Epidermal growth factor receptor inhibitor cancer drug gefitinib modulates cell growth and differentiation of acute myeloid leukemia cells via histamine receptors.

Manisha Yadav,Abhishek Singh,Harish Kumar,Geeta Rao,Bandana Chakravarti,Anagha Gurjar,Shalini Dogra,Sapana Kushwaha,Achchhe Lal Vishwakarma,Prem N. Yadav,Dipak Datta,Anil Kumar Tripathi,Naibedya Chattopadhyay,Arun Kumar Trivedi,Sabyasachi Sanyal

Biochimica et Biophysica Acta (BBA) - General Subjects（2016）

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摘要

•Gefitinib induces cytostasis and differentiation in EGFR-deficient AML cells.•Gefitinib reduces cAMP level and increases ERK phosphorylation in AML cells.•Gefitinib modulates multiple GPCRs including histamine receptors.•H2R and H4R modulation suppresses gefitinib functions in AML cells.•H2R/H4R modulation also suppresses gefitinib effects in EGFR-rich cells.

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4-MH,AML,CML,cAMP,CRE,EGFR,ER,FSK,GPCR,H1R,H2R,H3R,H4R,HDC,Her2,NFAT,NFAT-RE,NSCLC,PDE,PEA,RAMH,RTK,TKI

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