson, Andreas, Molina, Daniel Martinez, Artursson, Per, Lundbäck, Thomas, Nordlund, Pär

“…Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly…”
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CETSA beyond Soluble Targets: a Broad Application to Multipass Transmembrane Proteins by Kawatkar, Aarti, Schefter, Michelle, Hermansson, Nils-Olov, Snijder, Arjan, Dekker, Niek, Brown, Dean G, Lundbäck, Thomas, Zhang, Andrew X, Castaldi, M. Paola

“…Demonstration of target binding is a key requirement for understanding the mode of action of new therapeutics. The cellular thermal shift assay (CETSA) has…”
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Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery by Mateus, André, Gordon, Laurie J., Wayne, Gareth J., Almqvist, Helena, Axelsson, Hanna, Seashore-Ludlow, Brinton, Treyer, Andrea, Matsson, Pär, Lundbäck, Thomas, West, Andy, Hann, Michael M., Artursson, Per

“…Inadequate target exposure is a major cause of high attrition in drug discovery. Here, we show that a label-free method for quantifying the intracellular…”
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Inhibition of Insulin-Regulated Aminopeptidase by Imidazo [1,5-α]pyridines-Synthesis and Evaluation by Engen, Karin, Lundbäck, Thomas, Yadav, Anubha, Puthiyaparambath, Sharathna, Rosenström, Ulrika, Gising, Johan, Jenmalm-Jensen, Annika, Hallberg, Mathias, Larhed, Mats

“…Inhibition of insulin-regulated aminopeptidase (IRAP) has been shown to improve cognitive functions in several animal models. Recently, we performed a…”
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Quantitative Interpretation of Intracellular Drug Binding and Kinetics Using the Cellular Thermal Shift Assay by Seashore-Ludlow, Brinton, Axelsson, Hanna, Almqvist, Helena, Dahlgren, Björn, Jonsson, Mats, Lundbäck, Thomas

“…Evidence of physical interaction with the target protein is essential in the development of chemical probes and drugs. The cellular thermal shift assay (CETSA)…”
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Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis by Brunner, Katharina, Maric, Selma, Reshma, Rudraraju Srilakshmi, Almqvist, Helena, Seashore-Ludlow, Brinton, Gustavsson, Anna-Lena, Poyraz, Ömer, Yogeeswari, Perumal, Lundbäck, Thomas, Vallin, Michaela, Sriram, Dharmarajan, Schnell, Robert, Schneider, Gunter

“…Cysteine is an important amino acid in the redox defense of Mycobacterium tuberculosis, primarily as a building block of mycothiol. Genetic studies have…”
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Identification of epidermal growth factor receptor-tyrosine kinase inhibitor targeting the VP1 pocket of human rhinovirus by Miah, Masum, Davis, Andrew M, Hannoun, Charles, Said, Joanna S, Fitzek, Martina, Preston, Marian, Smith, Dave, Uwamariya, Colores, Kärmander, Ambjörn, Lundbäck, Thomas, Bergström, Tomas, Trybala, Edward

“…Screening a library of 1,200 preselected kinase inhibitors for anti-human rhinovirus 2 (HRV-2) activity in HeLa cells identified a class of epidermal growth…”
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A FabG inhibitor targeting an allosteric binding site inhibits several orthologs from Gram-negative ESKAPE pathogens by Vella, Peter, Rudraraju, Reshma Srilakshmi, Lundbäck, Thomas, Axelsson, Hanna, Almqvist, Helena, Vallin, Michaela, Schneider, Gunter, Schnell, Robert

“…[Display omitted] •FabG from the bacterial fatty acid biosynthesis (FAS-II) system is a potential target for antibiotics.•Inhibitors were identified by…”
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Letter to the Editor : Implementation of Acoustic Dispensing and 384-Well Based Workflows to Improve Assay Capacity and Reduce Compound and Solvent Use in Early Drug Metabolism and Pharmacokinetics Profiling by Wernevik, Johan, Hulthe, Johan, McPheat, Cameron, Di Castro, Silvio, Lundbäck, Thomas

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Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures by Plesniak, Mateusz P., Taylor, Emilia K., Eisele, Frederik, Kourra, Christopher M. B. K., Michaelides, Iacovos N., Oram, Alice, Wernevik, Johan, Valencia, Zulma Santisteban, Rowbottom, Hannah, Mann, Nadia, Fredlund, Linda, Pivnytska, Valentyna, Novén, Anna, Pirmoradian, Mohammad, Lundbäck, Thomas, Storer, R. Ian, Pettersson, Mariell, De Donatis, Gian M., Rehnström, Marie

“…Precise length, shape, and linker attachment points are all integral components to designing efficacious proteolysis targeting chimeras (PROTACs). Due to the…”
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In Situ Target Engagement Studies in Adherent Cells by Axelsson, Hanna, Almqvist, Helena, Otrocka, Magdalena, Vallin, Michaela, Lundqvist, Sara, Hansson, Pia, Karlsson, Ulla, Lundbäck, Thomas, Seashore-Ludlow, Brinton

“…A prerequisite for successful drugs is effective binding of the desired target protein in the complex environment of a living system. Drug–target engagement…”
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Targeting SAMHD1 with the Vpx protein to improve cytarabine therapy for hematological malignancies by Herold, Nikolas, Rudd, Sean G, Ljungblad, Linda, Sanjiv, Kumar, Myrberg, Ida Hed, Paulin, Cynthia B J, Heshmati, Yaser, Hagenkort, Anna, Kutzner, Juliane, Page, Brent D G, Calderón-Montaño, José M, Loseva, Olga, Jemth, Ann-Sofie, Bulli, Lorenzo, Axelsson, Hanna, Tesi, Bianca, Valerie, Nicholas C K, Höglund, Andreas, Bladh, Julia, Wiita, Elisée, Sundin, Mikael, Uhlin, Michael, Rassidakis, Georgios, Heyman, Mats, Tamm, Katja Pokrovskaja, Warpman-Berglund, Ulrika, Walfridsson, Julian, Lehmann, Sören, Grandér, Dan, Lundbäck, Thomas, Kogner, Per, Henter, Jan-Inge, Helleday, Thomas, Schaller, Torsten

“…The therapeutic response of acute myelogenous leukemia to the nucleoside analog ara-C is controlled by SAMHD1, an enzyme that hydrolyzes the activemetabolite…”
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All-photonic kinase inhibitors: light-controlled release-and-report inhibition by Fleming, Cassandra L, Benitez-Martin, Carlos, Bernson, Elin, Xu, Yongjin, Kristenson, Linnea, Inghardt, Tord, Lundbck, Thomas, Thorn, Fredrik B, Grtli, Morten, Andrasson, Joakim

“…Light-responsive molecular tools targeting kinases affords one the opportunity to study the underlying cellular function of selected kinases. In efforts to…”
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Design and development of photoswitchable DFG-Out RET kinase inhibitors by Xu, Yongjin, Gao, Chunxia, Andreasson, Måns, Håversen, Liliana, Carrasco, Marta P., Fleming, Cassandra, Lundbäck, Thomas, Andréasson, Joakim, Grøtli, Morten

“…REarranged during Transfection (RET) is a transmembrane receptor tyrosine kinase that is required for development of multiple human tissues, but which is also…”
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A Fully Integrated Assay Panel for Early Drug Metabolism and Pharmacokinetics Profiling by Wernevik, Johan, Bergström, Fredrik, Novén, Anna, Hulthe, Johan, Fredlund, Linda, Addison, Dan, Holmgren, Jan, Strömstedt, Per-Erik, Rehnström, Erika, Lundböck, Thomas

“…Evaluation and optimization of physicochemical and metabolic properties of compounds are a crucial component of the drug development process. Continuous access…”
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A high content screening assay for discovery of antimycobacterial compounds based on primary human macrophages infected with virulent Mycobacterium tuberculosis by Kalsum, Sadaf, Otrocka, Magdalena, Andersson, Blanka, Welin, Amanda, Schön, Thomas, Jenmalm-Jensen, Annika, Lundbäck, Thomas, Lerm, Maria

“…Drug resistance in Mycobacterium tuberculosis is an emerging threat that makes the discovery of new candidate drugs a priority. In particular, drugs with high…”
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Structure–Activity Relationships of Synthetic Cordycepin Analogues as Experimental Therapeutics for African Trypanosomiasis by Vodnala, Suman K, Lundbäck, Thomas, Yeheskieli, Esther, Sjöberg, Birger, Gustavsson, Anna-Lena, Svensson, Richard, Olivera, Gabriela C, Eze, Anthonius A, de Koning, Harry P, Hammarström, Lars G. J, Rottenberg, Martin E

“…Novel methods for treatment of African trypanosomiasis, caused by infection with Trypanosoma brucei are needed. Cordycepin (3′-deoxyadenosine, 1a) is a…”
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Virtual Screening for Transition State Analogue Inhibitors of IRAP Based on Quantum Mechanically Derived Reaction Coordinates by Svensson, Fredrik, Engen, Karin, Lundbäck, Thomas, Larhed, Mats, Sköld, Christian

“…Transition state and high energy intermediate mimetics have the potential to be very potent enzyme inhibitors. In this study, a model of peptide hydrolysis in…”
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Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors by Stefaniak, Jakub, Lewis, Andrew M, Conole, Daniel, Galan, Sébastien R. G, Bataille, Carole J. R, Wynne, Graham M, Castaldi, M. Paola, Lundbäck, Thomas, Russell, Angela J, Huber, Kilian V. M

“…Targeting the protein–protein interaction between p53 and MDM2/MDMX (MDM4) represents an attractive anticancer strategy for the treatment of p53-competent…”
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