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Medicinal Chemistry

Harvesting the power of the cell’s own protein degradation mechanisms in drug discovery

Constant production of proteins in living cells is subject to strict quality and concentration control. The ubiquitin-protease system (UPS) is one of the systems responsible for degrading misfolded and damaged proteins. Also, short-lived regulatory proteins that control many critical cellular processes, including cell cycle progression, cell proliferation and differentiation, cell signalling and transcription are degraded by UPS.1

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PROTAC drug discovery – prior preparation and planning

“By failing to prepare, you are preparing to fail” so said Benjamin Franklin, and as a veteran of early stage drug discovery you can bet that I, like you, have seen my fair share of successes but also more failures than I’d like.  

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Slides from the 4th Medicinal Chemistry & Protein Degradation Summit

The 4th Medicinal Chemistry & Protein Degradation Summit provided two days of fascinating topics and case studies about AI-assisted lead optimisation, DNA encoded libraries and the use of data and informatics in drug-discovery. We have made the following presentation slides available from Greg Makara, Paul Colbon and Yugal Sharma.

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Why drug designers will be at a disadvantage without AI

We spoke to John Griffin, CSO at Numerateto find out how AI is changing drug discovery and development. Numerate is a drug design company applying cutting-edge AI to transform the process of small molecule drug design.

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Controlling the fate of cancer cells with SF3B1 modulators

Andrew Cook has worked in the pharmaceutical industry for over 20 years. Throughout his career, he has endeavoured to do things differently, a little out of the ordinary, leading him to his work at H3 Biomedicine on splice modulators. “Part of the reason it attracted me” he says, “is it’s so different. It’s a natural product-based drug discovery effort, and I had never done that before”.

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Integrating AI and HCI for drug discovery

Bringing new therapeutics to patients is easier said than done due to the enormous intrinsic complexity behind being efficacious and safe.

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Why NOW for Targeting RNA with Small Molecules?

Before tackling the question of why everyone thinks drugging RNA is so hard, one might ask why drugging proteins is considered to be so easy (at least by comparison). Put differently, why were proteins first?

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Accelerating the Medicinal Chemistry Design Cycle

MedChemNet and Future Medicinal Chemistry editors Jasmine Harris and Ben Walden interviewed Emma Parmee from Merck & Co at the Global Medicinal Chemistry and GPCR Summit.

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