Cargando…

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on biophysical measurements of intracellular t...

Descripción completa

Detalles Bibliográficos
Autores principales:	Almqvist, Helena, Axelsson, Hanna, Jafari, Rozbeh, Dan, Chen, Mateus, André, Haraldsson, Martin, Larsson, Andreas, Molina, Daniel Martinez, Artursson, Per, Lundbäck, Thomas, Nordlund, Pär
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Nature Publishing Group 2016
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4820820/ https://www.ncbi.nlm.nih.gov/pubmed/27010513 http://dx.doi.org/10.1038/ncomms11040

Ejemplares similares

CETSA-based target engagement of taxanes as biomarkers for efficacy and resistance
por: Langebäck, Anette, et al.
Publicado: (2019)

Current Advances in CETSA
por: Tolvanen, Tuomas Aleksi
Publicado: (2022)

Monitoring structural modulation of redox-sensitive proteins in cells with MS-CETSA
por: Sun, Wendi, et al.
Publicado: (2019)

Thymidylate synthase polymorphism and survival of colorectal cancer patients treated with 5-fluorouracil
por: Ulrich, C M, et al.
Publicado: (2002)

Thymidylate synthase and methylenetetrahydrofolate reductase gene polymorphisms: relationships with 5-fluorouracil sensitivity
por: Etienne, M-C, et al.
Publicado: (2004)

Thymidylate synthase expression and activity: relation to S-phase parameters and 5-fluorouracil sensitivity.
por: Mirjolet, J. F., et al.
Publicado: (1998)

Trapping of 5-Fluorodeoxyuridine Monophosphate by Thymidylate Synthase Confers Resistance to 5-Fluorouracil
por: Kurasaka, Chinatsu, et al.
Publicado: (2022)

Reply: Thymidylate synthase polymorphism and survival of colorectal cancer patients treated with 5-fluorouracil
por: Iacopetta, B, et al.
Publicado: (2002)

5-Fluorouracil targets thymidylate synthase in the selective suppression of T(H)17 cell differentiation
por: Wang, Juan, et al.
Publicado: (2016)

Multi-level gene expression profiles affected by thymidylate synthase and 5-fluorouracil in colon cancer
por: Xi, Yaguang, et al.
Publicado: (2006)

Dynamic Modulation of Thymidylate Synthase Gene Expression and Fluorouracil Sensitivity in Human Colorectal Cancer Cells
por: Wakasa, Kentaro, et al.
Publicado: (2015)

High Expression of Thymidylate Synthase Leads to Resistance to 5‐Fluorouracil in Biliary Tract Carcinoma in vitro
por: Habara, Kazuto, et al.
Publicado: (2001)

Enhancement of 5-fluorouracil-induced cytotoxicity by leucovorin in 5-fluorouracil-resistant gastric cancer cells with upregulated expression of thymidylate synthase
por: Nakamura, Ayako, et al.
Publicado: (2013)

Effect of Hammerhead Ribozyme against Human Thymidylate Synthase on the Cytotoxicity of Thymidylate Synthase Inhibitors
por: Kobayashi, Hiroyuki, et al.
Publicado: (1995)

Structure of the Varicella Zoster Virus Thymidylate Synthase Establishes Functional and Structural Similarities as the Human Enzyme and Potentiates Itself as a Target of Brivudine
por: Hew, Kelly, et al.
Publicado: (2015)

Prolonged and enhanced suppression of thymidylate synthase by weekly 24-h infusion of high-dose 5-fluorouracil
por: Yeh, K-H, et al.
Publicado: (2000)

Pancytopenia and Severe Gastrointestinal Toxicities Associated with 5-Fluorouracil in a Patient with Thymidylate Synthase (TYMS) Polymorphism
por: Wang, Bo, et al.
Publicado: (2016)

Apigenin enhances apoptosis induction by 5-fluorouracil through regulation of thymidylate synthase in colorectal cancer cells
por: Yang, Changwon, et al.
Publicado: (2021)

Trichinella pseudospiralis vs. T. spiralis thymidylate synthase gene structure and T. pseudospiralis thymidylate synthase retrogene sequence
por: Jagielska, Elżbieta, et al.
Publicado: (2014)

Trifluridine/tipiracil overcomes the resistance of human gastric 5-fluorouracil-refractory cells with high thymidylate synthase expression
por: Matsuoka, Kazuaki, et al.
Publicado: (2018)

Study of Thymidylate Synthase (TS) and Dihydropyrimidine Dehydrogenase (DPD) Expressions on 5-Fluorouracil in Oral Squamous Cell Carcinoma
por: Akhter, Khaleda, et al.
Publicado: (2019)

MicroRNA‐375‐3p enhances chemosensitivity to 5‐fluorouracil by targeting thymidylate synthase in colorectal cancer
por: Xu, Fei, et al.
Publicado: (2020)

Regulation of 5‐fluorodeoxyuridine monophosphate‐thymidylate synthase ternary complex levels by autophagy confers resistance to 5‐fluorouracil
por: Nishizawa, Nana, et al.
Publicado: (2022)

Conservation and Role of Electrostatics in Thymidylate Synthase
por: Garg, Divita, et al.
Publicado: (2015)

A polymorphism in the enhancer region of the thymidylate synthase promoter influences the survival of colorectal cancer patients treated with 5-fluorouracil
por: Iacopetta, B, et al.
Publicado: (2001)

Liver-only metastatic colorectal cancer patients and thymidylate synthase polymorphisms for predicting response to 5-fluorouracil-based chemotherapy
por: Graziano, F, et al.
Publicado: (2008)

The effect of dose and interval between 5-fluorouracil and leucovorin on the formation of thymidylate synthase ternary complex in human cancer cells.
por: Drake, J. C., et al.
Publicado: (1995)

Analysis of the Thymidylate Synthase Gene Structure in Colorectal Cancer Patients and Its Possible Relation with the 5-Fluorouracil Drug Response
por: Calascibetta, A., et al.
Publicado: (2010)

Transcriptional Activation and Cell Cycle Block Are the Keys for 5-Fluorouracil Induced Up-Regulation of Human Thymidylate Synthase Expression
por: Ligabue, Alessio, et al.
Publicado: (2012)

Acquired resistance to 5-fluorouracil via HSP90/Src-mediated increase in thymidylate synthase expression in colon cancer
por: Ahn, Ji-Young, et al.
Publicado: (2015)

Uridine triacetate for severe 5-fluorouracil toxicity in a patient with thymidylate synthase gene variation: Potential pharmacogenomic implications
por: Baldeo, Candice, et al.
Publicado: (2018)

Evaluating serum level of thymidylate synthase in post burn keloid patients before and after intralesional injection of 5-fluorouracil
por: Ezzat Mohamad, Noha, et al.
Publicado: (2022)

Substrate Activation in Flavin-Dependent Thymidylate Synthase
por: Mishanina, Tatiana V., et al.
Publicado: (2014)

Concerted versus Stepwise Mechanism in Thymidylate Synthase
por: Islam, Zahidul, et al.
Publicado: (2014)

Expression of thymidylate synthase in gastric cancer patients treated with 5-fluorouracil and doxorubicin-based adjuvant chemotherapy after curative resection
por: Choi, J-H, et al.
Publicado: (2001)

MicroRNA-433 negatively regulates the expression of thymidylate synthase (TYMS) responsible for 5-fluorouracil sensitivity in HeLa cells
por: Gotanda, Keisuke, et al.
Publicado: (2013)

MicroRNA-330 inhibited cell proliferation and enhanced chemosensitivity to 5-fluorouracil in colorectal cancer by directly targeting thymidylate synthase
por: Xu, Weidong, et al.
Publicado: (2017)

Intracellular drug bioavailability: a new predictor of system dependent drug disposition
por: Mateus, André, et al.
Publicado: (2017)

Intracellular quantitative detection of human thymidylate synthase engagement with an unconventional inhibitor using tetracysteine-diarsenical-probe technology
por: Ponterini, Glauco, et al.
Publicado: (2016)

Thymidylate synthase expression in circulating tumor cells: A new tool to predict 5‐fluorouracil resistance in metastatic colorectal cancer patients
por: Abdallah, Emne Ali, et al.
Publicado: (2015)

Cannot write session to /tmp/vufind_sessions/sess_qd8srncm3d23cqhujd53qg5qgg