Publications by authors named "Tim Clackson"

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XTX101, a tumor-activated, Fc-enhanced anti-CTLA-4 monoclonal antibody, demonstrates tumor-growth inhibition and tumor-selective pharmacodynamics in mouse models of cancer.
Kurt A Jenkins, Miso Park, Magali Pederzoli-Ribeil, Ugur Eskiocak, Parker Johnson, Tim Clackson

J Immunother Cancer· December 2023

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Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Wei-Sheng Huang, Feng Li, Yongjin Gong, Yun Zhang, Willmen Youngsaye, Tim Clackson

Bioorg Med Chem Lett· January 2023

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Mobocertinib (TAK-788): A Targeted Inhibitor of Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.
Francois Gonzalvez, Sylvie Vincent, Theresa E Baker, Alexandra E Gould, Shuai Li, Tim Clackson

Cancer Discov· July 2021

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Exploratory Analysis of Brigatinib Activity in Patients With Anaplastic Lymphoma Kinase-Positive Non-Small-Cell Lung Cancer and Brain Metastases in Two Clinical Trials.
D Ross Camidge, Dong-Wan Kim, Marcello Tiseo, Corey J Langer, Myung-Ju Ahn, Tim Clackson

J Clin Oncol· September 2018

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The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
Sen Zhang, Rana Anjum, Rachel Squillace, Sara Nadworny, Tianjun Zhou, Tim Clackson

Clin Cancer Res· November 2016

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Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Wei-Sheng Huang, Shuangying Liu, Dong Zou, Mathew Thomas, Yihan Wang, Tim Clackson

J Med Chem· May 2016

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Compound mutations in BCR-ABL1 are not major drivers of primary or secondary resistance to ponatinib in CP-CML patients.
Michael W Deininger, J Graeme Hodgson, Neil P Shah, Jorge E Cortes, Dong-Wook Kim, Tim Clackson

Blood· February 2016

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Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients.
Andrew P Garner, Joseph M Gozgit, Rana Anjum, Sadanand Vodala, Alexa Schrock, Tim Clackson

Clin Cancer Res· November 2014

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Ponatinib in patients with refractory acute myeloid leukaemia: findings from a phase 1 study.
Neil P Shah, Moshe Talpaz, Michael W N Deininger, Michael J Mauro, Ian W Flinn, Tim Clackson

Br J Haematol· August 2013

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Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models.
Joseph M Gozgit, Rachel M Squillace, Matthew J Wongchenko, David Miller, Scott Wardwell, Tim Clackson

Cancer Chemother Pharmacol· May 2013

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Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.
Anna Kohlmann, Stephan G Zech, Feng Li, Tianjun Zhou, Rachel M Squillace, Tim Clackson

J Med Chem· February 2013

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Ponatinib in refractory Philadelphia chromosome-positive leukemias.
Jorge E Cortes, Hagop Kantarjian, Neil P Shah, Dale Bixby, Michael J Mauro, Tim Clackson

N Engl J Med· November 2012

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Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models.
Rachel M Squillace, David Miller, Scott D Wardwell, Frank Wang, Tim Clackson

Int J Oncol· August 2012

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Dimerizer-mediated regulation of gene expression.
Victor M Rivera, Lori Berk, Tim Clackson

Cold Spring Harb Protoc· July 2012

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Dimerizer-mediated regulation of gene expression in vitro.
Victor M Rivera, Lori Berk, Tim Clackson

Cold Spring Harb Protoc· July 2012

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Dimerizer-mediated regulation of gene expression in vivo.
Victor M Rivera, Lori Berk, Tim Clackson

Cold Spring Harb Protoc· July 2012

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Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial.
Lori Berk, Monica M Mita, Jeff Kreisberg, Camille L Bedrosian, Anthony W Tolcher, Tim Clackson

Cancer Chemother Pharmacol· May 2012

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Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models.
Joseph M Gozgit, Matthew J Wong, Lauren Moran, Scott Wardwell, Qurish K Mohemmad, Tim Clackson

Mol Cancer Ther· March 2012

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Phase II study of the mammalian target of rapamycin inhibitor ridaforolimus in patients with advanced bone and soft tissue sarcomas.
Sant P Chawla, Arthur P Staddon, Laurence H Baker, Scott M Schuetze, Anthony W Tolcher, Tim Clackson

J Clin Oncol· January 2012

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Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.
Sen Zhang, Frank Wang, Jeffrey Keats, Xiaotian Zhu, Yaoyu Ning, Tim Clackson

Chem Biol Drug Des· December 2011

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Antitumor activity of ridaforolimus and potential cell-cycle determinants of sensitivity in sarcoma and endometrial cancer models.
Rachel M Squillace, David Miller, Michelle Cookson, Scott D Wardwell, Lauren Moran, Tim Clackson

Mol Cancer Ther· October 2011

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Assessment of the safety and biodistribution of a regulated AAV2 gene transfer vector after delivery to murine submandibular glands.
Changyu Zheng, Antonis Voutetakis, Benjamin Goldstein, Sandra Afione, Victor M Rivera, Tim Clackson

Toxicol Sci· September 2011

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Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.
Joseph M Gozgit, Matthew J Wong, Scott Wardwell, Jeffrey W Tyner, Marc M Loriaux, Tim Clackson

Mol Cancer Ther· June 2011

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Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens.
Victor M Rivera, Rachel M Squillace, David Miller, Lori Berk, Scott D Wardwell, Tim Clackson

Mol Cancer Ther· June 2011

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Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Mathew Thomas, Wei-Sheng Huang, David Wen, Xiaotian Zhu, Yihan Wang, Tim Clackson

Bioorg Med Chem Lett· June 2011

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