Cargando…

FASCAPLYSIN as a Specific Inhibitor for CDK4: Insights from Molecular Modelling

Cyclin-dependent kinases (CDKs) play a key role in the cell cycle and are important anti-cancer drug targets. The natural product fascaplysin inhibits CDK4 with surprising selectivity (IC(50) = 0.4 µM) compared to the close homolog CDK2 (IC(50) = 500 µM). Free energy calculations of the positively c...

Descripción completa

Detalles Bibliográficos
Autores principales:	Shafiq, Muhammad Imtiaz, Steinbrecher, Thomas, Schmid, Ralf
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Public Library of Science 2012
Materias:	Research Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3419161/ https://www.ncbi.nlm.nih.gov/pubmed/22905154 http://dx.doi.org/10.1371/journal.pone.0042612

Ejemplares similares

Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer
por: Plangger, Adelina, et al.
Publicado: (2021)

Comparison of the Inhibitory Binding Modes Between the Planar Fascaplysin and Its Nonplanar Tetrahydro-β-carboline Analogs in CDK4
por: Liang, Yan, et al.
Publicado: (2021)

The Marine-Derived Kinase Inhibitor Fascaplysin Exerts Anti-Thrombotic Activity
por: Ampofo, Emmanuel, et al.
Publicado: (2015)

Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK
por: Oh, Taek-In, et al.
Publicado: (2017)

Cytotoxic Effects of Fascaplysin against Small Cell Lung Cancer Cell Lines
por: Hamilton, Gerhard
Publicado: (2014)

Total Syntheses and Preliminary Biological Evaluation of Brominated Fascaplysin and Reticulatine Alkaloids and Their Analogues
por: Zhidkov, Maxim E., et al.
Publicado: (2019)

Marine-Derived Lead Fascaplysin: Pharmacological Activity, Total Synthesis, and Structural Modification
por: Wang, Chao, et al.
Publicado: (2023)

A pyrone remodeling strategy to access diverse heterocycles: application to the synthesis of fascaplysin natural products
por: Palani, Vignesh, et al.
Publicado: (2020)

Study of Structure–Activity Relationships of the Marine Alkaloid Fascaplysin and Its Derivatives as Potent Anticancer Agents
por: Zhidkov, Maxim E., et al.
Publicado: (2022)

A New Mild Method for Synthesis of Marine Alkaloid Fascaplysin and Its Therapeutically Promising Derivatives
por: Tryapkin, Oleg A., et al.
Publicado: (2023)

Fascaplysin Exerts Anti-Cancer Effects through the Downregulation of Survivin and HIF-1α and Inhibition of VEGFR2 and TRKA
por: Oh, Taek-In, et al.
Publicado: (2017)

Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines
por: Rath, Barbara, et al.
Publicado: (2018)

Alkaloids of fascaplysin are effective conventional chemotherapeutic drugs, inhibiting the proliferation of C6 glioma cells and causing their death in vitro
por: Bryukhovetskiy, Igor, et al.
Publicado: (2017)

Inducible deletion of CDK4 and CDK6 – deciphering CDK4/6 inhibitor effects in the hematopoietic system
por: Maurer, Barbara, et al.
Publicado: (2020)

CDK4/6 inhibitor: from quiescence to senescence
por: Yoshida, Akihiro, et al.
Publicado: (2015)

CDK 4/6 inhibitors for the treatment of meningioma
por: Young, Jacob S., et al.
Publicado: (2022)

Co-targeting CDK2 and CDK4/6 overcomes resistance to aromatase and CDK4/6 inhibitors in ER+ breast cancer
por: Al-Qasem, Abeer J., et al.
Publicado: (2022)

9-Methylfascaplysin Is a More Potent Aβ Aggregation Inhibitor than the Marine-Derived Alkaloid, Fascaplysin, and Produces Nanomolar Neuroprotective Effects in SH-SY5Y Cells
por: Sun, Qingmei, et al.
Publicado: (2019)

Clinical CDK4/6 inhibitors induce selective and immediate dissociation of p21 from cyclin D-CDK4 to inhibit CDK2
por: Pack, Lindsey R., et al.
Publicado: (2021)

Molecular Modeling and Design Studies of Purine Derivatives as Novel CDK2 Inhibitors
por: Zhang, Gaomin, et al.
Publicado: (2018)

Molecular mechanisms of resistance to CDK4/6 inhibitors in breast cancer: A review
por: Pandey, Kamal, et al.
Publicado: (2019)

Analysing the Effect of Mutation on Protein Function and Discovering Potential Inhibitors of CDK4: Molecular Modelling and Dynamics Studies
por: N, Nagasundaram, et al.
Publicado: (2015)

Mechanistic understanding of the role of ATRX in senescence provides new insight for combinatorial therapies with CDK4 inhibitors.
por: Kovatcheva, Marta, et al.
Publicado: (2017)

Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor
por: Whittaker, Steven R., et al.
Publicado: (2018)

Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16
por: Dixon-Clarke, Sarah E., et al.
Publicado: (2017)

Allostery governs Cdk2 activation and differential recognition of CDK inhibitors
por: Majumdar, Abir, et al.
Publicado: (2021)

A hypothesis-driven approach identifies CDK4 and CDK6 inhibitors as candidate drugs for treatments of adrenocortical carcinomas
por: Hadjadj, Djihad, et al.
Publicado: (2017)

Molecular mechanism of G(1) arrest and cellular senescence induced by LEE011, a novel CDK4/CDK6 inhibitor, in leukemia cells
por: Tao, Yan-Fang, et al.
Publicado: (2017)

Molecular docking analysis of piperine with CDK2,CDK4,Cyclin D and Cyclin T proteins
por: Rekha, Umapathy Vidhya, et al.
Publicado: (2020)

Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders
por: Wu, Xuewei, et al.
Publicado: (2021)

CDK6 Immunophenotype Implicates Potential Therapeutic Application of CDK4/6 Inhibitors in Urothelial Carcinoma
por: Sun, Ran, et al.
Publicado: (2022)

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines
por: Coxon, Christopher R., et al.
Publicado: (2016)

Lipid–Protein Interactions in Niemann–Pick Type C Disease: Insights from Molecular Modeling
por: Wheeler, Simon, et al.
Publicado: (2019)

Flavonoids as CDK1 Inhibitors: Insights in Their Binding Orientations and Structure-Activity Relationship
por: Navarro-Retamal, Carlos, et al.
Publicado: (2016)

Fascaplysin Induces Apoptosis and Ferroptosis, and Enhances Anti-PD-1 Immunotherapy in Non-Small Cell Lung Cancer (NSCLC) by Promoting PD-L1 Expression
por: Luo, Lianxiang, et al.
Publicado: (2022)

Molecular docking analysis of CDK-1 inhibitors from Chrysophyllum cainito leaves
por: Antony Prabhu, Yesudass, et al.
Publicado: (2021)

The interplay of CDK4 and CDK6 in melanoma
por: Kollmann, Karoline, et al.
Publicado: (2019)

Unraveling the genomic determinants of response to CDK4/6 inhibitors
por: Litchfield, Lacey M., et al.
Publicado: (2018)

The role of CDK4/6 inhibitors in early breast cancer
por: Gil-Gil, Miguel, et al.
Publicado: (2021)

Mechanisms and Implications of CDK4/6 Inhibitors for the Treatment of NSCLC
por: Zhang, Jinmeng, et al.
Publicado: (2021)

Cannot write session to /tmp/vufind_sessions/sess_oe6tos3lber5qn19ajem4e9hio