Pin1 Inhibition Exerts Potent Activity Against Acute Myeloid Leukemia The unique peptidyl prolyl cis trans isomerase pin1 has been reported to promote tumorigenesis through upregulation of numerous cancer driving pathways. although pin1 is a key drug target for treating acute promyelocytic leukemia (apl) caused by a fusion oncogene, much less is known about the role of pin1 in other heterogeneous leukemia. Background the increasing genomic complexity of acute myeloid leukemia (aml), the most common form of acute leukemia, poses a major challenge to its therapy. to identify potent therapeutic targets with the ability to block multiple cancer driving pathways is thus imperative. the unique peptidyl prolyl cis trans isomerase pin1 has been reported to promote tumorigenesis through upregulation of.
Pin1 Inhibition Exerts Potent Activity Against Acute Myeloid Leukemia The expression of cancer related pin1 downstream oncoproteins in shpin1 (pin1 knockdown) and pin1 inhibitor all trans retinoic acid (atra) treated leukemia cells were examined by western blot. It is found that pin1 mrna and protein was significantly increased in both de novo leukemia clinical samples and multiple leukemia cell lines, compared with healthy controls and is a promising therapeutic target to block multiple cancer driving pathways in aml. backgroundthe increasing genomic complexity of acute myeloid leukemia (aml), the most common form of acute leukemia, poses a major. Here, we report the discovery of p1d 34, a first in class and potent protac degrader of pin1, which induced pin1 degradation with a dc 50 value of 177 nm and exhibited potent degradation dependent anti proliferative activities in a panel of acute myeloid leukemia (aml) cell lines. in contrast, pin1 inhibitor sulfopin did not show activity. Gianni, m. et al. inhibition of the peptidyl prolyl isomerase pin1 enhances the responses of acute myeloid leukemia cells to retinoic acid via stabilization of rarα and pml rarα. cancer res. 69.
Pin1 Inhibition Exerts Potent Activity Against Acute Myeloid Leukemia Here, we report the discovery of p1d 34, a first in class and potent protac degrader of pin1, which induced pin1 degradation with a dc 50 value of 177 nm and exhibited potent degradation dependent anti proliferative activities in a panel of acute myeloid leukemia (aml) cell lines. in contrast, pin1 inhibitor sulfopin did not show activity. Gianni, m. et al. inhibition of the peptidyl prolyl isomerase pin1 enhances the responses of acute myeloid leukemia cells to retinoic acid via stabilization of rarα and pml rarα. cancer res. 69. Pin1 overexpression induces chromosome instability and tumorigenesis. pin1 inactivates and activates more than 26 tumor suppressors and 56 oncogenes, respectively. in cancer stem cells, multiple pin1 substrates play an important role. pin1 regulates the tumorigenesis and expansion of cscs in leukemia and breast cancer. Correction to: pin1 inhibition exerts potent activity against acute myeloid leukemia through blocking multiple cancer driving pathways. xiaolan lian 1,2,3 na1, yu min lin 2 na1, shingo kozono 2, megan k. herbert 2, xin li 1, xiaohong yuan 1, jiangrui guo 1, yafei guo 1, min tang 1, jia lin 1, yiping huang 1, bixin wang 1, chenxi qiu 2, cheng yu.
Pdf Pin1 Inhibition Exerts Potent Activity Against Acute Pin1 overexpression induces chromosome instability and tumorigenesis. pin1 inactivates and activates more than 26 tumor suppressors and 56 oncogenes, respectively. in cancer stem cells, multiple pin1 substrates play an important role. pin1 regulates the tumorigenesis and expansion of cscs in leukemia and breast cancer. Correction to: pin1 inhibition exerts potent activity against acute myeloid leukemia through blocking multiple cancer driving pathways. xiaolan lian 1,2,3 na1, yu min lin 2 na1, shingo kozono 2, megan k. herbert 2, xin li 1, xiaohong yuan 1, jiangrui guo 1, yafei guo 1, min tang 1, jia lin 1, yiping huang 1, bixin wang 1, chenxi qiu 2, cheng yu.
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