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Publications

  • Fanti, R. C., Vasconcelos, S. N. S., Catta-Preta, C. M. C., Sullivan, J. R., Riboldi, G. P., dos Reis, C. v., Ramos, P. Z., Edwards, A. M., Behr, M. A., & Couñago, R. M. (2022). A Target Engagement Assay to Assess Uptake, Potency, and Retention of Antibiotics in Living Bacteria. ACS Infectious Diseases. https://doi.org/10.1021/acsinfecdis.2c00073
  • Lins, É. M., Oliveira, N. C. M., Reis, O., Ferrasa, A., Herai, R., Muotri, A. R., Massirer, K. B., & Bengtson, M. H. (2022). Genome-wide translation control analysis of developing human neurons. Molecular Brain, 15(1), 55. https://doi.org/10.1186/s13041-022-00940-9
  • Wu, Qin, David Y. Nie, Wail Ba-alawi, YiShuai Ji, ZiWen Zhang, Jennifer Cruickshank, Jillian Haight, et al. 2022. “PRMT Inhibition Induces a Viral Mimicry Response in Triple-Negative Breast Cancer.” Nature Chemical Biology, May. https://doi.org/10.1038/s41589-022-01024-4.
  • Segretti, Natanael D., Jéssica E. Takarada, Marcos A. Ferreira, André da Silva Santiago, Bruno V.M. Teodoro, Mariana C.F.C.B. Damião, Paulo H. Godoi, et al. 2022. “Discovery of Novel Benzothiophene Derivatives as Potent and Narrow Spectrum Inhibitors of DYRK1A and DYRK1B.” Bioorganic & Medicinal Chemistry Letters 68 (July): 128764. https://doi.org/10.1016/j.bmcl.2022.128764.
  • Papes, Fabio, Antonio P. Camargo, Janaina S. de Souza, Vinicius M. A. Carvalho, Ryan A. Szeto, Erin LaMontagne, José R. Teixeira, et al. 2022. “Transcription Factor 4 Loss-of-Function Is Associated with Deficits in Progenitor Proliferation and Cortical Neuron Content.” Nature Communications 13 (1): 2387. https://doi.org/10.1038/s41467-022-29942-w.
  • Ricardo, Ricardo A., André da Silva Santiago, Martin P. Schwalm, Zexi Hu, Caio v. dos Reis, Jessica E. Takarada, Priscila Mezzomo, et al. 2022. “Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.” Journal of Medicinal Chemistry 65 (4). https://doi.org/10.1021/acs.jmedchem.1c01165.
  • Scott, Fiona, Angela M. Fala, Jessica E. Takarada, Mihaela P. Ficu, Lewis E. Pennicott, Tristan D. Reuillon, Rafael M. Couñago, Katlin B. Massirer, Jonathan M. Elkins, and Simon E. Ward. 2022. “Development of Dihydropyrrolopyridinone-Based PKN2/PRK2 Chemical Tools to Enable Drug Discovery.” Bioorganic and Medicinal Chemistry Letters 60. https://doi.org/10.1016/j.bmcl.2022.128588.
  • Eduful, Benjamin J., Sean N. O’Byrne, Louisa Temme, Christopher R. M. Asquith, Yi Liang, Alfredo Picado, Joseph R. Pilotte, et al. 2021. “Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes.” Journal of Medicinal Chemistry 64 (15): 10849–77. https://doi.org/10.1021/acs.jmedchem.0c02274.
  • Ferreira, Tiago R., Rafael M. Couñago, and Nilmar S. Moretti. 2021. “Raising the Bar(-Seq) in Leishmania Genetic Screens.” Trends in Parasitology 37 (5): 367–69. https://doi.org/10.1016/j.pt.2021.03.002.
  • Cabarca, Sindy, Maximilia Frazão de Souza, Andrew Albert de Oliveira, Gabriel S. Vignoli Muniz, M. Teresa Lamy, Caio Vinicius dos Reis, Jessica Takarada, et al. 2021. “Structure of the Mycobacterium Tuberculosis CPknF and Conformational Changes Induced in Forkhead-Associated Regulatory Domains.” Current Research in Structural Biology 3: 165–78. https://doi.org/10.1016/j.crstbi.2021.07.001.
  • Oliveira, Natássia Cristina Martins, Érico Moreto Lins, Katlin Brauer Massirer, and Mário Henrique Bengtson. 2021. “Translational Control during Mammalian Neocortex Development and Postembryonic Neuronal Function.” Seminars in Cell & Developmental Biology 114 (June): 36–46. https://doi.org/10.1016/j.semcdb.2020.09.006.
  • Riboldi, Gustavo P., Rachael Zigweid, Peter J. Myler, Stephen J. Mayclin, Rafael M. Couñago, and Bart L. Staker. 2021. “Identification of P218 as a Potent Inhibitor of Mycobacterium Ulcerans DHFR.” RSC Medicinal Chemistry 12 (1): 103–9. https://doi.org/10.1039/D0MD00303D.
  • Sachamitr, Patty, Jolene C. Ho, Felipe E. Ciamponi, Wail Ba-Alawi, Fiona J. Coutinho, Paul Guilhamon, Michelle M. Kushida, et al. 2021. “PRMT5 Inhibition Disrupts Splicing and Stemness in Glioblastoma.” Nature Communications 12 (1): 979. https://doi.org/10.1038/s41467-021-21204-5.
  • Alves, Fernando Rodrigues de Sá, Rafael M. Couñago, and Stefan Laufer. 2020. “Chemical Space Exploration of Oxetanes.” International Journal of Molecular Sciences 21 (21): 8199. https://doi.org/10.3390/ijms21218199.
  • Aquino, Bruno, Viviane C. H. da Silva, Katlin B. Massirer, and Paulo Arruda. 2020. “Crystal Structure of DRIK1, a Stress-Responsive Receptor-like Pseudokinase, Reveals the Molecular Basis for the Absence of ATP Binding.” BMC Plant Biology 20 (1): 158. https://doi.org/10.1186/s12870-020-2328-3.
  • Asquith, Christopher R. M., Tuomo Laitinen, James M. Bennett, Carrow I. Wells, Jonathan M. Elkins, William J. Zuercher, Graham J. Tizzard, and Antti Poso. 2020. “Design and Analysis of the 4‐Anilinoquin(Az)Oline Kinase Inhibition Profiles of GAK/SLK/STK10 Using Quantitative Structure‐Activity Relationships.” ChemMedChem 15 (1): 26–49. https://doi.org/10.1002/cmdc.201900521.
  • Scott, Fiona, Angela M. Fala, Lewis E. Pennicott, Tristan D. Reuillon, Katlin B. Massirer, Jonathan M. Elkins, and Simon E. Ward. 2020. “Development of 2-(4-Pyridyl)-Benzimidazoles as PKN2 Chemical Tools to Probe Cancer.” Bioorganic & Medicinal Chemistry Letters 30 (8): 127040. https://doi.org/10.1016/j.bmcl.2020.127040.
  • Silva, Suélen Fernandes, Angélica Hollunder Klippel, Priscila Zonzini Ramos, André da Silva Santiago, Sandro Roberto Valentini, Mario Henrique Bengtson, Katlin Brauer Massirer, Elizabeth Bilsland, Rafael Miguez Couñago, and Cleslei Fernando Zanelli. 2020. “Structural Features and Development of an Assay Platform of the Parasite Target Deoxyhypusine Synthase of Brugia Malayi and Leishmania Major.” PLOS Neglected Tropical Diseases 14 (10): e0008762. https://doi.org/10.1371/journal.pntd.0008762.
  • Wells, Carrow, Rafael M. Couñago, Juanita C. Limas, Tuanny L. Almeida, Jeanette Gowen Cook, David H. Drewry, Jonathan M. Elkins, et al. 2020. “SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.” ACS Medicinal Chemistry Letters 11 (3): 340–45. https://doi.org/10.1021/acsmedchemlett.9b00399.
  • Barreto, Pedro, Rafael M. Couñago, and Paulo Arruda. 2020. “Mitochondrial Uncoupling Protein-Dependent Signaling in Plant Bioenergetics and Stress Response.” Mitochondrion 53 (July): 109–20. https://doi.org/10.1016/j.mito.2020.05.001.
  • O’Byrne, Sean N., John W. Scott, Joseph R. Pilotte, André da S. Santiago, Christopher G. Langendorf, Jonathan S. Oakhill, Benjamin J. Eduful, et al. 2020. “In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.” Molecules 25 (2): 325. https://doi.org/10.3390/molecules25020325.
  • De-Souza, Evandro A, Henrique Camara, Willian G Salgueiro, Raíssa P Moro, Thiago L Knittel, Guilherme Tonon, Silas Pinto, et al. 2019. “RNA Interference May Result in Unexpected Phenotypes in Caenorhabditis Elegans.” Nucleic Acids Research 47 (8): 3957–69. https://doi.org/10.1093/nar/gkz154.
  • Verdonck, Sven, Szu-Yuan Pu, Fiona J. Sorrell, Jon M. Elkins, Mathy Froeyen, Ling-Jie Gao, Laura I. Prugar, et al. 2019. “Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-Pyrrolo[2,3- b ]Pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.” Journal of Medicinal Chemistry 62 (12): 5810–31. https://doi.org/10.1021/acs.jmedchem.9b00136.
  • Serafim, Ricardo A. M., Fernando H. de Souza Gama, Luiz A. Dutra, Caio v. dos Reis, Stanley N. S. Vasconcelos, André da Silva Santiago, Jéssica E. Takarada, et al. 2019. “Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2.” ACS Medicinal Chemistry Letters 10 (9): 1266–71. https://doi.org/10.1021/acsmedchemlett.9b00082.
  • Sorrell, Fiona J., Lena Marie Kilian, and Jonathan M. Elkins. 2019. “Solution Structures and Biophysical Analysis of Full-Length Group A PAKs Reveal They Are Monomeric and Auto-Inhibited in Cis.” Biochemical Journal 476 (7): 1037–51. https://doi.org/10.1042/BCJ20180867
  • Toledo, Ian de, Thiago A. Grigolo, James M. Bennett, Jonathan M. Elkins, and Ronaldo A. Pilli. 2019. “Modular Synthesis of Di- and Trisubstituted Imidazoles from Ketones and Aldehydes: A Route to Kinase Inhibitors.” The Journal of Organic Chemistry 84 (21): 14187–201. https://doi.org/10.1021/acs.joc.9b01844.
  • Wang, Jing, Thibault Varin, Michal Vieth, and Jonathan M. Elkins. 2019. “Crystal Structure of Human RIOK2 Bound to a Specific Inhibitor.” Open Biology 9 (4): 190037. https://doi.org/10.1098/rsob.190037.
  • Abdul Azeez, Kamal R., Sneha Chatterjee, Channing Yu, Todd R. Golub, Frank Sobott, and Jonathan M. Elkins. 2019. “Structural Mechanism of Synergistic Activation of Aurora Kinase B/C by Phosphorylated INCENP.” Nature Communications 10 (1): 3166. https://doi.org/10.1038/s41467-019-11085-0.
  • Agajanian, Megan J., Matthew P. Walker, Alison D. Axtman, Roberta R. Ruela-de-Sousa, D. Stephen Serafin, Alex D. Rabinowitz, David M. Graham, et al. 2019. “WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.” Cell Reports 26 (1): 79-93.e8. https://doi.org/10.1016/j.celrep.2018.12.023.
  • Alam, Mahmood M., Ana Sanchez-Azqueta, Omar Janha, Erika L. Flannery, Amit Mahindra, Kopano Mapesa, Aditya B. Char, et al. 2019. “Validation of the Protein Kinase Pf CLK3 as a Multistage Cross-Species Malarial Drug Target.” Science 365 (6456). https://doi.org/10.1126/science.aau1682.
  • Asquith, Christopher R. M., James M. Bennett, Lianyong Su, Tuomo Laitinen, Jonathan M. Elkins, Julie E. Pickett, Carrow I. Wells, Zengbiao Li, Timothy M. Willson, and William J. Zuercher. 2019. “Towards the Development of an In Vivo Chemical Probe for Cyclin G Associated Kinase (GAK).” Molecules 24 (22): 4016. https://doi.org/10.3390/molecules24224016.
  • Asquith, Christopher R. M., Benedict-Tilman Berger, Jing Wan, James M. Bennett, Stephen J. Capuzzi, Daniel J. Crona, David H. Drewry, et al. 2019. “SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).” Journal of Medicinal Chemistry 62 (5): 2830–36. https://doi.org/10.1021/acs.jmedchem.8b01213.
  • Barbosa, Éverton de Almeida Alves, Thiago Vargas Seraphim, César Augusto Gandin, Leilane Ferreira Teixeira, Ronni Anderson Gonçalves da Silva, Germanna L. Righetto, Kaliandra De Almeida Goncalves, et al. 2019. “Insights into the Full-Length SRPK2 Structure and Its Hydrodynamic Behavior.” International Journal of Biological Macromolecules 137 (September): 205–14. https://doi.org/10.1016/j.ijbiomac.2019.06.135.
  • Righetto, Germanna Lima, Dev Sriranganadane, Levon Halabelian, Carla G. Chiodi, Jonathan M. Elkins, Katlin B. Massirer, Opher Gileadi, Marcelo Menossi, and Rafael M. Couñago. 2019. “The C-Terminal Domains SnRK2 Box and ABA Box Have a Role in Sugarcane SnRK2s Auto-Activation and Activity.” Frontiers in Plant Science 10 (September). https://doi.org/10.3389/fpls.2019.01105.
  • Profeta, Gerson S., Caio v. dos Reis, André da S. Santiago, Paulo H. C. Godoi, Angela M. Fala, Carrow I. Wells, Roger Sartori, et al. 2019. “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.” Scientific Reports 9 (1): 16452. https://doi.org/10.1038/s41598-019-52795-1.
  • Santiago, André da Silva, Rafael M. Couñago, Priscila Zonzini Ramos, Paulo H. C. Godoi, Katlin B. Massirer, Opher Gileadi, and Jonathan M. Elkins. 2018. “Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors.” Scientific Reports 8 (1): 14800. https://doi.org/10.1038/s41598-018-33043-4.
  • Tosarini, Thalita Ravazo, Priscila Zonzini Ramos, Gerson Souza Profeta, Renata Moro Baroni, Katlin B. Massirer, Rafael M. Couñago, and Jorge M.C. Mondego. 2018. “Cloning, Expression and Purification of Kinase Domains of Cacao PR-1 Receptor-like Kinases.” Protein Expression and Purification 146 (June): 78–84. https://doi.org/10.1016/j.pep.2018.01.004.
  • Wells, C. I., N. R. Kapadia, R. M. Couñago, and D. H. Drewry. 2018. “In Depth Analysis of Kinase Cross Screening Data to Identify Chemical Starting Points for Inhibition of the Nek Family of Kinases.” MedChemComm 9 (1): 44–66. https://doi.org/10.1039/C7MD00510E.
  • Asquith, Christopher, Paulo Godoi, Rafael Couñago, Tuomo Laitinen, John Scott, Christopher Langendorf, Jonathan Oakhill, et al. 2018. “1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.” Molecules 23 (5): 1221. https://doi.org/10.3390/molecules23051221.
  • Axtman, A. D., R. Couñago, D. H. Drewry, M. B. Robers, and C. I. Wells. 2018. “CHAPTER 10. Drugging the Kinome.” In , 253–80. https://doi.org/10.1039/9781788013093-00253.
  • Pinto, Silas, Vitor N. Sato, Evandro A. De-Souza, Rafael C. Ferraz, Henrique Camara, Ana Paula F. Pinca, Diego R. Mazzotti, et al. 2018. “Enoxacin Extends Lifespan of C. Elegans by Inhibiting MiR-34-5p and Promoting Mitohormesis.” Redox Biology 18 (September): 84–92. https://doi.org/10.1016/j.redox.2018.06.006.
  • Aquino, Bruno, Rafael M. Couñago, Natalia Verza, Lucas M. Ferreira, Katlin B. Massirer, Opher Gileadi, and Paulo Arruda. 2017. “Structural Characterization of Maize SIRK1 Kinase Domain Reveals an Unusual Architecture of the Activation Segment.” Frontiers in Plant Science 8 (May). https://doi.org/10.3389/fpls.2017.00852.
  • Couñago, Rafael M., Charles K. Allerston, Pavel Savitsky, Hatylas Azevedo, Paulo H. Godoi, Carrow I. Wells, Alessandra Mascarello, et al. 2017. “Structural Characterization of Human Vaccinia-Related Kinases (VRK) Bound to Small-Molecule Inhibitors Identifies Different P-Loop Conformations.” Scientific Reports 7 (1): 7501. https://doi.org/10.1038/s41598-017-07755-y.
  • Melo-Hanchuk, Talita D., Priscila Ferreira Slepicka, Gabriela Vaz Meirelles, Fernanda Luisa Basei, Diogo Ventura Lovato, Daniela Campos Granato, Bianca Alves Pauletti, et al. 2017. “NEK1 Kinase Domain Structure and Its Dynamic Protein Interactome after Exposure to Cisplatin.” Scientific Reports 7 (1): 5445. https://doi.org/10.1038/s41598-017-05325-w.
  • Pena, Izabella Agostinho, Lygia Azevedo Marques, Ângelo B.A. Laranjeira, José A. Yunes, Marcos N. Eberlin, Alex MacKenzie, and Paulo Arruda. 2017. “Mouse Lysine Catabolism to Aminoadipate Occurs Primarily through the Saccharopine Pathway; Implications for Pyridoxine Dependent Epilepsy (PDE).” Biochimica et Biophysica Acta (BBA) – Molecular Basis of Disease 1863 (1): 121–28. https://doi.org/10.1016/j.bbadis.2016.09.006.
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