Paulo H. Godoi
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View article: Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase Open
4-Anilinoquinolines were identified as potent and narrow-spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quin…
View article: Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases
Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases Open
Selective inhibitors of DYRK1A are of interest for the treatment of cancer, Type 2 diabetes and neurological disorders. Optimization of imidazo [1,2-b]pyridazine fragment 1 through structure-activity relationship exploration and in silico …
View article: Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors Open
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neur…
View article: Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations Open
The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of…
View article: The PRP4K Kinase protein overexpression, production, purification and crystallization
The PRP4K Kinase protein overexpression, production, purification and crystallization Open
The Pre-mRNA processing factor 4B Kinase is a serine/threonine kinase responsible for the phosphorylation of essentials proteins of the tri-snRNP complex in the B Complex of the spliceosome in mammals, being that the overexpression of PRP4…
View article: Validation of the protein kinase <i>Pf</i> CLK3 as a multistage cross-species malarial drug target
Validation of the protein kinase <i>Pf</i> CLK3 as a multistage cross-species malarial drug target Open
Targeting parasite's protein kinase Malaria elimination goals are constantly eroded by the challenge of emerging drug and insecticide resistance. Alam et al. have taken established drug targets—CLK protein kinases involved in regulation of…
View article: SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)
SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK) Open
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 control SGC-GAK-1N (14). 11 was highly selective in an in vitro kinome-wide scree…
View article: Structural and binding studies of human CAMKK2 kinase domain bound to small molecule ligands
Structural and binding studies of human CAMKK2 kinase domain bound to small molecule ligands Open
Calcium/Calmodulin-dependent Protein Kinase Kinase 2 (CAMKK2) acts as a signaling hub, receiving signals from various regulatory pathways and decoding them via phosphorylation of downstream protein kinases - such as AMPK (AMP-activated pro…
View article: SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK) Open
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 control SGC-GAK-1N ( 14 ). SGC-GAK-1 is highly selective in a kinome-wide scree…
View article: 1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors
1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors Open
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-…
View article: Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors
Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors Open
The calcium/calmodulin-dependent protein kinases (CAMKKs) are upstream activators of CAMK1 and CAMK4 signalling and have important functions in neural development, maintenance and signalling, as well as in other aspects of biology such as …
View article: AAK1 inhibits WNT signaling by promoting clathrin-mediated endocytosis of LRP6
AAK1 inhibits WNT signaling by promoting clathrin-mediated endocytosis of LRP6 Open
β-catenin-dependent WNT signal transduction governs normal development and adult tissue homeostasis. Inappropriate pathway activity mediates a vast array of human diseases, including bone density disorders, neurodegeneration and cancer. Al…
View article: Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
Identification and Optimization of 4‐Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase Open
4‐Anilinoquinolines were identified as potent and narrow‐spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4‐anilino group and the 6,7‐quin…
View article: Sgc-Gak-1: A Chemical Probe Candidate For The Understudied Kinase Gak
Sgc-Gak-1: A Chemical Probe Candidate For The Understudied Kinase Gak Open
SGC-GAK-1 is presented as a chemical probe for the understudied cyclin G associated kinase (GAK). SGC-GAK-1 is potent and shows submicromolar cellular target engagement with GAK. The compound shows > 30-fold selectivity relative to all oth…
View article: Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations Open
The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of…
View article: Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase Open
4-Anilinoquinolines were identified as potent and narrow spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quin…
View article: Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations Open
The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of…
View article: CCDC 1534020: Experimental Crystal Structure Determination
CCDC 1534020: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1534023: Experimental Crystal Structure Determination
CCDC 1534023: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1534018: Experimental Crystal Structure Determination
CCDC 1534018: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1534022: Experimental Crystal Structure Determination
CCDC 1534022: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1534017: Experimental Crystal Structure Determination
CCDC 1534017: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1534021: Experimental Crystal Structure Determination
CCDC 1534021: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …