Epidermal growth factor receptor inhibitor cancer drug gefitinib modulates cell growth and differentiation of acute myeloid leukemia cells via histamine receptors
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- 作者：Manisha Yadava ; Abhishek Kumar Singha ; Harish Kumara ; Geeta Raoa ; Bandana Chakravartib ; Anagha Gurjara ; Shalini Dograc ; Sapana Kushwahaa ; Achchhe Lal Vishwakarmad ; Prem Narayan Yadavc ; Dipak Dattaa ; Anil Kumar Tripathie ; Naibedya Chattopadhyayf ; Arun Kumar Trivedia ; Sabyasachi Sanyala ; sanyal@cdri.res.in" class="auth_mail" title="E-mail the corresponding author
- 关键词：4-MH ; 4-methylhistamine ; AML ; acute myelogenous leukemia ; CML ; chronic myelogenous leukemia ; cAMP ; cyclic adenosine monophosphate ; CRE ; cAMP response element ; EGFR ; epidermal growth factor receptor ; ER ; estrogen receptor alpha ; FSK ; Forskolin ; GPCR ; G-protein coupled receptor ; H1R ; H1 receptor ; H2R ; H2 receptor ; H3R ; H3 receptor ; H4R ; H4 receptor ; HDC ; histidine decarboxylase ; Her2 ; human epidermal growth factor receptor 2 ; NFAT ; nuclear factor of activated T-cells ; NFAT-RE ; NFAT-response eleme
- 刊名：Biochimica et Biophysica Acta (BBA) - General Subjects
- 出版年：2016
- 出版时间：October 2016
- 年：2016
- 卷：1860
- 期：10
- 页码：2178-2190
- 全文大小：2461 K
文摘
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Gefitinib induces cytostasis and differentiation in EGFR-deficient AML cells.
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Gefitinib reduces cAMP level and increases ERK phosphorylation in AML cells.
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Gefitinib modulates multiple GPCRs including histamine receptors.
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H2R and H4R modulation suppresses gefitinib functions in AML cells.
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H2R/H4R modulation also suppresses gefitinib effects in EGFR-rich cells.