Publications by authors named "Michelle Nannini"

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Preclinical assessment of the PI3Kα selective inhibitor inavolisib and prediction of its pharmacokinetics and efficacious dose in human.
Laurent Salphati, Jodie Pang, Emile G Plise, Jonathan Cheong, Marie-Gabrielle Braun, Michelle Nannini

Xenobiotica· October 2024

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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Emily J Hanan, Marie-Gabrielle Braun, Robert A Heald, Calum MacLeod, Connie Chan, Michelle Nannini

J Med Chem· December 2022

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy.
Kyung W Song, Kyle A Edgar, Emily J Hanan, Marc Hafner, Jason Oeh, Michelle A Nannini

Cancer Discov· January 2022

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Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Jason R Zbieg, Jun Liang, Jun Li, Robert A Blake, Jae Chang, Michelle Nannini

Bioorg Med Chem Lett· October 2021

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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Jun Liang, Jason R Zbieg, Robert A Blake, Jae H Chang, Stephen Daly, Michelle A Nannini

J Med Chem· August 2021

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Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Jun Liang, Robert Blake, Jae Chang, Lori S Friedman, Simon Goodacre, Michelle Nannini

ACS Med Chem Lett· June 2020

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Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.
Jane Guan, Wei Zhou, Marc Hafner, Robert A Blake, Cecile Chalouni, Michelle Nannini

Cell· August 2019

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Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Birong Zhang, James R Kiefer, Robert A Blake, Jae H Chang, Steven Hartman, Michelle Nannini

Bioorg Med Chem Lett· April 2019

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Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
James D Joseph, Beatrice Darimont, Wei Zhou, Alfonso Arrazate, Amy Young, Michelle A Nannini

Elife· January 2019

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The Kinase Activity of Hematopoietic Progenitor Kinase 1 Is Essential for the Regulation of T Cell Function.
Sairy Hernandez, Jing Qing, Rebecca Hong Thibodeau, Xiangnan Du, Summer Park, Michelle Nannini

Cell Rep· October 2018

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Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.
Anneleen Daemen, Bonnie Liu, Kyung Song, Mandy Kwong, Min Gao, Michelle Nannini

Cell Metab· September 2018

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Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.
Peter S Dragovich, Robert A Blake, Chunjiao Chen, Jinhua Chen, Josefa Chuh, Michelle Nannini

Chemistry· April 2018

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A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors.
Cristina Saura, Desamparados Roda, Susana Roselló, Mafalda Oliveira, Teresa Macarulla, Michelle Nannini

Cancer Discov· January 2017

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The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
James D Joseph, Beatrice Darimont, Wei Zhou, Alfonso Arrazate, Amy Young, Michelle A Nannini

Elife· July 2016

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Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer.
Wei Yang, Sarah R Hosford, Lloye M Dillon, Kevin Shee, Stephanie C Liu, Michelle A Nannini

Clin Cancer Res· May 2016

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Modeling targeted inhibition of MEK and PI3 kinase in human pancreatic cancer.
Melissa R Junttila, Vidusha Devasthali, Jason H Cheng, Joseph Castillo, Ciara Metcalfe, Michelle A Nannini

Mol Cancer Ther· January 2015

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MAPK pathway inhibition enhances the efficacy of an anti-endothelin B receptor drug conjugate by inducing target expression in melanoma.
Jyoti Asundi, Jennifer A Lacap, Suzanna Clark, Michelle Nannini, Leslie Roth

Mol Cancer Ther· June 2014

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Nanosuspension delivery of paclitaxel to xenograft mice can alter drug disposition and anti-tumor activity.
Po-Chang Chiang, Stephen Gould, Michelle Nannini, Ann Qin, Yuzhong Deng

Nanoscale Res Lett· April 2014

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Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068.
Yibing Yan, Violeta Serra, Ludmila Prudkin, Maurizio Scaltriti, Sumati Murli, Michelle Nannini

Clin Cancer Res· December 2013

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Supplementation of nicotinic acid with NAMPT inhibitors results in loss of in vivo efficacy in NAPRT1-deficient tumor models.
Thomas O'Brien, Jason Oeh, Yang Xiao, Xiaorong Liang, Alexander Vanderbilt, Michelle Nannini

Neoplasia· December 2013

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Anti-EGFL7 antibodies enhance stress-induced endothelial cell death and anti-VEGF efficacy.
Leisa Johnson, Mahrukh Huseni, Tanya Smyczek, Anthony Lima, Stacey Yeung, Michelle A Nannini

J Clin Invest· September 2013

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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.
Nguyen Tan, Maureen Wong, Michelle A Nannini, Rebecca Hong, Leslie B Lee

Mol Cancer Ther· June 2013

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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.
Chudi O Ndubaku, Timothy P Heffron, Steven T Staben, Matthew Baumgardner, Nicole Blaquiere, Michelle Nannini

J Med Chem· June 2013

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Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.
Jie Lin, Deepak Sampath, Michelle A Nannini, Brian B Lee, Michael Degtyarev

Clin Cancer Res· April 2013

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Anti-VEGF antibody therapy does not promote metastasis in genetically engineered mouse tumour models.
Mallika Singh, Suzana S Couto, William F Forrest, Anthony Lima, Jason H Cheng, Michelle A Nannini

J Pathol· August 2012

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