A5057251114- Protein Degradation and Inhibitors
- Ubiquitin and proteasome pathways
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Synthetic Organic Chemistry Methods
- Carbohydrate Chemistry and Synthesis
- Software Testing and Debugging Techniques
- History of Science and Medicine
- Marine Sponges and Natural Products
- Diverse Historical and Scientific Studies
- HIV Research and Treatment
- Advanced Proteomics Techniques and Applications
- Scientific Computing and Data Management
- Computational Drug Discovery Methods
- Topic Modeling
- 14-3-3 protein interactions
- Machine Learning in Materials Science
University of Dundee
2022-2024
Cancer Research UK Scotland Institute
2021-2022
Cancer Research UK
2022
AstraZeneca (United Kingdom)
2020
University of Glasgow
2017
Targeted protein degradation has recently emerged as a novel option in drug discovery. Natural half-life is expected to affect the efficacy of degrading agents, but what extent it influences target not been systematically explored. Using simple mathematical modeling degradation, we find that natural dramatic effect on level induced by degrader agent which can pose significant hurdles screening efforts. Moreover, show upon for degraders short-lived proteins, agents stall synthesis, such GSPT1...
With a resurgence in interest covalent drugs, there is need to identify new moieties capable of cysteine bond formation that are differentiated from commonly employed systems such as acrylamide. Herein, we report on the discovery alkynyl benzoxazine and dihydroquinazoline reaction with cysteine. Their utility alternative electrophilic warheads for chemical biological probes drug molecules demonstrated through site-selective protein modification incorporation into kinase scaffolds. A potent...
Summary Targeted protein degradation has recently emerged as a novel option in drug discovery. Natural half-life is expected to affect the efficacy of degrading agents, but what extent it influences target not been systematically explored. Using mathematical modelling degradation, we demonstrate that natural dramatic effect on level induced by degrader agent which can pose significant hurdles screening efforts. Moreover, show upon for degraders short-lived proteins, agents stall synthesis,...
Convergent total syntheses of the furanocembranoids 7-epi-pukalide and 7-acetylsinumaximol B have been achieved using a one-pot Knoevenagel condensation thioether-mediated furan-forming reaction. Furan formation proceeds via sulfur ylide results in rapid introduction structural complexity during coupling two highly functionalised fragments. The targets prepared 16 steps from (R)-perillyl alcohol.
Fragment-based hit identification (FBHI) allows proportionately greater coverage of chemical space using fewer molecules than traditional high-throughput screening approaches. However, effectively exploiting this advantage is highly dependent on the library design. Solubility, stability, complexity, chemical/shape diversity, and synthetic tractability for fragment elaboration are all critical aspects, molecule design remains a time-consuming task computational medicinal chemists. Artificial...
First published: 19 December 2022 Print ISBN:9783527350131| Online ISBN:9783527836208| DOI:10.1002/9783527836208 © 2023 Wiley-VCH GmbH