Their primary mechanism of action is thought to be the inhibition of phosphorylation of the retinoblastoma tumour suppressor, inducing G1 cell cycle arrest in tumour cells. Here we use mouse models of breast carcinoma and other solid tumours to show that selective CDK4/6 inhibitors not only ...
CDK4/6 Inhibitors: A Trio of Compounds with Distinct Advantages Although palbociclib was the first CDK4/6 inhibitor to demonstrate clinical efficacy (Finn et al., 2016), two others soon followed. Ribociclib is structurally very similar to palbociclib, and abemaciclib is significantly less similar...
R. Ribociclib (LEE011): mechanism of action and clinical impact of this selective cyclin-dependent kinase 4/6 inhibitor in various solid tumors. Clin. Cancer Res. 23, 3251–3262 (2017). Article CAS PubMed PubMed Central Google Scholar Gelbert, L. M. et al. Preclinical characterization ...
44. Finn RS, Crown JP, Lang I, et al. The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first–line treatment of oestrogen receptor-positive, HER2-negative, ...
[2] Tripathy, D., Bardia, A. & Sellers, W. R. Ribociclib (LEE011): mechanism of action and clinical impact of this selective cyclin-dependent kinase 4/6 inhibitor in various solid tumors. Clin. Cancer Res. 23, 3251–3262 (2017) ...
The cyclin-dependent kinases 4 and 6 inhibitors are the mainstay of treatment for patients with hormone receptor-positive and HER2-negative breast cancer. The ability of these drugs to improve the outcome of patients both in the metastatic and the early
3. Klein, M.E.; Kovatcheva, M.; Davis, L.E.; Tap, W.D.; Koff, A. CDK4/6 Inhibitors: The Mechanism of Action May Not Be as Simple as Once Thought. Cancer Cell 2018, 34, 9–20. 4. O’Leary, B.; Cutts, R.J.; Liu, Y.; Hrebien, S.; Huang, X.; Fenwick, K.; And...
3. Klein, M.E.; Kovatcheva, M.; Davis, L.E.; Tap, W.D.; Koff, A. CDK4/6 Inhibitors: The Mechanism of Action May Not Be as Simple as Once Thought. Cancer Cell 2018, 34, 9–20. 4. O’Leary, B.; Cutts, R....
Palbociclib（帕博西尼），Abemaciclib（玻玛西尼）和Ribociclib是目前三种针对CDK4 / 6的特异性抑制剂。这些药物的毒性低，可广泛用于治疗各种肿瘤，在乳腺癌中应用最广泛。CDK4 / 6抑制剂既可单独使用，也可以与其他药物一起联用，其临床潜力巨大。因此，了解它们发挥抗肿瘤作用的机制显得尤为重要。如图2中列举了...
3. Klein, M.E.; Kovatcheva, M.; Davis, L.E.; Tap, W.D.; Koff, A. CDK4/6 Inhibitors: The Mechanism of Action May Not Be as Simple as Once Thought. Cancer Cell 2018, 34, 9–20. 4. O’Leary, B.; Cutts, R.J.; Liu, Y.; Hrebien, S.; Huang, X.; Fenwick, K.; And...