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Thus, UCHL1 inhibitors could serve as a viable treatment strategy against these aggressive cancers. Herein, we describe a covalent fragmentscreen that identified the chloroacetohydrazide scaffold as a covalent UCHL1 inhibitor.
This receptor is also expressed in the brain, where it helps to regulate dopamine release, making it a therapeutic target for the treatment of insomnia, pain, depression and Parkinson’s disease. This crucial role in regulating vital bodily processes makes it a highly important drug target within GPCR research. References Sun D, et al.
Sygnature Discovery offers high throughput screening along with additional hit identification tools including virtual screening, knowledge-based design, and fragmentscreening. Sygnature Discovery integrates cutting-edge automation to ensure efficiency and precision in our HTS processes.
The mission of the CCDD is to discover novel small-molecule therapeutics for the treatment of cancer and progress them to hypothesis testing phase 1 clinical trials. In terms of compound libraries, we have a high-throughput screening library of about 200,000 ligands. We can screen with many different formats and modalities.
In the fourth of his rules for air fighting , ‘Sailor’ Malan (readers may also be interested in his insights into fragmentscreening library design ) asserts that “height gives you the initiative” which can be adapted for drug design as “affinity gives you the initiative”.
Viral protease inhibitors that block enzymes critical for viral replication have long been used in the treatment of human immunodeficiency (HIV) and hepatitis C viruses. Researchers are now studying the potential of protease inhibitors for the treatment of SARS-CoV-2. For research use only. Not for use in diagnostic procedures.
While I’m not particularly keen on the use of the term ‘open source’ in this context, I have absolutely no quibble with the goal of seeking cures and treatments for diseases that are ignored by commercial drug discovery organizations.
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