Search Results - "Godoi, Paulo H"
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SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)
Published in Journal of medicinal chemistry (14-03-2019)“…We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK), together with a structurally related negative…”
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WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop
Published in Cell reports (Cambridge) (02-01-2019)“…β-Catenin-dependent WNT signal transduction governs development, tissue homeostasis, and a vast array of human diseases. Signal propagation through a…”
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3
Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
Published in ChemMedChem (08-01-2018)“…4‐Anilinoquinolines were identified as potent and narrow‐spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and…”
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4
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations
Published in Scientific reports (08-08-2017)“…The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular…”
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1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors
Published in Molecules (Basel, Switzerland) (19-05-2018)“…We demonstrate for the first time that 4 -1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using…”
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TR-FRET-based high-throughput screening assay for identification of UBC13 inhibitors
Published in Journal of biomolecular screening (01-02-2012)“…UBC13 is a noncanonical ubiquitin conjugating enzyme (E2) that has been implicated in a variety of cellular signaling processes due to its ability to catalyze…”
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Structure of the Thiazole Biosynthetic Enzyme THI1 from Arabidopsis thaliana
Published in The Journal of biological chemistry (13-10-2006)“…Thiamin pyrophosphate is an essential coenzyme in all organisms that depend on fermentation, respiration or photosynthesis to produce ATP. It is synthesized…”
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Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors
Published in Journal of medicinal chemistry (12-08-2021)“…Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development…”
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Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target
Published in Science (American Association for the Advancement of Science) (30-08-2019)“…Targeting parasite's protein kinaseMalaria elimination goals are constantly eroded by the challenge of emerging drug and insecticide resistance. Alam et al…”
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Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases
Published in European journal of medicinal chemistry (05-04-2024)“…Selective inhibitors of DYRK1A are of interest for the treatment of cancer, Type 2 diabetes and neurological disorders. Optimization of imidazo…”
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Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors
Published in Bioorganic & medicinal chemistry (15-01-2024)“…The dual-specificity protein kinase MKK3 has been implicated in tumor cell proliferation and survival, yet its precise role in cancer remains inconclusive. A…”
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12
Identification and Optimization of 4-Anilinoquinolines as Inhibitors of CyclinG Associated Kinase
Published in ChemMedChem (08-01-2018)“…4-Anilinoquinolines were identified as potent and narrow-spectrum inhibitors of the cyclinG associated kinase (GAK), an important regulator of viral and…”
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13
Discovery of novel benzothiophene derivatives as potent and narrow spectrum inhibitors of DYRK1A and DYRK1B
Published in Bioorganic & medicinal chemistry letters (15-07-2022)“…[Display omitted] The discovery of potent and selective inhibitors for understudied kinases can provide relevant pharmacological tools to illuminate their…”
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Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors
Published in Scientific reports (11-11-2019)“…Calcium/Calmodulin-dependent Protein Kinase Kinase 2 (CAMKK2) acts as a signaling hub, receiving signals from various regulatory pathways and decoding them via…”
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15
Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors
Published in Scientific reports (04-10-2018)“…The calcium/calmodulin-dependent protein kinases (CAMKKs) are upstream activators of CAMK1 and CAMK4 signalling and have important functions in neural…”
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Orphan Nuclear Receptor NR4A1 Binds a Novel Protein Interaction Site on Anti-apoptotic B Cell Lymphoma Gene 2 Family Proteins
Published in The Journal of biological chemistry (01-07-2016)“…B cell lymphoma gene 2 (Bcl-2) family proteins are key regulators of programmed cell death and important targets for drug discovery. Pro-apoptotic and…”
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17
Validation of the protein kinase Pf CLK3 as a multistage cross-species malarial drug target
Published in Science (American Association for the Advancement of Science) (30-08-2019)“…The requirement for next-generation antimalarials to be both curative and transmission-blocking necessitates the identification of previously undiscovered…”
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A TR3/Nur77 peptide-based high-throughput fluorescence polarization screen for small molecule Bcl-B inhibitors
Published in Journal of biomolecular screening (01-08-2008)“…Nuclear receptor TR3/Nur77/NR4A1 binds several antiapoptotic Bcl-2-family proteins (Bcl-B, Bcl-2, Bfl-1) in a non-BH3-dependent manner. A 9-amino-acid peptide…”
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Binding and structural analyses of potent inhibitors of the human Ca 2+ /calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors
Published in Scientific reports (11-11-2019)“…Calcium/Calmodulin-dependent Protein Kinase Kinase 2 (CAMKK2) acts as a signaling hub, receiving signals from various regulatory pathways and decoding them via…”
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A polymorphism in endostatin, an angiogenesis inhibitor, predisposes for the development of prostatic adenocarcinoma
Published in Cancer research (Chicago, Ill.) (15-10-2001)“…We have performed association studies between a novel coding single nucleotide polymorphism (D104N) in endostatin, one of the most potent inhibitors of…”
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