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The results showed that the decoction incubation reduced the levels of CCNA1, CCND1, CCND2, CCNH, CDKN1B, MCM2, ORC6L, and WEE1 and increased the levels of CDC7, CDK6, CDK7, E2F3, and RB1 (Table 1).
ARG (6 [micro]/m1) lowered the level of regulatory proteins involved in the [G.sub.1]/S checkpoint signaling, including cyclin CDK7, cyclin E, CDK2, p-CDK, and NPAT (Fig.
Triptolide downregulated the cell cycle-related genes E2F2 E2F3, E2F5, CDKN2C, CDK7, CDC23, and SMAD3; the MAPK signaling pathway genes FOS, CASP3, JUND, KRAS, MAP2K2; and the Wnt signaling pathway genes WNT4, MYC, and AXIN2.
Milciclib (PHA-848125AC) is a small molecule inhibitor of several cyclin dependent kinases such as CDK1, CDK4, CDK5 and CDK7.
Syros Pharmaceuticals announced that it will present new preclinical data on SY-1365, its first-in-class selective cyclin-dependent kinase 7 inhibitor currently in a Phase 1 clinical trial focused on ovarian and breast cancers, and on SY-5609, its selective oral CDK7 inhibitor that the company has named as its next development candidate, at the American Association for Cancer Research Annual Meeting taking place March 29-April 3 in Atlanta.
New data on SY-1365, a first-in-class selective CDK7 inhibitor currently in a Phase 1 clinical trial, suggest that RB pathway alterations are predictive of response in preclinical models of high-grade ovarian cancer and support the ongoing clinical investigation of SY-1365 in patient populations enriched for RB pathway alterations.
These data, the first clinical data reported on a selective CDK7 inhibitor, were highlighted in an oral plenary session at the 30th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium in Dublin.
CDK7 and ESR1 are critical for in vitro cell growth in both CDK4/6 inhibitor-sensitive and CDK4/6 inhibitor-resistant cells.
The Company also announced the first preclinical data on its class of highly selective oral CDK7 inhibitors, which showed significant anti-proliferative activity in preclinical models of breast and ovarian cancers.
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- CDK2-associated dual specificity phosphatase
- CDK2-associated dual-specificity phosphatase
- CDK4 gene
- CDK4 gene
- CDK4 inhibitor p16-INK4, INK4a
- CDK4B inhibitor
- CDK5-Binding Protein
- CDK6 inhibitor p18
- CDK8 protein kinase
- CDK8-like cyclin-dependent kinase
- CDK9-associated C-type protein