Concepedia

Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7

Jason Marineau, Kristin B. Hamman, Shanhu Hu, Sydney Alnemy, Janessa Mihalich, A. Kabro, Kenneth Matthew Whitmore, Dana K. Winter, Stéphanie Roy, Stéphane Ciblat,

Journal of Medicinal Chemistry · 2021 · 84 citations · 16 references

DOIFull text

Open access

Concepts

Abstract

displays potent inhibition of CDK7 in cells and demonstrates strong efficacy in mouse xenograft models when dosed as low as 2 mg/kg.

References

16

A simple method for displaying the hydropathic character of a protein

Jack Kyte, Russell F. Doolittle · Journal of Molecular Biology · 1982 · 23.1K citations

, , +12

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

Nicholas Kwiatkowski, Tinghu Zhang, Peter B. Rahl et al. · Nature · 2014 · 900 citations · Full text

, , +12

CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer

Yubao Wang, Tinghu Zhang, Nicholas Kwiatkowski et al. · Cell · 2015 · 485 citations · Full text

, , +14

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

Wei‐Sheng Huang, Shuangying Liu, Dong Zou et al. · Journal of Medicinal Chemistry · 2016 · 404 citations · Full text

, , +13

Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II

Stéphane Larochelle, Ramon Amat, Kira Glover-Cutter et al. · Nature Structural & Molecular Biology · 2012 · 391 citations · Full text

, , +16