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Select item 111894421.

APR-246 as a radiosensitization strategy for mutant p53 cancers treated with alpha-particles-based radiotherapy

Or Michaeli, Ishai Luz, Maayan Vatarescu, Tal Manko, Noam Weizman, Yevgeniya Korotinsky, Alexandra Tsitrina, Alex Braiman, Lior Arazi, Tomer Cooks

Cell Death Dis. 2024 Jun; 15(6): 426. Published online 2024 Jun 18. doi: 10.1038/s41419-024-06830-3

PMCID:: PMC11189442

Abstract Article PDF–4.3M

Select item 96818662.

Mutant p53 gain of function mediates cancer immune escape that is counteracted by APR-246

Xiaolei Zhou, Gema Sanz Santos, Yue Zhan, Mariana M. S. Oliveira, Shiva Rezaei, Madhurendra Singh, Sylvain Peuget, Lisa S. Westerberg, John Inge Johnsen, Galina Selivanova

Br J Cancer. 2022 Nov 23; 127(11): 2060–2071. Published online 2022 Sep 22. doi: 10.1038/s41416-022-01971-8

PMCID:: PMC9681866

Abstract Article PDF–2.2M

Select item 95888803.

Phase Ib study of eprenetapopt (APR-246) in combination with pembrolizumab in patients with advanced or metastatic solid tumors

H. Park, G.I. Shapiro, X. Gao, A. Mahipal, J. Starr, M. Furqan, P. Singh, A. Ahrorov, L. Gandhi, A. Ghosh, D. Hickman, P.D. Gallacher, A. Wennborg, E.C. Attar, M.M. Awad, S. Das, E.E. Dumbrava

ESMO Open. 2022 Oct; 7(5): 100573. Published online 2022 Sep 7. doi: 10.1016/j.esmoop.2022.100573

PMCID:: PMC9588880

Abstract Article PDF–368K

Select item 94796034.

Increased p53 expression induced by APR-246 reprograms tumor-associated macrophages to augment immune checkpoint blockade

Arnab Ghosh, Judith Michels, Riccardo Mezzadra, Divya Venkatesh, Lauren Dong, Ricardo Gomez, Fadi Samaan, Yu-Jui Ho, Luis Felipe Campesato, Levi Mangarin, John Fak, Nathan Suek, Aliya Holland, Cailian Liu, Mohsen Abu-Akeel, Yonina Bykov, Hong Zhong, Kelly Fitzgerald, Sadna Budhu, Andrew Chow, Roberta Zappasodi, Katherine S. Panageas, Olivier de Henau, Marcus Ruscetti, Scott W. Lowe, Taha Merghoub, Jedd D. Wolchok

J Clin Invest. 2022 Sep 15; 132(18): e148141. Published online 2022 Sep 15. doi: 10.1172/JCI148141

PMCID:: PMC9479603

Abstract Article PDF–2.2M

Select item 92567665.

Ovarian cancers with low CIP2A tumor expression constitute an APR-246 sensitive disease subtype

Anna N. Cvrljevic, Umar Butt, Kaisa Huhtinen, Tove J. Grönroos, Camilla Böckelman, Heini Lassus, Ralf Butzow, Caj Haglund, Katja Kaipio, Tiina Arsiola, Teemu D. Laajala, Denise C. Connolly, Ari Ristimäki, Olli Carpen, Jeroen Pouwels, Jukka Westermarck

Mol Cancer Ther. Author manuscript; available in PMC 2023 Jan 5.

Published in final edited form as: Mol Cancer Ther. 2022 Jul 5; 21(7): 1236–1245. doi: 10.1158/1535-7163.MCT-21-0622

PMCID:: PMC9256766

Abstract Article PDF–1.0M

Select item 89616096.

APR-246—The Mutant TP53 Reactivator—Increases the Effectiveness of Berberine and Modified Berberines to Inhibit the Proliferation of Pancreatic Cancer Cells

James Andrew McCubrey, Stephen L. Abrams, Linda S. Steelman, Lucio Cocco, Stefano Ratti, Alberto M. Martelli, Paolo Lombardi, Agnieszka Gizak, Przemysław Duda

Biomolecules. 2022 Feb; 12(2): 276. Published online 2022 Feb 8. doi: 10.3390/biom12020276

PMCID:: PMC8961609

Abstract Article PDF–3.6M

Select item 89097567.

Effects of the Mutant TP53 Reactivator APR-246 on Therapeutic Sensitivity of Pancreatic Cancer Cells in the Presence and Absence of WT-TP53

Stephen L. Abrams, Przemysław Duda, Shaw M. Akula, Linda S. Steelman, Matilde L. Follo, Lucio Cocco, Stefano Ratti, Alberto M. Martelli, Giuseppe Montalto, Maria Rita Emma, Melchiorre Cervello, Dariusz Rakus, Agnieszka Gizak, James A. McCubrey

Cells. 2022 Mar; 11(5): 794. Published online 2022 Feb 24. doi: 10.3390/cells11050794

PMCID:: PMC8909756

Abstract Article PDF–2.9M

Select item 88202368.

Potential and mechanism of mebendazole for treatment and maintenance of ovarian cancer

Suganthapriya Elayapillai, Satishkumar Ramraj, Doris Mangiaracina Benbrook, Magdalena Bieniasz, Lin Wang, Gopal Pathuri, Zitha Redempta Isingizwe, Amy L. Kennedy, Yan D. Zhao, Stanley Lightfoot, Lauri A. Hunsucker, Camille C. Gunderson

Gynecol Oncol. Author manuscript; available in PMC 2022 Feb 7.

Published in final edited form as: Gynecol Oncol. 2021 Jan; 160(1): 302–311. Published online 2020 Oct 31. doi: 10.1016/j.ygyno.2020.10.010

PMCID:: PMC8820236

Abstract Article PDF–1.9M

Select item 88045789.

APR-246 induces early cell death by ferroptosis in acute myeloid leukemia

Rudy Birsen, Clement Larrue, Justine Decroocq, Natacha Johnson, Nathan Guiraud, Mathilde Gotanegre, Lilia Cantero-Aguilar, Eric Grignano, Tony Huynh, Michaela Fontenay, Olivier Kosmider, Patrick Mayeux, Nicolas Chapuis, Jean Emmanuel Sarry, Jerome Tamburini, Didier Bouscary

Haematologica. 2022 Feb 1; 107(2): 403–416. Published online 2021 Jan 7. doi: 10.3324/haematol.2020.259531

PMCID:: PMC8804578

Abstract Article PDF–2.1M

Select item 864253210.

Structural basis of reactivation of oncogenic p53 mutants by a small molecule: methylene quinuclidinone (MQ)

Oksana Degtjarik, Dmitrij Golovenko, Yael Diskin-Posner, Lars Abrahmsén, Haim Rozenberg, Zippora Shakked

Nat Commun. 2021; 12: 7057. Published online 2021 Dec 3. doi: 10.1038/s41467-021-27142-6

PMCID:: PMC8642532

Abstract Article PDF–4.2M

Select item 860890311.

APR-246 induces apoptosis and enhances chemo-sensitivity via activation of ROS and TAp73-Noxa signal in oesophageal squamous cell cancer with TP53 missense mutation

Teruyuki Kobayashi, Tomoki Makino, Kotaro Yamashita, Takuro Saito, Koji Tanaka, Tsuyoshi Takahashi, Yukinori Kurokawa, Makoto Yamasaki, Kiyokazu Nakajima, Eiichi Morii, Hidetoshi Eguchi, Yuichiro Doki

Br J Cancer. 2021 Nov 23; 125(11): 1523–1532. Published online 2021 Oct 1. doi: 10.1038/s41416-021-01561-0

PMCID:: PMC8608903

Abstract Article PDF–4.4M

Select item 847108312.

Personalized Medicine for TP53 Mutated Myelodysplastic Syndromes and Acute Myeloid Leukemia

Thomas Cluzeau, Michael Loschi, Pierre Fenaux, Rami Komrokji, David A. Sallman

Int J Mol Sci. 2021 Sep; 22(18): 10105. Published online 2021 Sep 18. doi: 10.3390/ijms221810105

PMCID:: PMC8471083

Abstract Article PDF–243K

Select item 828266213.

Mutant p53-reactivating compound APR-246 synergizes with asparaginase in inducing growth suppression in acute lymphoblastic leukemia cells

Sophia Ceder, Sofi E. Eriksson, Ying Yu Liang, Emarndeena H. Cheteh, Si Min Zhang, Kenji M. Fujihara, Julie Bianchi, Vladimir J. N. Bykov, Lars Abrahmsen, Nicholas J. Clemons, Pär Nordlund, Sean G. Rudd, Klas G. Wiman

Cell Death Dis. 2021 Jul; 12(7): 709. Published online 2021 Jul 15. doi: 10.1038/s41419-021-03988-y

Correction in:: Cell Death Dis. 2022 Aug; 13(8): 672.

PMCID:: PMC8282662

Abstract Article PDF–1.8M

Select item 819883114.

CX-5461 Enhances the Efficacy of APR-246 via Induction of DNA Damage and Replication Stress in Triple-Negative Breast Cancer

Ashwini Makhale, Devathri Nanayakkara, Prahlad Raninga, Kum Kum Khanna, Murugan Kalimutho

Int J Mol Sci. 2021 Jun; 22(11): 5782. Published online 2021 May 28. doi: 10.3390/ijms22115782

PMCID:: PMC8198831

Abstract Article PDF–2.7M

Select item 809941015.

Eprenetapopt (APR-246) and Azacitidine in TP53-Mutant Myelodysplastic Syndromes

David A. Sallman, Amy E. DeZern, Guillermo Garcia-Manero, David P. Steensma, Gail J. Roboz, Mikkael A. Sekeres, Thomas Cluzeau, Kendra L. Sweet, Amy McLemore, Kathy L. McGraw, John Puskas, Ling Zhang, Jiqiang Yao, Qianxing Mo, Lisa Nardelli, Najla H. Al Ali, Eric Padron, Greg Korbel, Eyal C. Attar, Hagop M. Kantarjian, Jeffrey E. Lancet, Pierre Fenaux, Alan F. List, Rami S. Komrokji

J Clin Oncol. 2021 May 10; 39(14): 1584–1594. Published online 2021 Jan 15. doi: 10.1200/JCO.20.02341

PMCID:: PMC8099410

Abstract Article PDF–507K

Select item 809940916.

Eprenetapopt Plus Azacitidine in TP53-Mutated Myelodysplastic Syndromes and Acute Myeloid Leukemia: A Phase II Study by the Groupe Francophone des Myélodysplasies (GFM)

Thomas Cluzeau, Marie Sebert, Ramy Rahmé, Stefania Cuzzubbo, Jacqueline Lehmann-Che, Isabelle Madelaine, Pierre Peterlin, Blandine Bève, Habiba Attalah, Fatiha Chermat, Elsa Miekoutima, Odile Beyne Rauzy, Christian Recher, Aspasia Stamatoullas, Lise Willems, Emmanuel Raffoux, Céline Berthon, Bruno Quesnel, Michael Loschi, Antoine F. Carpentier, David A. Sallman, Rami Komrokji, Anouk Walter-Petrich, Sylvie Chevret, Lionel Ades, Pierre Fenaux

J Clin Oncol. 2021 May 10; 39(14): 1575–1583. Published online 2021 Feb 18. doi: 10.1200/JCO.20.02342

PMCID:: PMC8099409

Abstract Article PDF–535K

Select item 802507617.

PRIMA-1^met induces autophagy in colorectal cancer cells through upregulation of the mTOR/AMPK-ULK1-Vps34 signaling cascade

Xiao-Lan Li, Jianbiao Zhou, Chen-Jing Xia, Han Min, Zhong-Kai Lu, Zhi-Rong Chen

Oncol Rep. 2021 May; 45(5): 86. Published online 2021 Mar 31. doi: 10.3892/or.2021.8037

Correction in:: Oncol Rep. 2024 Mar; 51(3): 44.

PMCID:: PMC8025076

Abstract Article PDF–1.6M

Select item 790480518.

Transketolase regulates sensitivity to APR-246 in p53-null cells independently of oxidative stress modulation

Julia V. Milne, Bonnie Z. Zhang, Kenji M. Fujihara, Swati Dawar, Wayne A. Phillips, Nicholas J. Clemons

Sci Rep. 2021; 11: 4480. Published online 2021 Feb 24. doi: 10.1038/s41598-021-83979-3

PMCID:: PMC7904805

Abstract Article PDF–2.0M

Select item 786338319.

A thiol‐bound drug reservoir enhances APR‐246‐induced mutant p53 tumor cell death

Sophia Ceder, Sofi E Eriksson, Emarndeena H Cheteh, Swati Dawar, Mariana Corrales Benitez, Vladimir J N Bykov, Kenji M Fujihara, Mélodie Grandin, Xiaodun Li, Susanne Ramm, Corina Behrenbruch, Kaylene J Simpson, Frédéric Hollande, Lars Abrahmsen, Nicholas J Clemons, Klas G Wiman

EMBO Mol Med. 2021 Feb 5; 13(2): e10852. Published online 2020 Dec 14. doi: 10.15252/emmm.201910852

PMCID:: PMC7863383

Abstract Article PDF–1.8M

Select item 759922520.

New directions for emerging therapies in acute myeloid leukemia: the next chapter

Naval Daver, Andrew H. Wei, Daniel A. Pollyea, Amir T. Fathi, Paresh Vyas, Courtney D. DiNardo

Blood Cancer J. 2020 Oct; 10(10): 107. Published online 2020 Oct 30. doi: 10.1038/s41408-020-00376-1

PMCID:: PMC7599225

Abstract Article PDF–513K

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