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Combination of PAKs inhibitors IPA-3 and PF-3758309 effectively suppresses colon carcinoma cell growth by perturbing DNA damage response.

• Authors : Dukel, Muzaffer¹ (AUTHOR); Fiskin, Kayahan² (AUTHOR)

• Source: International Journal of Radiation Biology. 2023, Vol. 99 Issue 2, p340-354. 15p.

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Mechanism by Which PF-3758309, a Pan Isoform Inhibitor of p21-Activated Kinases, Blocks Reactivation of HIV-1 Latency.

• Authors : Vargas, Benni¹ (AUTHOR); Boslett, James² (AUTHOR); Yates, Nathan^2,3 (AUTHOR)

• Source: Biomolecules (2218-273X). Jan2023, Vol. 13 Issue 1, p100. 12p.

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Mechanism by Which PF-3758309, a Pan Isoform Inhibitor of p21-Activated Kinases, Blocks Reactivation of HIV-1 Latency

• Authors : Benni Vargas; James Boslett; Nathan Yates

Subjects: HIV-1; latency; p21-activated kinase

• Source: Biomolecules, Vol 13, Iss 1, p 100 (2023)

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PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings.

• Authors : Ryu, Byung¹; Lee, Hyuk²; Kim, Seong-Ho²

Subjects: *METASTASIS; *LUNG cancer; *MATRIX metalloproteinases

• Source: Molecular & Cellular Biochemistry. Apr2014, Vol. 389 Issue 1/2, p69-77. 9p.

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Association of the Epithelial-to-Mesenchymal Transition (EMT) Phenotype with Responsiveness to the p21-Activated Kinase Inhibitor, PF-3758309, in Colon Cancer Models

• Authors : Todd M Pitts; Gillian N Kulikowski; Aik-Choon eTan

Subjects: colorectal cancer; EMT; PF-3758309

• Source: Frontiers in Pharmacology, Vol 4 (2013)

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Tumor p-glycoprotein correlates with efficacy of PF-3758309 in in vitro and in vivo models of colorectal cancer.

• Authors : Erica Lynn Bradshaw-Pierce; Todd M Pitts; Aik-Choon eTan

Subjects: P-Glycoprotein; colorectal cancer; PF-3758309

• Source: Frontiers in Pharmacology, Vol 4 (2013)

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A Novel AMPK Inhibitor Sensitizes Pancreatic Cancer Cells to Ferroptosis Induction.

• Authors : Schneider, Carolin¹; Hilbert, Jorina¹; Genevaux, Franziska²

• Source: Advanced Science. 8/21/2024, Vol. 11 Issue 31, p1-18. 18p.

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Association of the epithelial-to-mesenchymal transition phenotype with responsiveness to the p21-activated kinase inhibitor, PF-3758309, in colon cancer models

• Authors : Pitts, Todd M.; Kulikowski, Gillian N.; Tan, Aik-Choon

Subjects: Pharmacology (medical); Pharmacology

• Source: Frontiers in Pharmacology ; volume 4 ; ISSN 1663-9812

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Tumor P-Glycoprotein Correlates with Efficacy of PF-3758309 in in vitro and in vivo Models of Colorectal Cancer

• Authors : Bradshaw-Pierce, Erica Lynn; Pitts, Todd M.; Tan, Aik-Choon

Subjects: Pharmacology (medical); Pharmacology

• Source: Frontiers in Pharmacology ; volume 4 ; ISSN 1663-9812

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Figure 6—figure supplement 3. Kinase inhibitors which have MELK kinase as an off-target do not reduce mitotic protein synthesis. ; (a) Protein synthesis rates of G2 (blue) and mitotic (red) L1210 cells after 3 hr treatment with 1 µM SNS-032 (CDK2 inhibitor) or 50 nM Tozasertib (Aurora kinase inhibitor), or 5 hr treatment with 1 µM GSK 626616 (DYRK kinase inhibitor). (n = 5–8 separate cultures). p-Values obtained using two-tailed Welch’s t-test. (b) Ratio of protein synthesis rates between mitotic and G2 L1210 cells after 3 hr treatment with OTSSP167, Defactinib (also known as PF-04554878), PF-3758309 (also known as PF-309) or Nintedanib (also known as BIBF 1120), all of which inhibit MELK kinase with sub-micromolar affinity (Klaeger et al., 2017). Light blue area indicates the typical range observed in control cells. (n = 4 separate cultures). Note that OTSSP167 is a nonspecific multikinase inhibitor (Klaeger et al., 2017), making it likely that MELK kinase does not contribute to the drug-induced mitotic growth reduction. (c) Representative FACS scatter plots indicating the cell cycle distribution after 6 hr treatment with indicated chemicals. The relative portion of cells in G1/S, G2 and mitosis are indicated (mean ± SD). (n = 4–6 separate cultures). Note that OTSSP167 reduced mitotic entry, a phenotype typical for CDK1 inhibition, while the alternative MELK inhibitors did not display similar cell cycle profile. CDK1 is one of the off-targets of OTSSP167 (Klaeger et al., 2017).

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