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Protein Kinase Chemical Biology Center: supporting drug development through open-access research

Grant number: 13/50724-5
Support type:Research Grants - Research Partnership for Technological Innovation - PITE
Duration: March 01, 2015 - February 29, 2020
Field of knowledge:Interdisciplinary Subjects
Principal researcher:Paulo Arruda
Grantee:Paulo Arruda
Home Institution: Instituto de Biologia (IB). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
City: Campinas
Partner institutions: Structural Genomics Consortium
Pesquisadores principais:
Aníbal Eugênio Vercesi ; Licio Augusto Velloso ; Mario Jose Abdalla Saad ; Paulo Mazzafera ; Ronaldo Aloise Pilli
Associated grant(s):15/50024-9 - An integrative analysis of protein kinases in childhood acute lymphoblastic leukemia, AP.R SPRINT
Associated scholarship(s):19/18771-0 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research, BP.TT
19/02059-9 - PROTEIN KINASE CHEMICAL BIOLOGY CENTER: SUPPORTING DRUG DEVELOPMENT THROUGH OPEN-ACCESS RESEARCH, BP.TT
19/02158-7 - PROTEIN KINASE CHEMICAL BIOLOGY CENTER: SUPPORTING DRUG DEVELOPMENT THROUGH OPEN-ACCESS RESEARCH, BP.TT
+ associated scholarships 19/00202-9 - PROTEIN KINASE CHEMICAL BIOLOGY CENTER: SUPPORTING DRUG DEVELOPMENT THROUGH OPEN-ACCESS RESEARCH, BP.TT
18/09342-5 - Protein kinase Chemical Biology center supporting drug development through open access research, BP.TT
18/11871-6 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research, BP.TT
18/07844-3 - Protein kinase chemical biology center: supporting drug development through open-access research, BP.TT
18/02528-6 - Protein kinase chemical biology center: supporting drug development through open-access research, BP.TT
18/03063-7 - Protein kinase chemical biology center: supporting drug development through open-access research, BP.TT
18/03359-3 - Protein kinase chemical biology center: supporting drug development through open-access research, BP.TT
17/21179-0 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research, BP.TT
17/19605-0 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research, BP.TT
17/08535-1 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research, BP.TT - associated scholarships

Abstract

Mais de 500 proteínas quinases estão presentes no genoma humano, atuando como chaves regulatórias de praticamente todos os processos fisiológicos do organismo humano. As quinases podem ser moduladas através de pequenas moléculas químicas altamente potentes. No entanto, apesar de sua importância e adequação para a descoberta de fármacos, a maioria das pesquisas acadêmicas e farmacêuticas tem se concentrado em apenas uma pequena fração de quinases. Ou seja, a maioria das quinases são “sub-exploradas”. Estas quinases sub-exploradas representam uma rica fonte de inovação em biologia e são o foco deste projeto de pesquisa. A UNICAMP, se propõe a entrar em parceria com o Structural Genomics Consortium (SGC) e conjuntamente trabalhar em uma lista de alvos contendo 26 quinases sub-exploradas envolvidas na regulação do splicing de RNA e da biologia da cromatina – alvos estes implicados em doenças neurológicas, angiogênese e câncer. A SGC-UNICAMP tem como objetivo a geração de pequenas moléculas inibidoras seletivas (“sondas químicas”), para pelo menos oito (8) quinases dessa lista. Para atingirmos esse objetivo, iremos estabelecer uma plataforma de “química medicinal guiada por estruturas” na UNICAMP, com financiamento e aconselhamento dos nossos oito parceiros da indústria farmacêutica e de um conselho consultivo externo composto por líderes globais em biologia química. A plataforma, em colaboração com uma rede de acadêmicos de Campinas e mundial, irá caracterizar as sondas (i) em ensaios bioquímicos, com o objetivo de determinar a potência e a seletividade, e (ii) em ensaios celulares para demonstrar “acoplamento no alvo” no interior das células. Uma vez que as sondas químicas atingirem rigorosos critérios de qualificação, iremos disponibilizá-los para cientistas brasileiros e internacionais, sem restrição de uso. A disponibilidade dessas sondas químicas irá possibilitar a descoberta de novas vias biológicas e identificação de novas oportunidades de intervenção terapêutica. Ao estabelecer esta plataforma química de acesso aberto, temos como objetivo tornar a UNICAMP em um dos centros mundiais em biologia química de quinases. (AU)

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Scientific publications (23)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
BARRETO, PEDRO; COUNAGO, RAFAEL M.; ARRUDA, PAULO. Mitochondrial uncoupling protein-dependent signaling in plant bioenergetics and stress response. MITOCHONDRION, v. 53, p. 109-120, . (14/50897-0, 16/23218-0, 13/50724-5)
JAMIESON, SAM A.; RUAN, ZHENG; BURGESS, ABIGAIL E.; CURRY, JACK R.; MCMILAN, HAMISH D.; BREWSTER, JODI L.; DUNBIER, ANITA K.; AXTMAN, ALISON D.; KANNAN, NATARAJAN; MACE, PETER D.. Substrate binding allosterically relieves autoinhibition of the pseudokinase TRIB1. Science Signaling, v. 11, n. 549, . (13/50724-5)
SANTIAGO, ANDRE DA SILVA; COUNAGO, RAFAEL M.; RAMOS, PRISCILA ZONZINI; GODOI, PAULO H. C.; MASSIRER, KATLIN B.; GILEADI, OPHER; ELKINS, JONATHAN M.. Structural Analysis of Inhibitor Binding to CAMKK1 Identifies Features Necessary for Design of Specific Inhibitors. SCIENTIFIC REPORTS, v. 8, . (13/50724-5)
KRAHN, ANDREA I.; WELLS, CARROW; DREWRY, DAVID H.; BEITEL, LENORE K.; DURCAN, THOMAS M.; AXTMAN, ALISON D.. Defining the Neural Kinome: Strategies and Opportunities for Small Molecule Drug Discovery to Target Neurodegenerative Diseases. ACS Chemical Neuroscience, v. 11, n. 13, p. 1871-1886, . (13/50724-5)
AQUINO, BRUNO; COUNAGO, RAFAEL M.; VERZA, NATALIA; FERREIRA, LUCAS M.; MASSIRER, KATLIN B.; GILEADI, OPHER; ARRUDA, PAULO. Structural Characterization of Maize SIRK1 Kinase Domain Reveals an Unusual Architecture of the Activation Segment. FRONTIERS IN PLANT SCIENCE, v. 8, . (13/50724-5)
RIGHETTO, GERMANNA LIMA; SRIRANGANADANE, DEV; HALABELIAN, LEVON; CHIODI, CARLA G.; ELKINS, JONATHAN M.; MASSIRER, KATLIN B.; GILEADI, OPHER; MENOSSI, MARCELO; COUNAGO, RAFAEL M.. The C-Terminal Domains SnRK2 Box and ABA Box Have a Role in Sugarcane SnRK2s Auto-Activation and Activity. FRONTIERS IN PLANT SCIENCE, v. 10, . (13/50724-5)
SCOTT, FIONA; FALA, ANGELA M.; PENNICOTT, LEWIS E.; REUILLON, TRISTAN D.; MASSIRER, KATLIN B.; ELKINS, JONATHAN M.; WARD, SIMON E.. Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer. Bioorganic & Medicinal Chemistry Letters, v. 30, n. 8, . (14/50897-0, 13/50724-5)
RIBOLDI, GUSTAVO P.; ZIGWEID, RACHAEL; MYLER, PETER J.; MAYCLIN, STEPHEN J.; COUNAGO, RAFAEL M.; STAKER, BART L.. Identification of P218 as a potent inhibitor of Mycobacterium ulcerans DHFR. RSC MEDICINAL CHEMISTRY, v. 12, n. 1, p. 103-109, . (13/50724-5, 14/50897-0)
EDUFUL, BENJAMIN J.; O'BYRNE, SEAN N.; TEMME, LOUISA; ASQUITH, CHRISTOPHER R. M.; LIANG, YI; PICADO, ALFREDO; PILOTTE, JOSEPH R.; HOSSAIN, MOHAMMAD ANWAR; WELLS, I, CARROW; ZUERCHER, WILLIAM J.; et al. Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes. Journal of Medicinal Chemistry, v. 64, n. 15, p. 10849-10877, . (13/50724-5, 14/50897-0, 19/14275-8)
HENDERSON, SCOTT H.; SORRELL, FIONA; BENNETT, JAMES; FEDOROV, OLEG; HANLEY, MARCUS T.; GODOI, PAULO H.; DE SOUSA, ROBERTA RUELA; ROBINSON, SEAN; ASHALL-KELLY, ALEXANDER; NAVRATILOVA, IVA HOPKINS; et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. Journal of Medicinal Chemistry, v. 64, n. 15, p. 11709-11728, . (16/17469-0, 13/50724-5)
SILVA, SUELEN FERNANDES; KLIPPEL, ANGELICA HOLLUNDER; RAMOS, PRISCILA ZONZINI; SANTIAGO, ANDREE DA SILVA; VALENTINI, SANDRO ROBERTO; BENGTSON, MARIO HENRIQUE; MASSIRER, KATLIN BRAUER; BILSLAND, ELIZABETH; COUNAGO, RAFAEL MIGUEZ; ZANELLI, CLESLEI FERNANDO. Structural features and development of an assay platform of the parasite target deoxyhypusine synthase of Brugia malayi and Leishmania major. PLoS Neglected Tropical Diseases, v. 14, n. 10, . (14/50897-0, 18/16672-1, 16/16970-7, 19/14275-8, 15/03553-6, 13/50724-5)
ALVES, FERNANDO RODRIGUES DE SA; COUNAGO, RAFAEL M.; LAUFER, STEFAN. Chemical Space Exploration of Oxetanes. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, v. 21, n. 21, . (14/50897-0, 13/50724-5)
O'BYRNE, SEAN N.; SCOTT, JOHN W.; PILOTTE, JOSEPH R.; SANTIAGO, ANDRE DA S.; LANGENDORF, CHRISTOPHER G.; OAKHILL, JONATHAN S.; EDUFUL, BENJAMIN J.; COUNAGO, RAFAEL M.; WELLS, CARROW I.; ZUERCHER, WILLIAM J.; et al. In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds. Molecules, v. 25, n. 2, . (13/50724-5, 14/50897-0, 19/14275-8)
WELLS, CARROW; COUNAGO, RAFAEL M.; LIMAS, JUANITA C.; ALMEIDA, TUANNY L.; COOK, JEANETTE GOWEN; DREWRY, DAVID H.; ELKINS, JONATHAN M.; GILEADI, OPHER; KAPADIA, NIRAV R.; LORENTE-MACIAS, ALVARO; et al. SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K. ACS Medicinal Chemistry Letters, v. 11, n. 3, p. 340-345, . (14/50897-0, 13/50724-5, 16/17469-0)
HERNEISEN, ALICE L.; SIDIK, SAIMA M.; MARKUS, BENEDIKT M.; DREWRY, DAVID H.; ZUERCHER, WILLIAM J.; LOURIDO, SEBASTIAN. Identifying the Target of an Antiparasitic Compound in Toxoplasma Using Thermal Proteome Profiling. ACS Chemical Biology, v. 15, n. 7, p. 1801-1807, . (13/50724-5, 16/17469-0)
WELLS, CARROW I.; VASTA, JAMES D.; CORONA, CESEAR R.; WILKINSON, JENNIFER; ZIMPRICH, CHAD A.; INGOLD, MORGAN R.; PICKETT, JULIE E.; DREWRY, DAVID H.; PUGH, KATHRYN M.; SCHWINN, MARIE K.; et al. Quantifying CDK inhibitor selectivity in live cells. NATURE COMMUNICATIONS, v. 11, n. 1, . (14/50897-0, 13/50724-5, 16/17469-0)
ALAM, MAHMOOD M.; SANCHEZ-AZQUETA, ANA; JANHA, OMAR; FLANNERY, ERIKA L.; MAHINDRA, AMIT; MAPESA, KOPANO; CHAR, ADITYA B.; SRIRANGANADANE, DEV; BRANCUCCI, NICOLAS M. B.; ANTONOVA-KOCH, YEVGENIYA; et al. Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science, v. 365, n. 6456, p. 884+, . (13/50724-5)
ALVES BARBOSA, EVERTON DE ALMEIDA; SERAPHIM, THIAGO VARGAS; GANDIN, CESAR AUGUSTO; TEIXEIRA, LEILANE FERREIRA; GONCALVES DA SILVA, RONNI ANDERSON; RIGHETTO, GERMANNA L.; GONCALVES, KALIANDRA DE ALMEIDA; VASCONCELLOS, RAPHAEL DE SOUZA; ALMEIDA, MARCIA ROGERIA; SILVA JUNIOR, ABELARDO; et al. Insights into the full-length SRPK2 structure and its hydrodynamic behavior. International Journal of Biological Macromolecules, v. 137, p. 205-214, . (14/07206-6, 13/50724-5, 11/23110-0, 12/00195-3, 17/03489-1, 12/50161-8, 17/07335-9)
SERAFIM, RICARDO A. M.; DE SOUZA GAMA, FERNANDO H.; DUTRA, LUIZ A.; DOS REIS, CAIO V.; VASCONCELOS, STANLEY N. S.; SANTIAGO, ANDRE DA SILVA; TAKARADA, JESSICA E.; DI PILLO, FULVIA; AZEVEDO, HATYLAS; MASCARELLO, ALESSANDRA; et al. Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2. ACS Medicinal Chemistry Letters, v. 10, n. 9, p. 1266-1271, . (18/03359-3, 18/09475-5, 13/50724-5, 16/25320-6)
PROFETA, GERSON S.; DOS REIS, CAIO V.; SANTIAGO, ANDRE DA S.; GODOI, PAULO H. C.; FALA, ANGELA M.; WELLS, CARROW I.; SARTORI, ROGER; SALMAZO, ANITA P. T.; RAMOS, PRISCILA Z.; MASSIRER, KATLIN B.; et al. 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, v. 9, . (19/14275-8, 14/50897-0, 13/50724-5)
TOSARINI, THALITA RAVAZO; RAMOS, PRISCILA ZONZINI; PROFETA, GERSON SOUZA; BARONI, RENATA MORO; MASSIRER, KATLIN B.; COUNAGO, RAFAEL M.; MONDEGO, JORGE M. C.. Cloning, expression and purification of kinase domains of cacao PR-1 receptor-like kinases. Protein Expression and Purification, v. 146, p. 78-84, . (13/50724-5, 12/07657-2)
AGAJANIAN, MEGAN J.; WALKER, MATTHEW P.; AXTMAN, ALISON D.; RUELA-DE-SOUSA, ROBERTA R.; SERAFIN, D. STEPHEN; RABINOWITZ, ALEX D.; GRAHAM, DAVID M.; RYAN, MEAGAN B.; TAMIR, TIGIST; NAKAMICHI, YUKO; et al. WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. CELL REPORTS, v. 26, n. 1, p. 79+, . (13/50724-5, 16/17469-0)
COUNAGO, RAFAEL M.; ALLERSTON, CHARLES K.; SAVITSKY, PAVEL; AZEVEDO, HATYLAS; GODOI, PAULO H.; WELLS, CARROW I.; MASCARELLO, ALESSANDRA; DE SOUZA GAMA, FERNANDO H.; MASSIRER, KATLIN B.; ZUERCHER, WILLIAM J.; et al. Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations. SCIENTIFIC REPORTS, v. 7, . (13/50724-5)

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