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Page 1
Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.
Guan J, Zhou W, Hafner M, Blake RA, Chalouni C, Chen IP, De Bruyn T, Giltnane JM, Hartman SJ, Heidersbach A, Houtman R, Ingalla E, Kategaya L, Kleinheinz T, Li J, Martin SE, Modrusan Z, Nannini M, Oeh J, Ubhayakar S, Wang X, Wertz IE, Young A, Yu M, Sampath D, Hager JH, Friedman LS, Daemen A, Metcalfe C. Guan J, et al. Among authors: kategaya l. Cell. 2019 Aug 8;178(4):949-963.e18. doi: 10.1016/j.cell.2019.06.026. Epub 2019 Jul 25. Cell. 2019. PMID: 31353221 Free article.
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X. Liang J, et al. Among authors: kategaya l. J Med Chem. 2021 Aug 26;64(16):11841-11856. doi: 10.1021/acs.jmedchem.1c00847. Epub 2021 Jul 12. J Med Chem. 2021. PMID: 34251202
Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: kategaya l. Elife. 2019 Jan 7;8:e44851. doi: 10.7554/eLife.44851. Elife. 2019. PMID: 30614786 Free PMC article.
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.
Di Lello P, Pastor R, Murray JM, Blake RA, Cohen F, Crawford TD, Drobnick J, Drummond J, Kategaya L, Kleinheinz T, Maurer T, Rougé L, Zhao X, Wertz I, Ndubaku C, Tsui V. Di Lello P, et al. Among authors: kategaya l. J Med Chem. 2017 Dec 28;60(24):10056-10070. doi: 10.1021/acs.jmedchem.7b01293. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29166018
USP7 small-molecule inhibitors interfere with ubiquitin binding.
Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE. Kategaya L, et al. Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18. Nature. 2017. PMID: 29045385
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: kategaya l. Elife. 2016 Jul 13;5:e15828. doi: 10.7554/eLife.15828. Elife. 2016. PMID: 27410477 Free PMC article.
Erratum: Phosphorylation and linear ubiquitin direct A20 inhibition of inflammation.
Wertz IE, Newton K, Seshasayee D, Kusam S, Lam C, Zhang J, Popovych N, Helgason E, Schoeffler A, Jeet S, Ramamoorthi N, Kategaya L, Newman RJ, Horikawa K, Dugger D, Sandoval W, Mukund S, Zindal A, Martin F, Quan C, Tom J, Fairbrother WJ, Townsend M, Warming S, DeVoss J, Liu J, Dueber E, Caplazi P, Lee WP, Goodnow CC, Balazs M, Yu K, Kolumam G, Dixit VM. Wertz IE, et al. Among authors: kategaya l. Nature. 2016 Apr 21;532(7599):402. doi: 10.1038/nature16541. Epub 2016 Jan 13. Nature. 2016. PMID: 26760210 No abstract available.
Phosphorylation and linear ubiquitin direct A20 inhibition of inflammation.
Wertz IE, Newton K, Seshasayee D, Kusam S, Lam C, Zhang J, Popovych N, Helgason E, Schoeffler A, Jeet S, Ramamoorthi N, Kategaya L, Newman RJ, Horikawa K, Dugger D, Sandoval W, Mukund S, Zindal A, Martin F, Quan C, Tom J, Fairbrother WJ, Townsend M, Warming S, DeVoss J, Liu J, Dueber E, Caplazi P, Lee WP, Goodnow CC, Balazs M, Yu K, Kolumam G, Dixit VM. Wertz IE, et al. Among authors: kategaya l. Nature. 2015 Dec 17;528(7582):370-5. doi: 10.1038/nature16165. Epub 2015 Dec 9. Nature. 2015. PMID: 26649818
Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
Leverson JD, Zhang H, Chen J, Tahir SK, Phillips DC, Xue J, Nimmer P, Jin S, Smith M, Xiao Y, Kovar P, Tanaka A, Bruncko M, Sheppard GS, Wang L, Gierke S, Kategaya L, Anderson DJ, Wong C, Eastham-Anderson J, Ludlam MJ, Sampath D, Fairbrother WJ, Wertz I, Rosenberg SH, Tse C, Elmore SW, Souers AJ. Leverson JD, et al. Among authors: kategaya l. Cell Death Dis. 2015 Jan 15;6(1):e1590. doi: 10.1038/cddis.2014.561. Cell Death Dis. 2015. PMID: 25590800 Free PMC article.
16 results