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Progress towards a public chemogenomic set for protein kinases and a call for contributions.
Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM. Drewry DH, et al. Among authors: gileadi o. PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017. PLoS One. 2017. PMID: 28767711 Free PMC article.
The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins.
Gileadi O, Knapp S, Lee WH, Marsden BD, Müller S, Niesen FH, Kavanagh KL, Ball LJ, von Delft F, Doyle DA, Oppermann UC, Sundström M. Gileadi O, et al. J Struct Funct Genomics. 2007 Sep;8(2-3):107-19. doi: 10.1007/s10969-007-9027-2. Epub 2007 Oct 12. J Struct Funct Genomics. 2007. PMID: 17932789 Free PMC article. Review.
Expressing the human proteome for affinity proteomics: optimising expression of soluble protein domains and in vivo biotinylation.
Keates T, Cooper CD, Savitsky P, Allerston CK, Phillips C, Hammarström M, Daga N, Berridge G, Mahajan P, Burgess-Brown NA, Müller S, Gräslund S, Gileadi O. Keates T, et al. Among authors: gileadi o. N Biotechnol. 2012 Jun 15;29(5):515-25. doi: 10.1016/j.nbt.2011.10.007. Epub 2011 Oct 19. N Biotechnol. 2012. PMID: 22027370 Free PMC article.
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations.
Couñago RM, Allerston CK, Savitsky P, Azevedo H, Godoi PH, Wells CI, Mascarello A, de Souza Gama FH, Massirer KB, Zuercher WJ, Guimarães CRW, Gileadi O. Couñago RM, et al. Among authors: gileadi o. Sci Rep. 2017 Aug 8;7(1):7501. doi: 10.1038/s41598-017-07755-y. Sci Rep. 2017. PMID: 28790404 Free PMC article.
WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.
Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB. Agajanian MJ, et al. Among authors: gileadi c, gileadi o. Cell Rep. 2019 Jan 2;26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023. Cell Rep. 2019. PMID: 30605688 Free PMC article.
Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2.
Serafim RAM, de Souza Gama FH, Dutra LA, Dos Reis CV, Vasconcelos SNS, da Silva Santiago A, Takarada JE, Di Pillo F, Azevedo H, Mascarello A, Elkins JM, Massirer KB, Gileadi O, Guimarães CRW, Couñago RM. Serafim RAM, et al. Among authors: gileadi o. ACS Med Chem Lett. 2019 Aug 19;10(9):1266-1271. doi: 10.1021/acsmedchemlett.9b00082. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531195 Free PMC article.
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.
Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM. Profeta GS, et al. Among authors: gileadi o. Sci Rep. 2019 Nov 11;9(1):16452. doi: 10.1038/s41598-019-52795-1. Sci Rep. 2019. PMID: 31712618 Free PMC article.
SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD. Wells C, et al. Among authors: gileadi o. ACS Med Chem Lett. 2019 Oct 23;11(3):340-345. doi: 10.1021/acsmedchemlett.9b00399. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184967 Free PMC article.
117 results