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Page 1
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X. Liang J, et al. Among authors: nannini m. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347. doi: 10.1021/acsmedchemlett.0c00224. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551022 Free PMC article.
Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.
Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K. Lin J, et al. Among authors: nannini ma. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3. Clin Cancer Res. 2013. PMID: 23287563
Bcl-2/Bcl-xL inhibition increases the efficacy of MEK inhibition alone and in combination with PI3 kinase inhibition in lung and pancreatic tumor models.
Tan N, Wong M, Nannini MA, Hong R, Lee LB, Price S, Williams K, Savy PP, Yue P, Sampath D, Settleman J, Fairbrother WJ, Belmont LD. Tan N, et al. Among authors: nannini ma. Mol Cancer Ther. 2013 Jun;12(6):853-64. doi: 10.1158/1535-7163.MCT-12-0949. Epub 2013 Mar 8. Mol Cancer Ther. 2013. PMID: 23475955
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Ndubaku CO, et al. Among authors: nannini m. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. J Med Chem. 2013. PMID: 23662903
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: nannini ma. Elife. 2016 Jul 13;5:e15828. doi: 10.7554/eLife.15828. Elife. 2016. PMID: 27410477 Free PMC article.
Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.
Dragovich PS, Blake RA, Chen C, Chen J, Chuh J, den Besten W, Fan F, Fourie A, Hartman SJ, He C, He J, Ingalla ER, Kozak KR, Leong SR, Lu J, Ma Y, Meng L, Nannini M, Oeh J, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Sampath D, Vandlen R, Vollmar B, Wai J, Wertz IE, Xu K, Xu Z, Zhang D. Dragovich PS, et al. Among authors: nannini m. Chemistry. 2018 Apr 3;24(19):4830-4834. doi: 10.1002/chem.201800859. Epub 2018 Mar 25. Chemistry. 2018. PMID: 29493023
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: nannini ma. Elife. 2019 Jan 7;8:e44851. doi: 10.7554/eLife.44851. Elife. 2019. PMID: 30614786 Free PMC article.
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J. Zhang B, et al. Among authors: nannini m. Bioorg Med Chem Lett. 2019 Apr 1;29(7):905-911. doi: 10.1016/j.bmcl.2019.01.036. Epub 2019 Feb 1. Bioorg Med Chem Lett. 2019. PMID: 30732944
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: nannini m. 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.
240 results