Cargando…

Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation

Bcr-Abl threonine 315 to isoleucine 315 (T315I) gatekeeper mutation induced drug resistance remains an unmet clinical challenge for the treatment of chronic myeloid leukemia (CML). Chemical degradation of Bcr-Abl(T315I) protein has become a potential strategy to overcome drug resistance. Herein, we...

Descripción completa

Detalles Bibliográficos
Autores principales:	Jiang, Liang, Wang, Yuting, Li, Qian, Tu, Zhengchao, Zhu, Sihua, Tu, Sanfang, Zhang, Zhang, Ding, Ke, Lu, Xiaoyun
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Elsevier 2021
Materias:	Original Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8148061/ https://www.ncbi.nlm.nih.gov/pubmed/34094836 http://dx.doi.org/10.1016/j.apsb.2020.11.009

Ejemplares similares

Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl(T315I) inhibitor overcoming acquired imatinib resistance
por: Lu, Xiaoyun, et al.
Publicado: (2017)

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)

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

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)

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)

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)

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)

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

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

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)

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)

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

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)

EPS8 regulates proliferation, apoptosis and chemosensitivity in BCR-ABL positive cells via the BCR-ABL/PI3K/AKT/mTOR pathway
por: Huang, Rui, et al.
Publicado: (2018)

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

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)

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)

Detection of BCR-ABL T315I mutation by peptide nucleic acid directed PCR clamping and by peptide nucleic acid FISH
por: Rosso, Valentina, et al.
Publicado: (2015)

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)

Single amino acid–based PROTACs trigger degradation of the oncogenic kinase BCR–ABL in chronic myeloid leukemia (CML)
por: Zhang, Jianchao, et al.
Publicado: (2023)

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)

The Activity of Novel BCR-ABL Small-Molecule Degraders Containing Pyrimidine Rings and Their Role in Overcoming Drug Resistance
por: Zhang, Xu, et al.
Publicado: (2022)

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

Successful treatment of T315I BCR-ABL mutated lymphoid blast phase chronic myeloid leukemia with chimeric antigen receptor T cell therapy followed by dasatinib
por: Zhang, Hao, et al.
Publicado: (2020)

Validation of a Drosophila model of wild-type and T315I mutated BCR-ABL1 in chronic myeloid leukemia: an effective platform for treatment screening
por: Outa, Amani Al, et al.
Publicado: (2020)

PB1711: DROPLET DIGITAL PCR DETECTION OF THE T315I BCR::ABL1 KD MUTATION IN ADULT PH-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
por: Cardinali, Deborah, et al.
Publicado: (2023)

Synthesis and biological evaluation of niclosamide PROTACs
por: Munoz, Erick, et al.
Publicado: (2022)

T315I mutation of BCR-ABL1 into human Philadelphia chromosome-positive leukemia cell lines by homologous recombination using the CRISPR/Cas9 system
por: Tamai, Minori, et al.
Publicado: (2018)

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

Discovery of a small molecule targeting SET-PP2A interaction to overcome BCR-ABLT315I mutation of chronic myeloid leukemia
por: Wang, Shuzhen, et al.
Publicado: (2015)

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)

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)

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)

Expanding the Diversity of Allosteric Bcr-Abl Inhibitors
por: Deng, Xianming, et al.
Publicado: (2010)

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)

Identification of novel tyrosine kinase inhibitors for drug resistant T315I mutant BCR-ABL: a virtual screening and molecular dynamics simulations study
por: Banavath, Hemanth Naick, et al.
Publicado: (2014)

JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo
por: Wang, Jie, et al.
Publicado: (2022)

P370: EFFICACY AND SAFETY OF THE THIRD-GENERATION TKI OLVEREMBATINIB IN ADULTS PH/BCR-ABL1-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA WITH T315I MUTATION AND RELAPSED/REFRACTORY DISEASE
por: Liu, Weiyang, et al.
Publicado: (2023)

CDK4/CDK6 inhibition as a novel strategy to suppress the growth and survival of BCR-ABL1(T315I)+ clones in TKI-resistant CML
por: Schneeweiss-Gleixner, Mathias, et al.
Publicado: (2019)

Cannot write session to /tmp/vufind_sessions/sess_v4meb7l11fm78h00bsj1gooepp