TY - JOUR
T1 - Molecular docking studies of angiogenesis target protein HIF-1α and genistein in breast cancer
AU - Mukund, Vidya
AU - Saddala, Madhu Sudhana
AU - Farran, Batoul
AU - Mannavarapu, Mastan
AU - Alam, Afroz
AU - Nagaraju, Ganji Purnachandra
N1 - Publisher Copyright:
© 2019 Elsevier B.V.
PY - 2019/6/15
Y1 - 2019/6/15
N2 - Therapeutic inhibition of hypoxia inducible factor-1α (HIF-1α) action has emerged as a potential approach for managing several diseases including breast cancer (BC). Genistein has been found to exert anti-malignant activity. However, its mechanisms of action remain unknown. Studies indicate that it could act by downregulating HIF-1α. Based on these findings, we investigated whether genistein could reduce HIF-1α in BC cell lines. Furthermore, we performed molecular docking studies to characterize the sites of interaction between genistein and HIF-1α. In the present investigation, we prove, for the first time, that genistein downregulates HIF-1α in BC cells. Molecular docking analysis also revealed that genistein binds to the FIH-1 binding site of HIF-1α protein. These findings thus indicate that genistein and/or HIF-1α antagonists could be a potential treatment for BC.
AB - Therapeutic inhibition of hypoxia inducible factor-1α (HIF-1α) action has emerged as a potential approach for managing several diseases including breast cancer (BC). Genistein has been found to exert anti-malignant activity. However, its mechanisms of action remain unknown. Studies indicate that it could act by downregulating HIF-1α. Based on these findings, we investigated whether genistein could reduce HIF-1α in BC cell lines. Furthermore, we performed molecular docking studies to characterize the sites of interaction between genistein and HIF-1α. In the present investigation, we prove, for the first time, that genistein downregulates HIF-1α in BC cells. Molecular docking analysis also revealed that genistein binds to the FIH-1 binding site of HIF-1α protein. These findings thus indicate that genistein and/or HIF-1α antagonists could be a potential treatment for BC.
KW - Breast cancer
KW - Docking
KW - Genistein
KW - HIF-1α
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U2 - 10.1016/j.gene.2019.03.062
DO - 10.1016/j.gene.2019.03.062
M3 - Article
C2 - 30930227
AN - SCOPUS:85063646950
SN - 0378-1119
VL - 701
SP - 169
EP - 172
JO - Gene
JF - Gene
ER -