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Page 1
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. 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.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: gileadi c. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
Discovery of an MLLT1/3 YEATS Domain Chemical Probe.
Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Brennan PE, Fedorov O. Moustakim M, et al. Among authors: gileadi c. Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. doi: 10.1002/anie.201810617. Epub 2018 Nov 16. Angew Chem Int Ed Engl. 2018. PMID: 30288907 Free PMC article.
Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.
Christott T, Bennett J, Coxon C, Monteiro O, Giroud C, Beke V, Felce SL, Gamble V, Gileadi C, Poda G, Al-Awar R, Farnie G, Fedorov O. Christott T, et al. Among authors: gileadi c. SLAS Discov. 2019 Feb;24(2):133-141. doi: 10.1177/2472555218809904. Epub 2018 Oct 25. SLAS Discov. 2019. PMID: 30359161 Free article.
Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.
Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundström M, Doyle DA, Siderovski DP. Soundararajan M, et al. Among authors: gileadi c. Proc Natl Acad Sci U S A. 2008 Apr 29;105(17):6457-62. doi: 10.1073/pnas.0801508105. Epub 2008 Apr 23. Proc Natl Acad Sci U S A. 2008. PMID: 18434541 Free PMC article.
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.
Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Faram R, Cribbs AP, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett J, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith C, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann U. Fagan V, et al. Among authors: gileadi c. J Med Chem. 2019 Oct 24;62(20):9008-9025. doi: 10.1021/acs.jmedchem.9b00562. Epub 2019 Oct 15. J Med Chem. 2019. PMID: 31550156
SARS-CoV-2 infects the human kidney and drives fibrosis in kidney organoids.
Jansen J, Reimer KC, Nagai JS, Varghese FS, Overheul GJ, de Beer M, Roverts R, Daviran D, Fermin LAS, Willemsen B, Beukenboom M, Djudjaj S, von Stillfried S, van Eijk LE, Mastik M, Bulthuis M, Dunnen WD, van Goor H, Hillebrands JL, Triana SH, Alexandrov T, Timm MC, van den Berge BT, van den Broek M, Nlandu Q, Heijnert J, Bindels EMJ, Hoogenboezem RM, Mooren F, Kuppe C, Miesen P, Grünberg K, Ijzermans T, Steenbergen EJ, Czogalla J, Schreuder MF, Sommerdijk N, Akiva A, Boor P, Puelles VG, Floege J, Huber TB; COVID Moonshot consortium; van Rij RP, Costa IG, Schneider RK, Smeets B, Kramann R. Jansen J, et al. Cell Stem Cell. 2022 Feb 3;29(2):217-231.e8. doi: 10.1016/j.stem.2021.12.010. Epub 2021 Dec 25. Cell Stem Cell. 2022. PMID: 35032430 Free PMC article.
Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
Londregan AT, Aitmakhanova K, Bennett J, Byrnes LJ, Canterbury DP, Cheng X, Christott T, Clemens J, Coffey SB, Dias JM, Dowling MS, Farnie G, Fedorov O, Fennell KF, Gamble V, Gileadi C, Giroud C, Harris MR, Hollingshead BD, Huber K, Korczynska M, Lapham K, Loria PM, Narayanan A, Owen DR, Raux B, Sahasrabudhe PV, Ruggeri RB, Sáez LD, Stock IA, Thuma BA, Tsai A, Varghese AE. Londregan AT, et al. Among authors: gileadi c. J Med Chem. 2023 Jan 12;66(1):460-472. doi: 10.1021/acs.jmedchem.2c01421. Epub 2022 Dec 23. J Med Chem. 2023. PMID: 36562986
32 results