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2012 1
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2016 2
2017 1
2019 1
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p65BTK is a novel potential actionable target in KRAS-mutated/EGFR-wild type lung adenocarcinoma.
Giordano F, Vaira V, Cortinovis D, Bonomo S, Goedmakers J, Brena F, Cialdella A, Ianzano L, Forno I, Cerrito MG, Giovannoni R, Ferri GL, Tasciotti E, Vicent S, Damarco F, Bosari S, Lavitrano M, Grassilli E. Giordano F, et al. J Exp Clin Cancer Res. 2019 Jun 14;38(1):260. doi: 10.1186/s13046-019-1199-7. J Exp Clin Cancer Res. 2019. PMID: 31200752 Free PMC article.
The effects of p65BTK inhibition by BTK Tyrosine Kinase Inhibitors (TKIs) (Ibrutinib, AVL-292, RN486) and first-generation EGFR-TKIs (Gefitinib, Erlotinib) on cell viability were evaluated by MTT. ...
The effects of p65BTK inhibition by BTK Tyrosine Kinase Inhibitors (TKIs) (Ibrutinib, AVL-292, RN486) and first-generation EGF …
Bruton's tyrosine kinase (BTK) inhibitors in clinical trials.
Burger JA. Burger JA. Curr Hematol Malig Rep. 2014 Mar;9(1):44-9. doi: 10.1007/s11899-013-0188-8. Curr Hematol Malig Rep. 2014. PMID: 24357428 Review.
Other BTK inhibitors in earlier clinical development include CC-292 (AVL-292), and ONO-4059. In CLL and MCL, ibrutinib characteristically induces redistribution of malignant B cells from tissue sites into the peripheral blood, along with rapid resolution of e …
Other BTK inhibitors in earlier clinical development include CC-292 (AVL-292), and ONO-4059. In CLL and MCL, ibrutinib …
Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders.
Robak T, Robak E. Robak T, et al. Expert Opin Investig Drugs. 2012 Jul;21(7):921-47. doi: 10.1517/13543784.2012.685650. Epub 2012 May 22. Expert Opin Investig Drugs. 2012. PMID: 22612424 Review.
The search terms used were Bruton's tyrosine kinase (Btk) inhibitors, PCI-32765, GDC-0834, LFM-A13, AVL-101, AVL-292, spleen tyrosine kinase (Syk) inhibitors, R343, R406, R112, R788, fostamatinib, BAY-61-3606, C-61, piceatannol, Lyn, imatinib, nilotinib, bafe …
The search terms used were Bruton's tyrosine kinase (Btk) inhibitors, PCI-32765, GDC-0834, LFM-A13, AVL-101, AVL-292, s …
BTK inhibition is a potent approach to block IgE-mediated histamine release in human basophils.
Smiljkovic D, Blatt K, Stefanzl G, Dorofeeva Y, Skrabs C, Focke-Tejkl M, Sperr WR, Jaeger U, Valenta R, Valent P. Smiljkovic D, et al. Allergy. 2017 Nov;72(11):1666-1676. doi: 10.1111/all.13166. Epub 2017 Apr 20. Allergy. 2017. PMID: 28328081 Free PMC article.
METHODS: We examined the effects of four BTK inhibitors (ibrutinib, dasatinib, AVL-292, and CNX-774) on IgE-dependent activation and histamine release in blood basophils obtained from allergic patients (n=11) and nonallergic donors (n=5). ...Dasatinib and ibrutinib …
METHODS: We examined the effects of four BTK inhibitors (ibrutinib, dasatinib, AVL-292, and CNX-774) on IgE-dependent activati …
Bruton's Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells.
Wang X, Wong J, Sevinsky CJ, Kokabee L, Khan F, Sun Y, Conklin DS. Wang X, et al. Mol Cancer Ther. 2016 Sep;15(9):2198-208. doi: 10.1158/1535-7163.MCT-15-0813. Epub 2016 Jun 2. Mol Cancer Ther. 2016. PMID: 27256378 Free PMC article.
In this study, we show that recently developed inhibitors of BTK, such as ibrutinib (PCI-32765), AVL-292, and CGI-1746, reduce breast cancer cell survival and prevent drug-resistant clones from arising. ...HER2(+) breast cancer cell proliferation is blocked by ibrut …
In this study, we show that recently developed inhibitors of BTK, such as ibrutinib (PCI-32765), AVL-292, and CGI-1746, reduce …
Optimized Near-IR Fluorescent Agents for in Vivo Imaging of Btk Expression.
Kim E, Yang KS, Kohler RH, Dubach JM, Mikula H, Weissleder R. Kim E, et al. Bioconjug Chem. 2015 Aug 19;26(8):1513-8. doi: 10.1021/acs.bioconjchem.5b00152. Epub 2015 Jun 9. Bioconjug Chem. 2015. PMID: 26017814 Free PMC article.
To develop robust companion imaging diagnostics for in vivo use, we set out to explore the effects of red wavelength fluorochrome modifications of two highly potent irreversible Btk inhibitors, Ibrutinib and AVL-292. Surprisingly, we found that subtle chemical diffe …
To develop robust companion imaging diagnostics for in vivo use, we set out to explore the effects of red wavelength fluorochrome modificati …
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a N,9-Diphenyl-9H-purin-2-amine Scaffold.
Ge Y, Jin Y, Wang C, Zhang J, Tang Z, Peng J, Liu K, Li Y, Zhou Y, Ma X. Ge Y, et al. ACS Med Chem Lett. 2016 Sep 21;7(12):1050-1055. doi: 10.1021/acsmedchemlett.6b00235. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994736 Free PMC article.
The activity of the subject compound as determined by the CCK-8 method and apoptosis analysis validated that inhibitor 10j is slightly more potent than AVL-292 and ibrutinib. The results of these experimental explorations suggested that 10j could serve as a valuable …
The activity of the subject compound as determined by the CCK-8 method and apoptosis analysis validated that inhibitor 10j is slightly more …
Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer.
Kokabee L, Wang X, Sevinsky CJ, Wang WL, Cheu L, Chittur SV, Karimipoor M, Tenniswood M, Conklin DS. Kokabee L, et al. Cancer Biol Ther. 2015;16(11):1604-15. doi: 10.1080/15384047.2015.1078023. Epub 2015 Sep 18. Cancer Biol Ther. 2015. PMID: 26383180 Free PMC article.
Down regulation of this protein with RNAi or inhibition with BTK-specific inhibitors, Ibrutinib, AVL-292 or CGI-1746 decrease cell survival and induce apoptosis in prostate cancer cells. ...
Down regulation of this protein with RNAi or inhibition with BTK-specific inhibitors, Ibrutinib, AVL-292 or CGI-1746 decrease …