ArticleNature communications2016
Diversity-oriented synthetic strategy for developing a chemical modulator of protein-protein interaction.
Article in Nature communications, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed.
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- Revisiting Pyrimidine-Embedded Molecular Frameworks to Probe the Unexplored Chemical Space for Protein-Protein Interactions.Accounts of chemical research · 2024Article
- Medium-Sized Ring Expansion Strategies: Enhancing Small-Molecule Library Development.Molecules (Basel, Switzerland) · 2024Review
- Inflachromene ameliorates Parkinson's disease by targeting Nrf2-binding Keap1.Chemical science · 2024Article
- Drug discovery by targeting the protein-protein interactions involved in autophagy.Acta pharmaceutica Sinica. B · 2023Review
- Synthesis and Conformational Analysis of Hydantoin-Based Universal Peptidomimetics.The Journal of organic chemistry · 2023Article
- Scaffold Remodelling of Diazaspirotricycles Enables Synthesis of Diverse spChemistry (Weinheim an der Bergstrasse, Germany) · 2023Article
- Bis(oxiranes) Containing Cyclooctane Core: Synthesis and Reactivity towards NaNMolecules (Basel, Switzerland) · 2022Article
- Recent Advances in Divergent Synthetic Strategies for Indole-Based Natural Product Libraries.Molecules (Basel, Switzerland) · 2022Review
- Inhibition of ACE2-Spike Interaction by an ACE2 Binder Suppresses SARS-CoV-2 Entry.Angewandte Chemie (International ed. in English) · 2022Article
- Design and Synthesis of Conformationally Diverse Pyrimidine-Embedded Medium/Macro- and Bridged CyclesFrontiers in chemistry · 2022Article
- Limonin as a Starting Point for the Construction of Compounds with High Scaffold Diversity.Angewandte Chemie (International ed. in English) · 2021Article
- Dabrafenib Promotes Schwann Cell Differentiation by Inhibition of the MEK-ERK Pathway.Molecules (Basel, Switzerland) · 2021Article
- Phenotypic Discovery of Neuroprotective Agents by Regulation of Tau Proteostasis via Stress-Responsive Activation of PERK Signaling.Angewandte Chemie (International ed. in English) · 2021Article
- Nature-inspired remodeling of (aza)indoles to meta-aminoaryl nicotinates for late-stage conjugation of vitamin BNature communications · 2020Article
- Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.Chemical science · 2020Article
- A one-step, atom economical synthesis of thieno[2,3-European journal of organic chemistry · 2019Article
- Green and Facile Assembly of Diverse FusedMolecules (Basel, Switzerland) · 2019Article
- A divergent synthetic pathway for pyrimidine-embedded medium-sized azacycles through an N-quaternizing strategy.Chemical science · 2019Article
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Diversity-oriented synthesis (DOS) can provide a collection of diverse and complex drug-like small molecules, which is critical in the development of new chemical probes for biological research of undruggable targets. However, the design and synthesis of small-molecule libraries with improved biological relevance as well as maximized molecular diversity represent a key challenge. Herein, we employ functional group-pairing strategy for the DOS of a chemical library containing privileged substructures, pyrimidodiazepine or pyrimidine moieties, as chemical navigators towards unexplored bioactive chemical space. To validate the utility of this DOS library, we identify a new small-molecule inhibitor of leucyl-tRNA synthetase-RagD protein-protein interaction, which regulates the amino acid-dependent activation of mechanistic target of rapamycin complex 1 signalling pathway. This work highlights that privileged substructure-based DOS strategy can be a powerful research tool for the construction of drug-like compounds to address challenging biological targets.
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