Английская Википедия:Dinaciclib
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Шаблон:Short description Шаблон:Infobox drug
Dinaciclib (SCH-727965) is an experimental drug that inhibits cyclin-dependent kinases (CDKs).[1] It is being evaluated in clinical trials for various cancer indications.[2]
Dinaciclib is being developed by Merck & Co. It was granted orphan drug status by the FDA in 2011.[3]
Mechanisms of action
- Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains.[4]
- Dinaciclib (SCH727665) inhibits the unfolded protein response (UPR) through a CDK1 and CDK5-dependent mechanism.[5]
Anti-tumoral action
- In melanoma
- The anti-melanoma activity of dinaciclib is dependent on p53 signaling.[6]
- In chronic lymphocytic leukemia (CLL)
- In pancreatic cancer
- Dinaciclib inhibits pancreatic cancer growth and progression in murine xenograft models.[8]
- In osteosarcoma
Role in developing neurons
In primary cultured neurons, dinaciclib regulates neurogenesis, where it reduces expression of upper layer marker Satb2, and induces CTIP2, expressed in neurons of deeper layers.[11]
Clinical trials
- Phase II
- Phase III
- A comparison of dinaciclib and ofatumumab for treatment of CLL[16]
References
External links
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite web
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:ClinicalTrialsGov
- ↑ Шаблон:ClinicalTrialsGov
- ↑ Шаблон:ClinicalTrialsGov