Results 201 to 210 of about 417,703 (296)

Inhibition of CDK9 enhances AML cell death induced by combined venetoclax and azacitidine

Molecular Oncology, EarlyView.
The CDK9 inhibitor AZD4573 downregulates c‐MYC and MCL‐1 to induce death of cytarabine (AraC)‐resistant AML cells. This enhances VEN + AZA‐induced cell death significantly more than any combination of two of the three drugs in AraC‐resistant AML cells.
Shuangshuang Wu, Jianlei Zhao, Aaban Asfar Azmi, Avanti Gupte, Jenna Thibodeau, Shuang Liu, Jinli Yang, Guan Wang, Holly Edwards, Lisa A. Polin, Juiwanna Kushner, Sijana H. Dzinic, Kathryn White, Julie Boerner, Maik Hüttemann, Jay Yang, Yue Wang, Jeffrey W. Taub, Yubin Ge   +18 more
wiley   +1 more source

A conifer metabolite corrects episodic ataxia type 1 by voltage sensor-mediated ligand activation of Kv1.1. [PDF]

Proc Natl Acad Sci U S A
Manville RW, Foglia L, Yoshimura RF, Hogenkamp DJ, Nguyen A, Yu A, Abbott GW.   +6 more
europepmc   +1 more source

Phosphoinositide regulates dynamic movement of the S4 voltage sensor in the second repeat in two-pore channel 3. [PDF]

J Biol Chem, 2021
Hirazawa K, Tateyama M, Kubo Y, Shimomura T.   +3 more
europepmc   +1 more source

A synthetic benzoxazine dimer derivative targets c‐Myc to inhibit colorectal cancer progression

Molecular Oncology, EarlyView.
Benzoxazine dimer derivatives bind to the bHLH‐LZ region of c‐Myc, disrupting c‐Myc/MAX complexes, which are evaluated from SAR analysis. This increases ubiquitination and reduces cellular c‐Myc. Impairing DNA repair mechanisms is shown through proteomic analysis.
Nicharat Sriratanasak, Bodee Nutho, Worawat Wattanathana, Narumon Phaonakrop, Bunnatut Panasawatwong, Katharina Erlenbach‐Wuensch, Sittiruk Roytrakul, Regine Schneider‐Stock, Pithi Chanvorachote   +8 more
wiley   +1 more source

Different fluorescent labels report distinct components of spHCN channel voltage sensor movement. [PDF]

J Gen Physiol
Wojciechowski MN, McKenzie CE, Hung A, Kuanyshbek A, Soh MS, Reid CA, Forster IC.   +6 more
europepmc   +1 more source

Adaptaquin is selectively toxic to glioma stem cells through disruption of iron and cholesterol metabolism

Molecular Oncology, EarlyView.
Adaptaquin selectively kills glioma stem cells while sparing differentiated brain cells. Transcriptomic and proteomic analyses show Adaptaquin disrupts iron and cholesterol homeostasis, with iron chelation amplifying cytotoxicity via cholesterol depletion, mitochondrial dysfunction, and elevated reactive oxygen species.
Adrien M. Vaquié, Davod R. Shah, Eliane E. S. Brechbühl, Michael McNicholas, Zhaoyang Xu, John H. Stockley, Laura Morcom, Diana Gold Diaz, Gemma C. Girdler, Rachel V. Seear, Gabriel Balmus, Rajiv R. Ratan, Harry Bulstrode, James A. Nathan, Manav Pathania, Kevin M. Brindle, David H. Rowitch   +16 more
wiley   +1 more source

Cholesterol modulates the structural dynamics of the paddle motif loop of KvAP voltage sensor. [PDF]

Curr Res Struct Biol
Das A, Bysack A, Raghuraman H.
europepmc   +1 more source

Patient‐specific pharmacogenomics demonstrates xCT as predictive therapeutic target in colon cancer with possible implications in tumor connectivity

Molecular Oncology, EarlyView.
This study integrates transcriptomic profiling of matched tumor and healthy tissues from 32 colorectal cancer patients with functional validation in patient‐derived organoids, revealing dysregulated metabolic programs driven by overexpressed xCT (SLC7A11) and SLC3A2, identifying an oncogenic cystine/glutamate transporter signature linked to ...
Marco Strecker, Keren Zohar, Martin Böttcher, Thomas Wartmann, Henry Freudenstein, Maximilian Doelling, Mihailo Andric, Wenjie Shi, Or Kakhlon, Katrin Hippe, Beatrix Jahnke, Dimitrios Mougiakakos, Franziska Baenke, Daniel Stange, Roland S. Croner, Michal Linial, Ulf D. Kahlert   +16 more
wiley   +1 more source

Loose Coupling between the Voltage Sensor and the Activation Gate in Mammalian HCN Channels Suggests a Gating Mechanism. [PDF]

Int J Mol Sci
Wu X, Cunningham KP, Bruening-Wright A, Pandey S, Larsson HP.   +4 more
europepmc   +1 more source

Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na⁺ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases. [PDF]

Molecules, 2022
Coquerel Q, Legendre C, Frangieh J, Waard S, Montnach J, Cmarko L, Khoury J, Hassane CS, Bréard D, Siegler B, Fajloun Z, De Pomyers H, Mabrouk K, Weiss N, Henrion D, Richomme P, Mattei C, Waard M, Le Ray AM, Legros C.   +19 more
europepmc   +1 more source