Publications by authors named "Methvin Isaac"

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Structure-based discovery of sulfamoyl-ethyl-4-oxo-3,4-dihydro-7H-pyrrolo[2,3-d]pyrimidine amides and sulfonamides as potent B-Cell Lymphoma 6 (BCL6)-BTB inhibitors.
Ahmed Mamai, Mohammed M Morshed, Michael Prakesch, Gennady Poda, Pandiaraju Subramanian, Methvin Isaac

Bioorg Med Chem Lett· February 2026

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Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
Václav Němec, Marek Remeš, Petr Beňovský, Michael C Böck, Eliška Šranková, Methvin B Isaac

J Med Chem· August 2024

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The Imipridone ONC213 Targets α-Ketoglutarate Dehydrogenase to Induce Mitochondrial Stress and Suppress Oxidative Phosphorylation in Acute Myeloid Leukemia.
Yongwei Su, Jenna L Carter, Xinyu Li, Yu Fukuda, Ashley Gray, Methvin B Isaac

Cancer Res· April 2024

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Discovery of Conformationally Constrained ALK2 Inhibitors.
Héctor González-Álvarez, Deeba Ensan, Tao Xin, Jong Fu Wong, Carlos A Zepeda-Velázquez, Methvin B Isaac

J Med Chem· March 2024

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Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Ahmed Mamai, Anh M Chau, Brian J Wilson, Iain D Watson, Babu B Joseph, Methvin B Isaac

ACS Med Chem Lett· February 2023

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Correction to "Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma".
David E Uehling, Babu Joseph, Kim Chan Chung, Andrew X Zhang, Spencer Ler, Methvin B Isaac

J Med Chem· January 2022

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Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation in Lung Cancer Cells.
Punit Saraon, Jamie Snider, Wiebke Schormann, Ankit Rai, Nikolina Radulovich, Methvin Isaac

J Mol Biol· November 2021

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The PKN1- TRAF1 signaling axis as a potential new target for chronic lymphocytic leukemia.
Maria I Edilova, Jaclyn C Law, Safoura Zangiabadi, Kenneth Ting, Achire N Mbanwi, Methvin Isaac

Oncoimmunology· October 2021

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Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
David E Uehling, Babu Joseph, Kim Chan Chung, Andrew X Zhang, Spencer Ler, Methvin B Isaac

J Med Chem· August 2021

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Leveraging Open Science Drug Development for PET: Preliminary Neuroimaging of C-Labeled ALK2 Inhibitors.
Emily Murrell, Junchao Tong, David Smil, Taira Kiyota, Ahmed M Aman, Methvin B Isaac

ACS Med Chem Lett· May 2021

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Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
David Smil, Jong Fu Wong, Eleanor P Williams, Roslin J Adamson, Alison Howarth, Methvin B Isaac

J Med Chem· September 2020

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Antagonists of the serotonin receptor 5A target human breast tumor initiating cells.
William D Gwynne, Mirza S Shakeel, Adele Girgis-Gabardo, Kwang H Kim, Emily Ford, Methvin Isaac

BMC Cancer· August 2020

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Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
Deeba Ensan, David Smil, Carlos A Zepeda-Velázquez, Dimitrios Panagopoulos, Jong Fu Wong, Methvin B Isaac

J Med Chem· May 2020

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Sorafenib as an Inhibitor of RUVBL2.
Nardin Nano, Francisca Ugwu, Thiago V Seraphim, Tangzhi Li, Gina Azer, Methvin Isaac

Biomolecules· April 2020

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PI3K/AKT/mTOR inhibition in combination with doxorubicin is an effective therapy for leiomyosarcoma.
Yael Babichev, Leah Kabaroff, Alessandro Datti, David Uehling, Methvin Isaac

J Transl Med· March 2016

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Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Patrick Raboisson, Anna Breitholtz-Emanuelsson, Henrik Dahllöf, Louise Edwards, William L Heaton, Methvin Isaac

Bioorg Med Chem Lett· November 2012

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TWEAK and cIAP1 regulate myoblast fusion through the noncanonical NF-κB signaling pathway.
Emeka K Enwere, Janelle Holbrook, Rim Lejmi-Mrad, Jennifer Vineham, Kristen Timusk, Methvin Isaac

Sci Signal· October 2012

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The oncogenic PIM kinase family regulates drug resistance through multiple mechanisms.
Methvin Isaac, Allan Siu, Jan Jongstra

Drug Resist Updat· February 2012

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A small molecule screening strategy with validation on human leukemia stem cells uncovers the therapeutic efficacy of kinetin riboside.
Sean P McDermott, Kolja Eppert, Faiyaz Notta, Methvin Isaac, Alessandro Datti

Blood· February 2012

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Wnt inhibitor screen reveals iron dependence of β-catenin signaling in cancers.
Siyuan Song, Tania Christova, Stephen Perusini, Solmaz Alizadeh, Ren-Yue Bao, Methvin Isaac

Cancer Res· December 2011

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Virus-tumor interactome screen reveals ER stress response can reprogram resistant cancers for oncolytic virus-triggered caspase-2 cell death.
Douglas J Mahoney, Charles Lefebvre, Kristina Allan, Jan Brun, Cina A Sanaei, Methvin Isaac

Cancer Cell· October 2011

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Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells.
Natalie Grinshtein, Alessandro Datti, Mayumi Fujitani, David Uehling, Michael Prakesch, Methvin Isaac

Cancer Res· February 2011

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4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.
Hui Xiong, Todd A Brugel, Michael Balestra, Dean G Brown, Kelly A Brush, Methvin Isaac

Bioorg Med Chem Lett· December 2010

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The anti-epileptic drug lacosamide (Vimpat) has anxiolytic property in rodents.
Guy A Higgins, Nathalie Breysse, Elijus Undzys, Calvin Kuo, Narges Joharchi, Methvin Isaac

Eur J Pharmacol· December 2009

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Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice.
Paul J Fletcher, Maria Tampakeras, Judy Sinyard, Abdelmalik Slassi, Methvin Isaac

Neuropharmacology· September 2009

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