scholarly journals Mechanistic Insights into a CDK9 Inhibitor Via Orthogonal Proteomics Methods

2021 ◽  
Author(s):  
J. Adam Hendricks ◽  
Nigel Beaton ◽  
Alexey Chernobrovkin ◽  
Eric Miele ◽  
Ghaith M. Hamza ◽  
...  
Keyword(s):  
Cdk9 Inhibitor

scholarly journals Repression of Mcl-1 expression by the CDC7/CDK9 inhibitor PHA-767491 overcomes bone marrow stroma-mediated drug resistance in AML

2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Eimear O’ Reilly ◽  
Sukhraj Pal S. Dhami ◽  
Denis V. Baev ◽  
Csaba Ortutay ◽  
Anna Halpin-McCormick ◽  
...  
Keyword(s):  
Bone Marrow ◽  
Drug Resistance ◽  
Bone Marrow Stroma ◽  
Marrow Stroma ◽  
Cdk9 Inhibitor

CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia

2018 ◽  
Vol 37 (4) ◽  
pp. 625-635 ◽  
Author(s):  
Muhammed H. Rahaman ◽  
Yingyi Yu ◽  
Longjin Zhong ◽  
Julian Adams ◽  
Frankie Lam ◽  
...  
Keyword(s):  
Acute Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Orally Bioavailable ◽  
Cdk9 Inhibitor ◽  
Acute Myeloid

scholarly journals Nuclear Progestin Receptor Phosphorylation by Cdk9 Is Required for the Expression of Mmp15, a Protease Indispensable for Ovulation in Medaka

Cells ◽  
2019 ◽  
Vol 8 (3) ◽  
pp. 215 ◽  
Author(s):  
Katsueki Ogiwara ◽  
Takayuki Takahashi
Keyword(s):  
Critical Role ◽  
Cdk Inhibitor ◽  
Vertebrate Species ◽  
Dependent Protein Kinase ◽  
Progestin Receptor ◽  
Follicle Rupture ◽  
Dependent Protein ◽  
Ecm Degradation ◽  
Cdk9 Inhibitor

Ovulation denotes the discharge of fertilizable oocytes from ovarian follicles. Follicle rupture during ovulation requires extracellular matrix (ECM) degradation at the apex of the follicle. In the teleost medaka, an excellent model for vertebrate ovulation studies, LH-inducible matrix metalloproteinase 15 (Mmp15) plays a critical role during rupture. In this study, we found that follicle ovulation was inhibited not only by roscovitine, the cyclin-dependent protein kinase (CDK) inhibitor, but also by CDK9-inhibitor II, a specific CDK9 inhibitor. Inhibition of follicle ovulation by the inhibitors was accompanied by the suppression of Mmp15 expression in the follicle. In follicles treated with the inhibitors, the formation of the phosphorylated nuclear progestin receptor (Pgr) was inhibited. Roscovitine treatment caused a reduction in the binding of Pgr to the promoter region of mmp15. The expression of Cdk9 and cyclin I (Ccni), and their association in the follicle was demonstrated, suggesting that Cdk9 and Ccni may be involved in the phosphorylation of Pgr in vivo. LH-induced follicular expression of ccni/Ccni was also shown. This study is the first to report the involvement of CDK in ECM degradation during ovulation in a vertebrate species.

CDK9 Inhibitor FIT-039 Suppresses Viral Oncogenes E6 and E7 and Has a Therapeutic Effect on HPV-Induced Neoplasia

2018 ◽  
Vol 24 (18) ◽  
pp. 4518-4528 ◽  
Author(s):  
Masahiko Ajiro ◽  
Hiroyuki Sakai ◽  
Hiroshi Onogi ◽  
Makoto Yamamoto ◽  
Eriko Sumi ◽  
...  
Keyword(s):  
Therapeutic Effect ◽  
Viral Oncogenes ◽  
E6 And E7 ◽  
Cdk9 Inhibitor

Design of Tat-Activated Cdk9 Inhibitor

2018 ◽  
Vol 25 (2) ◽  
pp. 807-817 ◽  
Author(s):  
Yunjie Zhao ◽  
Hao Chen ◽  
Chenghang Du ◽  
Yiren Jian ◽  
Haotian Li ◽  
...  
Keyword(s):  
Cdk9 Inhibitor

Inhibitory effect of CDK9 inhibitor FIT-039 on hepatitis B virus propagation

2016 ◽  
Vol 133 ◽  
pp. 156-164 ◽  
Author(s):  
Tomohisa Tanaka ◽  
Kaori Okuyama-Dobashi ◽  
Shuko Murakami ◽  
Wenjia Chen ◽  
Toru Okamoto ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Inhibitory Effect ◽  
Virus Propagation ◽  
B Virus ◽  
Cdk9 Inhibitor

scholarly journals The CDK9 Inhibitor Dinaciclib Exerts Potent Apoptotic and Antitumor Effects in Preclinical Models of MLL-Rearranged Acute Myeloid Leukemia

2015 ◽  
Vol 76 (5) ◽  
pp. 1158-1169 ◽  
Author(s):  
Adele Baker ◽  
Gareth P. Gregory ◽  
Inge Verbrugge ◽  
Lev Kats ◽  
Joshua J. Hilton ◽  
...  
Keyword(s):  
Acute Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Preclinical Models ◽  
Antitumor Effects ◽  
Cdk9 Inhibitor ◽  
Acute Myeloid
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