Cargando…

Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl(T315I) inhibitor overcoming acquired imatinib resistance

Bcr-Abl(T315I) induced drug resistance remains a major challenge to chronic myelogenous leukemia (CML) treatment. Herein, we reported GZD856 as a novel orally bioavailable Bcr-Abl(T315I) inhibitor, which strongly suppressed the kinase activities of both native Bcr-Abl and the T315I mutant with IC(50...

Descripción completa

Detalles Bibliográficos
Autores principales:	Lu, Xiaoyun, Zhang, Zhang, Ren, Xiaomei, Wang, Deping, Ding, Ke
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Taylor & Francis 2017
Materias:	Research Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010122/ https://www.ncbi.nlm.nih.gov/pubmed/28260399 http://dx.doi.org/10.1080/14756366.2016.1250757

Ejemplares similares

Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation
por: Jiang, Liang, et al.
Publicado: (2021)

Prevalence of BCR-ABL T315I Mutation in Malaysian Patients with Imatinib-Resistant Chronic Myeloid Leukemia
por: Yusoff, Yuslina Mat, et al.
Publicado: (2018)

Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism
por: Khateb, Mamduh, et al.
Publicado: (2012)

Differentiation of imatinib -resistant chronic myeloid leukemia cells with BCR-ABL-T315I mutation induced by Jiyuan Oridonin A
por: Xu, Yun, et al.
Publicado: (2023)

Sensitivity of imatinib-resistant T315I BCR-ABL CML to a synergistic combination of ponatinib and forskolin treatment
por: Oaxaca, Derrick M., et al.
Publicado: (2016)

BCR: a new target in resistance mediated by BCR/ABL-315I?
por: Haberbosch, Isabella, et al.
Publicado: (2016)

Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I
por: Mian, Afsar Ali, et al.
Publicado: (2012)

The HSP90 inhibitor KW-2478 depletes the malignancy of BCR/ABL and overcomes the imatinib-resistance caused by BCR/ABL amplification
por: Zeng, Dachuan, et al.
Publicado: (2022)

Cantharidin Overcomes Imatinib Resistance by Depleting BCR-ABL in Chronic Myeloid Leukemia
por: Sun, Xiaoyan, et al.
Publicado: (2016)

Pterostilbene downregulates BCR/ABL and induces apoptosis of T315I-mutated BCR/ABL-positive leukemic cells
por: Kawakami, Shohei, et al.
Publicado: (2022)

GZD824 overcomes FGFR1‐V561F/M mutant resistance in vitro and in vivo
por: Jiang, Kaili, et al.
Publicado: (2021)

Mechanistic Insights Into Co-Administration of Allosteric and Orthosteric Drugs to Overcome Drug-Resistance in T315I BCR-ABL1
por: Zhang, Hao, et al.
Publicado: (2022)

Targeting BCR-ABL(+) stem/progenitor cells and BCR-ABL-T315I mutant cells by effective inhibition of the BCR-ABL-Tyr177-GRB2 complex
por: Chen, Min, et al.
Publicado: (2017)

Crizotinib acts as ABL1 inhibitor combining ATP-binding with allosteric inhibition and is active against native BCR-ABL1 and its resistance and compound mutants BCR-ABL1(T315I) and BCR-ABL1(T315I-E255K)
por: Mian, Afsar Ali, et al.
Publicado: (2021)

Targeting the PTP1B‐Bcr‐Abl1 interaction for the degradation of T315I mutant Bcr‐Abl1 in chronic myeloid leukemia
por: Elgehama, Ahmed, et al.
Publicado: (2022)

The chimeric ubiquitin ligase SH2-U-box inhibits the growth of imatinib-sensitive and resistant CML by targeting the native and T315I-mutant BCR-ABL
por: Ru, Yi, et al.
Publicado: (2016)

The novel anticancer agent JNJ-26854165 is active in chronic myeloid leukemic cells with unmutated BCR/ABL and T315I mutant BCR/ABL through promoting proteosomal degradation of BCR/ABL proteins
por: You, Liangshun, et al.
Publicado: (2016)

Semi-random mutagenesis profile of BCR-ABL during imatinib resistance acquirement in K562 cells
por: Dong, Yan, et al.
Publicado: (2017)

Target Inhibition of CBP Induced Cell Senescence in BCR-ABL- T315I Mutant Chronic Myeloid Leukemia
por: Yang, Ke, et al.
Publicado: (2021)

Expression of chronic myeloid leukemia oncogenes BCR-ABL (P210) and BCR-ABL (T315I) affect cellular and humoral innate immunity in Drosophila melanogaster
por: Abubaker, Dana, et al.
Publicado: (2022)

AHI-1 interacts with BCR-ABL and modulates BCR-ABL transforming activity and imatinib response of CML stem/progenitor cells
por: Zhou, Liang L., et al.
Publicado: (2008)

Overcoming the imatinib-resistant BCR-ABL mutants with new ureidobenzothiazole chemotypes endowed with potent and broad-spectrum anticancer activity
por: El-Damasy, Ashraf K., et al.
Publicado: (2023)

Pristimerin induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation by blocking NF-κB signaling and depleting Bcr-Abl
por: Lu, Zhongzheng, et al.
Publicado: (2010)

The Proteolytic Activity of Separase in BCR-ABL-Positive Cells Is Increased by Imatinib
por: Haaß, Wiltrud, et al.
Publicado: (2012)

Identification of Drug Combinations Containing Imatinib for Treatment of BCR-ABL+ Leukemias
por: Kang, Yunyi, et al.
Publicado: (2014)

A Small Molecule Inhibitor, OGP46, Is Effective against Imatinib-Resistant BCR-ABL Mutations via the BCR-ABL/JAK-STAT Pathway
por: Wei, Liuya, et al.
Publicado: (2020)

Anti-leukemic activity of axitinib against cells harboring the BCR-ABL T315I point mutation
por: Okabe, Seiichi, et al.
Publicado: (2015)

Targeting SOS1 overcomes imatinib resistance with BCR-ABL independence through uptake transporter SLC22A4 in CML
por: Liu, Yanjun, et al.
Publicado: (2021)

Anthelmintic niclosamide suppresses transcription of BCR-ABL fusion oncogene via disabling Sp1 and induces apoptosis in imatinib-resistant CML cells harboring T315I mutant
por: Jin, Bei, et al.
Publicado: (2018)

Correction to: Pristimerin induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation by blocking NF-κB signaling and depleting Bcr-Abl
por: Lu, Zhongzheng, et al.
Publicado: (2021)

Nickel pyrithione induces apoptosis in chronic myeloid leukemia cells resistant to imatinib via both Bcr/Abl-dependent and Bcr/Abl-independent mechanisms
por: Lan, Xiaoying, et al.
Publicado: (2016)

Imatinib and tyrosine kinase inhibition, in the management of BCR-ABL negative myeloproliferative disorders
por: Mesa, Ruben A
Publicado: (2007)

I13 overrides resistance mediated by the T315I mutation in chronic myeloid leukemia by direct BCR-ABL inhibition
por: Gao, Congying, et al.
Publicado: (2023)

BCR-ABL1-independent PI3Kinase activation causing imatinib-resistance
por: Quentmeier, Hilmar, et al.
Publicado: (2011)

Inhibition of BCR/ABL Protein Expression by miR-203 Sensitizes for Imatinib Mesylate
por: Li, Yajuan, et al.
Publicado: (2013)

AML with BCR-ABL1 Fusion treated with Imatinib, a Hypomethylating Agent and Venetoclax
por: Low, Soon Khai, et al.
Publicado: (2022)

GZD824 as a FLT3, FGFR1 and PDGFRα Inhibitor Against Leukemia In Vitro and In Vivo
por: Wang, Yuting, et al.
Publicado: (2020)

Hyperdiploidy associated with T315I mutation in BCR-ABL kinase domain in an accelerated phase-chronic myeloid leukemia case
por: Al-Achkar, Walid, et al.
Publicado: (2014)

P210(T315I-BCR/ABL)转基因小鼠模型的建立与鉴定
Publicado: (2015)

BCR-ABL1 transcript decline ratio combined BCR-ABL1(IS) as a precise predictor for imatinib response and outcome in the patients with chronic myeloid leukemia
por: Cai, Zhimei, et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_tlqs85jfisajkddt1g7ihrjqbh