Search Results - "Sippl, Wolfgang"

Editorial for Special Issue-"Early-Stage Drug Discovery: Advances and Challenges" by Sippl, Wolfgang

“…The development of a new drug from the first hit to the launch of an approved product is a complex process that usually take around 12-15 years and costs more…”
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Computational Drug Repurposing: Current Trends by Karaman, Berin, Sippl, Wolfgang

“…Biomedical discovery has been reshaped upon the exploding digitization of data which can be retrieved from a number of sources, ranging from clinical…”
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Activation, regulation, and inhibition of DYRK1A by Becker, Walter, Sippl, Wolfgang

“…Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a protein kinase with diverse functions in neuronal development and adult brain…”
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The Current State of NAD+‐Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets by Schiedel, Matthias, Robaa, Dina, Rumpf, Tobias, Sippl, Wolfgang, Jung, Manfred

“…Sirtuins are NAD+‐dependent protein deacylases that cleave off acetyl, as well as other acyl groups, from the ε‐amino group of lysines in histones and other…”
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Regulation of G2/M Transition by Inhibition of WEE1 and PKMYT1 Kinases by Schmidt, Matthias, Rohe, Alexander, Platzer, Charlott, Najjar, Abdulkarim, Erdmann, Frank, Sippl, Wolfgang

“…In the cell cycle, there are two checkpoint arrests that allow cells to repair damaged DNA in order to maintain genomic integrity. Many cancer cells have…”
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Natural Products as Modulators of Sirtuins by Karaman Mayack, Berin, Sippl, Wolfgang, Ntie-Kang, Fidele

“…Natural products have been used for the treatment of human diseases since ancient history. Over time, due to the lack of precise tools and techniques for the…”
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HDAC8: a multifaceted target for therapeutic interventions by Chakrabarti, Alokta, Oehme, Ina, Witt, Olaf, Oliveira, Guilherme, Sippl, Wolfgang, Romier, Christophe, Pierce, Raymond J, Jung, Manfred

“…Highlights • HDAC8, a unique class I HDAC, recognizes both histone and nonhistone substrates. • HDAC8 is implicated in cancer, schistosomiasis, and Cornelia de…”
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Editorial to Special Issue-"Structure-Activity Relationships (SAR) of Natural Products" by Sippl, Wolfgang, Ntie-Kang, Fidele

“…The topic of structure-activity-relationships (SAR) has recently drawn a lot of attention, and there is increasing interest in natural products (NPs) as a…”
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Histone Acetyltransferase and Deacetylase Inhibitors-New Aspects and Developments by Ibrahim, Hany S, Sippl, Wolfgang

“…Epigenetic processes modulate gene transcription and genomic stability, ensuring proper cell development and differentiation [...]…”
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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) by Schiedel, Matthias, Herp, Daniel, Hammelmann, Sören, Swyter, Sören, Lehotzky, Attila, Robaa, Dina, Oláh, Judit, Ovádi, Judit, Sippl, Wolfgang, Jung, Manfred

“…Here we report the development of a proteolysis targeting chimera (PROTAC) based on the combination of the unique features of the sirtuin rearranging ligands…”
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Comparative Structure-Based Virtual Screening Utilizing Optimized AlphaFold Model Identifies Selective HDAC11 Inhibitor by Baselious, Fady, Hilscher, Sebastian, Robaa, Dina, Barinka, Cyril, Schutkowski, Mike, Sippl, Wolfgang

“…HDAC11 is a class IV histone deacylase with no crystal structure reported so far. The catalytic domain of HDAC11 shares low sequence identity with other HDAC…”
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Selective agonist of TRPML2 reveals direct role in chemokine release from innate immune cells by Plesch, Eva, Chen, Cheng-Chang, Butz, Elisabeth, Scotto Rosato, Anna, Krogsaeter, Einar K, Yinan, Hua, Bartel, Karin, Keller, Marco, Robaa, Dina, Teupser, Daniel, Holdt, Lesca M, Vollmar, Angelika M, Sippl, Wolfgang, Puertollano, Rosa, Medina, Diego, Biel, Martin, Wahl-Schott, Christian, Bracher, Franz, Grimm, Christian

“…Cytokines and chemokines are produced and secreted by a broad range of immune cells including macrophages. Remarkably, little is known about how these…”
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KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases by Simon, Roman P, Robaa, Dina, Alhalabi, Zayan, Sippl, Wolfgang, Jung, Manfred

“…The reversible acetylation of lysines is one of the best characterized epigenetic modifications. Its involvement in many key physiological and pathological…”
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Selective Sirt2 inhibition by ligand-induced rearrangement of the active site by Rumpf, Tobias, Schiedel, Matthias, Karaman, Berin, Roessler, Claudia, North, Brian J., Lehotzky, Attila, Oláh, Judit, Ladwein, Kathrin I., Schmidtkunz, Karin, Gajer, Markus, Pannek, Martin, Steegborn, Clemens, Sinclair, David A., Gerhardt, Stefan, Ovádi, Judit, Schutkowski, Mike, Sippl, Wolfgang, Einsle, Oliver, Jung, Manfred

“…Sirtuins are a highly conserved class of NAD + -dependent lysine deacylases. The human isotype Sirt2 has been implicated in the pathogenesis of cancer,…”
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Exploring aromatic cage flexibility of the histone methyllysine reader protein Spindlin1 and its impact on binding mode prediction: an in silico study by Luise, Chiara, Robaa, Dina, Sippl, Wolfgang

“…Some of the main challenges faced in drug discovery are pocket flexibility and binding mode prediction. In this work, we explored the aromatic cage flexibility…”
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Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants by Marek, Martin, Shaik, Tajith B, Heimburg, Tino, Chakrabarti, Alokta, Lancelot, Julien, Ramos-Morales, Elizabeth, Da Veiga, Cyrielle, Kalinin, Dmitrii, Melesina, Jelena, Robaa, Dina, Schmidtkunz, Karin, Suzuki, Takayoshi, Holl, Ralph, Ennifar, Eric, Pierce, Raymond J, Jung, Manfred, Sippl, Wolfgang, Romier, Christophe

“…Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that represent promising therapeutic targets for the treatment of numerous human…”
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Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors by Rüben, Katharina, Wurzlbauer, Anne, Walte, Agnes, Sippl, Wolfgang, Bracher, Franz, Becker, Walter

“…DYRK1A is a pleiotropic protein kinase with diverse functions in cellular regulation, including cell cycle control, neuronal differentiation, and synaptic…”
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Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors by Senger, Johanna, Melesina, Jelena, Marek, Martin, Romier, Christophe, Oehme, Ina, Witt, Olaf, Sippl, Wolfgang, Jung, Manfred

“…Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of…”
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New chemical tools for probing activity and inhibition of the NAD+-dependent lysine deacylase sirtuin 2 by Swyter, Sören, Schiedel, Matthias, Monaldi, Daria, Szunyogh, Sándor, Lehotzky, Attila, Rumpf, Tobias, Ovádi, Judit, Sippl, Wolfgang, Jung, Manfred

“…Sirtuins are NAD+-dependent protein deacylases capable of cleaving off acetyl as well as other acyl groups from the ɛ-amino group of lysines in histones and…”
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Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors by Vögerl, Katharina, Ong, Nghia, Senger, Johanna, Herp, Daniel, Schmidtkunz, Karin, Marek, Martin, Müller, Martin, Bartel, Karin, Shaik, Tajith B, Porter, Nicholas J, Robaa, Dina, Christianson, David W, Romier, Christophe, Sippl, Wolfgang, Jung, Manfred, Bracher, Franz

“…The phenothiazine system was identified as a favorable cap group for potent and selective histone deacetylase 6 (HDAC6) inhibitors. Here, we report the…”
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