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A 'Three‐in‐One' Multifunctional Probe for Bcl‐2/Mcl‐1 Profiling and Visualizing in Situ

Autor: Ziqian Wang, Zongwei Guo, Xiaodong Zhang, Ting Song, Keke Cao, Zhichao Zhang, Junjie Zhu, Nianzhe He

Publikováno v: Zhang, X, Wang, Z, Guo, Z, Song, T, He, N, Zhu, J, Cao, K & Zhang, Z 2021, ' A "three-in-one" multi-functional probe for Bcl-2/Mcl-1 profiling and visualizing in situ ', ChemBioChem, vol. 22, no. 2, pp. 326-329 . https://doi.org/10.1002/cbic.202000441

Bcl-2 and Mcl-1, the two arms of the anti-apoptotic Bcl-2 family proteins, have been identified as key regulators of apoptosis and effective therapeutic targets of cancer. However, no small molecular probe is capable of profiling and visualizing both

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b03d14a629b9bf136acd84ff45713646
https://doi.org/10.1002/cbic.202000441

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Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands

Autor: Zhichao Zhang, Junjie Zhu, Ziqian Wang, Yafei Guo, Nianzhe He, Zongwei Guo, Ting Song, Keke Cao, Xiaodong Zhang, Anhui Wang, Cuili Niu

Publikováno v: Journal of Medicinal Chemistry. 62:8152-8163

Proteolysis targeting chimera (PROTAC) recruits an E3 ligase to a target protein to induce its ubiquitination and subsequent degradation. We reported success in the development of two PROTACs (C3 and C5) that potently and selectively induce the degra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18fb8dd5be3b73de5abad0ed2f2e72be
https://doi.org/10.1021/acs.jmedchem.9b00919

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Discovery of selective Mcl-1 inhibitors via structure-based design and structure-activity relationship analysis

Autor: Peng Liu, Ziqian Wang, Xinxin Yan, Zhichao Zhang, Zongwei Guo, Nianzhe He, Hongbo Chen

Publikováno v: Biochemical and Biophysical Research Communications. 512:921-926

Based on Nap-1, a Mcl-1/Bcl-2 dual inhibitor reported by our group, we carried out a structure-guided molecular design and structure-activity relationship (SAR) analysis to study structural features contributing to Mcl-1 binding selectivity and affin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c6c498a34e636cc6f5e11930abbd23e
https://doi.org/10.1016/j.bbrc.2019.03.102

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A novel turn-on fluorescent probe for selective sensing and imaging of glutathione in live cells and organisms

Autor: Peng Liu, Zongwei Guo, Xiufen Yan, Xiaodong Zhang, Ziqian Wang, Zhichao Zhang, Nianzhe He, Dasha Xia

Publikováno v: The Analyst. 144:3260-3266

We synthesized six 1-oxo-1H-phenalene-2,3-dicarbonitrile (OPD)-based probes with various leaving groups using an arylthioether linker and for the first time identified the probe O-NH2 capable of highly selective detection of glutathione over cysteine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0921498ff171ad7e5f3b2a0bcff178a
https://doi.org/10.1039/c9an00115h

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Cover Feature: A 'Three‐in‐One' Multifunctional Probe for Bcl‐2/Mcl‐1 Profiling and Visualizing in Situ (ChemBioChem 2/2021)

Autor: Junjie Zhu, Ting Song, Zhichao Zhang, Zongwei Guo, Keke Cao, Xiaodong Zhang, Ziqian Wang, Nianzhe He

Publikováno v: ChemBioChem. 22:262-262

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ba1f02634b617edc5f43994788150d30
https://doi.org/10.1002/cbic.202000861

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Proteome-Wide Identification of On- and Off-Targets of Bcl-2 Inhibitors in Native Biological Systems by Using Affinity-Based Probes (AfBPs)

Autor: Ziqian Wang, Peng Liu, Peiran Wang, Xiaodong Zhang, Ting Song, Zhichao Zhang, Zongwei Guo, Nianzhe He

Publikováno v: Chembiochem : a European journal of chemical biology. 19(21)

Selective inhibition of proteins of the Bcl-2 family by small-molecule inhibitors is a promising new approach in drug discovery. However, information about how these molecules interact with their cellular targets (on- and off-) is highly limited. We

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc7704b6461d9124fca3ad9e57bb68cb
https://pubmed.ncbi.nlm.nih.gov/30133085

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