Search Results - "CZECH, Joerg"
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Novel Inhibitors of Nicotinamide- N -Methyltransferase for the Treatment of Metabolic Disorders
Published in Molecules (Basel, Switzerland) (13-02-2021)“…Nicotinamide- -methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from -adenosyl-methionine (SAM) to nicotinamide (Nam)…”
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Novel tricyclic small molecule inhibitors of Nicotinamide N-methyltransferase for the treatment of metabolic disorders
Published in Scientific reports (14-09-2022)“…Nicotinamide N-methyltransferase (NNMT) is a metabolic regulator that catalyzes the methylation of nicotinamide (Nam) using the co-factor…”
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Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
Published in Bioorganic & medicinal chemistry letters (01-03-2018)“…Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic…”
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A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders
Published in Scientific reports (26-02-2018)“…Nicotinamide N-methyltransferase (NNMT) is a cytosolic enzyme that catalyzes the transfer of a methyl group from the co-factor S-adenosyl-L-methionine (SAM)…”
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Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin
Published in Journal of medicinal chemistry (11-06-2015)“…Anabaenopeptins isolated from cyanobacteria were identified as inhibitors of carboxypeptidase TAFIa. Cocrystal structures of these macrocyclic natural product…”
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Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes
Published in Angewandte Chemie International Edition (23-01-2012)“…More than just the sum of its parts: The superadditivity effect of fragment linking on ΔG was quantified by deconstructing two fXa inhibitors with congeneric…”
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Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa)
Published in Journal of medicinal chemistry (27-10-2016)“…Previously disclosed TAFIa inhibitors having a urea zinc-binding motif were used as the starting point for the development of a novel class of highly potent…”
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Isolation, Co-Crystallization and Structure-Based Characterization of Anabaenopeptins as Highly Potent Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa)
Published in Scientific reports (08-09-2016)“…Mature thrombin activatable fibrinolysis inhibitor (TAFIa) is a carboxypeptidase that stabilizes fibrin clots by removing C-terminal arginines and lysines from…”
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Discovery of N‑[4-(1H‑Pyrazolo[3,4‑b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors
Published in ACS medicinal chemistry letters (08-01-2015)“…From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical…”
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A Solid Supported Membrane-Based Technology for Electrophysical Screening of B 0 AT1-Modulating Compounds
Published in SLAS discovery (01-07-2021)“…Classical high-throughput screening (HTS) technologies for the analysis of ionic currents across biological membranes can be performed using…”
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Elucidation of the mechanism enabling tumor selective prodrug monotherapy
Published in Cancer research (Chicago, Ill.) (15-03-1998)“…Elucidation of the mechanism enabling tumor selective PMT in vivo with appropriate glucuronyl-spacer-doxorubicin prodrugs, such as HMR 1826, is important for…”
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Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition
Published in Bioorganic & medicinal chemistry letters (16-07-2004)“…The amidinophenylurea scaffold was earlier shown to provide an excellent template for the synthesis of novel and potent inhibitors of the blood coagulation…”
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Design, synthesis, and structure–activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors
Published in Bioorganic & medicinal chemistry letters (17-04-2003)“…Selective inhibition of coagulation factor VIIa has recently gained attraction as interesting approach towards antithrombotic treatment. Using parallel…”
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Prodrugs of Anthracyclines for Use in Antibody-Directed Enzyme Prodrug Therapy
Published in Journal of medicinal chemistry (10-09-1998)“…A series of new prodrugs of daunorubicin and doxorubicin which are candidates for antibody-directed enzyme prodrug therapy (ADEPT) is reported. These compounds…”
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Innenrücktitelbild: Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein–Ligand Complexes (Angew. Chem. 4/2012)
Published in Angewandte Chemie (23-01-2012)“…Die Superadditivität von Affinitäten beim Verbinden einzelner Fragmente wurde durch systematischen Abbau eines fXa‐Inhibitors quantifiziert. In ihrer Zuschrift…”
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The Change in Research for the Therapy of Tumors
Published in Chimia (01-10-1991)Get full text
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The Change in Research for the Therapy of Tumors
Published in Chimia (01-10-1991)Get full text
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