Paper
Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.
Published Oct 1, 2011 · H. Zeng, David B. Belanger, Patrick J. Curran
Bioorganic & medicinal chemistry letters
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32
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0
Influential Citations
Abstract
Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.
Study Snapshot
Novel imidazo[1,2-a]pyrazin-8-amines show low-nanomolar Brk inhibition activity, high selectivity towards other kinases, and desirable DMPK properties for exploring Brk as an oncology target.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
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References
Brk/PTK6 signaling in normal and cancer cell models.
Overexpression of Brk in tumors leads to increased proliferation, survival, and migration, potentially guiding the development of targeted cancer therapies and preventing chemo-resistance.
2010·68citations·J. Ostrander et al.·Current opinion in pharmacology
Current opinion in pharmacology
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors show potential for anti-tumor activity and improved off-target inhibition.
2010·16citations·David B. Belanger et al.·Bioorganic & medicinal chemistry letters
Bioorganic & medicinal chemistry letters
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors show promising potential, with compound 10i identified as a lead compound with promising overall profile.
2010·40citations·David B. Belanger et al.·Bioorganic & medicinal chemistry letters
Bioorganic & medicinal chemistry letters
Breast tumor kinase and extracellular signal-regulated kinase 5 mediate Met receptor signaling to cell migration in breast cancer cells
Brk and ERK5 are important downstream effectors of Met signaling in breast cancer cells, and targeting ERK5 kinase activity or inhibiting Brk/ERK5 complex formation may provide an additional means of blocking cell migration.
2010·76citations·Nancy E. Castro et al.·Breast Cancer Research : BCR
Breast Cancer Research : BCR
BRK phosphorylates PSF promoting its cytoplasmic localization and cell cycle arrest.
BRK phosphorylates PSF, a breast cancer cell marker, promoting cytoplasmic localization and cell cycle arrest during EGF stimulation.
2009·67citations·K. Lukong et al.·Cellular signalling
Cellular signalling
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Two lead compounds identified in Euphorbia thymifolia Linn show potential anticancer activity against breast cancer.
2024·0citations·Vasavi Kumblekar et al.·F1000Research
F1000Research
Protein tyrosine kinase 6 regulates activation of SRC kinase
PTK6 promotes SRC activation in cancer cells, with unique functions and coexpressed in prostate and breast cancer cells.
2022·6citations·Wanian M. Alwanian et al.·The Journal of Biological Chemistry
The Journal of Biological Chemistry
Recent Advances in PROTACs for Drug Targeted Protein Research
PROTACs show promising clinical efficacy in treating various cancers, neurodegenerative diseases, inflammations, and other diseases by degrading specific proteins.
2022·33citations·T. Yao et al.·International Journal of Molecular Sciences
International Journal of Molecular Sciences
Synthesis, characterization, biological evaluation and molecular docking of novel amide derivatives of indole-1,2,4-oxadiazole clubbed thiazoles
Novel amide derivatives of indole-1,2,4-oxadiazole clubbed thiazoles show potent antiproliferative activity against various human cancer cell lines, with good oral bioavailability and no toxicity observed.
2022·0citations·Veera Reddy Yenireddy et al.·Chemical Data Collections
Chemical Data Collections
Putting the BRK on breast cancer: From molecular target to therapeutics
BRK is a key oncogenic kinase in breast cancer, leading to the development of inhibitors, but none have progressed into clinical phase.
2021·19citations·H. L. Ang et al.·Theranostics
Theranostics
The therapeutic potential of PROTACs
PROTACs show potential as therapeutic agents for treating multiple diseases by modulating target biology through proteasomal degradation, but require differentiated medicines and intellectual property protection.
2020·31citations·Andrew B. Benowitz et al.·Expert Opinion on Therapeutic Patents
Expert Opinion on Therapeutic Patents
Targeting protein tyrosine kinase 6 in cancer.
Targeting PTK6 may have beneficial therapeutic outcomes in some cancers, such as breast and prostate cancer, by reducing tumorigenesis and inhibiting tumor growth in animal models.
2020·15citations·Milica B Gilic et al.·Biochimica et biophysica acta. Reviews on cancer
Biochimica et biophysica acta. Reviews on cancer
Effective synthesis of benzimidazoles-imidazo[1,2-a]pyrazine conjugates: A comparative study of mono-and bis-benzimidazoles for antitumor activity.
The novel series of imidazo[1,2-a]pyrazine-benzimidazoles show antitumor activity for various cancer cell types, with monobenzimidazole showing better activity than bisbenzimidazole.
2019·23citations·Iqubal Singh et al.·European journal of medicinal chemistry
European journal of medicinal chemistry