A review of volumetric titration as an efficient method for the quantification of ions and compounds in lithium-ion battery components DOI
M. Loghavi,

Mohsen Babaiee,

Rahim Eqra

et al.

Chemical Papers, Journal Year: 2023, Volume and Issue: 77(12), P. 7395 - 7408

Published: Sept. 21, 2023

Language: Английский

One-pot domino synthesis of 1H-isochromene and pyran carbonitrile from pyrazole aldehyde derivatives as potential anti-diabetic and antioxidant targets DOI
Periyasamy Monisha, Singamoorthy Amalraj,

Peramaiyan Gangapriya

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1311, P. 138308 - 138308

Published: April 10, 2024

Language: Английский

Citations

1
Identification of Suitable Target/E3 Ligase Pairs for PROTAC Development using a Rapamycin-induced Proximity Assay (RiPA) DOI Creative Commons
Bikash Adhikari, Katharina Schneider, Mathias Diebold

et al.

eLife, Journal Year: 2024, Volume and Issue: 13

Published: July 26, 2024

The development of proteolysis targeting chimeras (PROTACs), which induce the degradation target proteins by bringing them into proximity with cellular E3 ubiquitin ligases, has revolutionized drug development. While human genome encodes more than 600 different current PROTACs use only a handful them, drastically limiting their full potential. Furthermore, many PROTAC campaigns fail because selected ligase candidates are unable to particular interest. As and ligands for novel ligases discovered, chemical effort identify best given is exploding. Therefore, genetic system degradation-causing suitable target/E3 pairs urgently needed. Here, we used well-established dimerization FKBP12 protein FRB domain rapamycin bring WDR5 candidate ligases. Strikingly, this rapamycin-induced assay (RiPA) revealed that VHL, but not Cereblon, able - finding previously made PROTACs, demonstrating its predictive power. By optimizing steric arrangement all components fusing minimal luciferase, RiPA can ideal any interest in living cells, significantly reducing focusing early stages

Language: Английский

Citations

1
Identification of suitable target/E3 ligase pairs for PROTAC development using a rapamycin-induced proximity assay (RiPA) DOI Creative Commons
Bikash Adhikari, Katharina Schneider, Mathias Diebold

et al.

eLife, Journal Year: 2024, Volume and Issue: 13

Published: Dec. 6, 2024

The development of proteolysis targeting chimeras (PROTACs), which induce the degradation target proteins by bringing them into proximity with cellular E3 ubiquitin ligases, has revolutionized drug development. While human genome encodes more than 600 different current PROTACs use only a handful them, drastically limiting their full potential. Furthermore, many PROTAC campaigns fail because selected ligase candidates are unable to particular interest. As and ligands for novel ligases discovered, chemical effort identify best given is exploding. Therefore, genetic system degradation-causing suitable target/E3 pairs urgently needed. Here, we used well-established dimerization FKBP12 protein FRB domain rapamycin bring WDR5 candidate ligases. Strikingly, this rapamycin-induced assay (RiPA) revealed that VHL, but not Cereblon, able - finding previously made PROTACs, demonstrating its predictive power. By optimizing steric arrangement all components fusing minimal luciferase, RiPA can ideal any interest in living cells, significantly reducing focusing early stages

Language: Английский

Citations

1
Rapid PROTAC discovery platform: nanomole scale array synthesis and direct screening of reaction mixtures to facilitate the expedited discovery and follow-up of PROTAC hits. DOI Creative Commons
Mateusz P. Plesniak,

Emilia K. Taylor,

Frederik Eisele

et al.

Published: July 18, 2023

Precise linker length, shape and attachment point are all integral components to designing efficacious PROTACs. Due the increased synthetic complexity of these heterobifunctional degraders difficulty computational modelling aid PROTAC design, exploration structure-activity-relationship (SAR) remains mostly empirical, which requires a significant time resource investment. To facilitate rapid hit finding we developed capabilities for parallel synthesis purification by harnessing an array pre-formed E3-ligand intermediates. In next iteration this approach, rapid, nanomole-scale methodology using amide coupling that enables direct screening non-purified reaction mixtures in cell-based degradation assays, as well logD EPSA measurements. This approach greatly expands accelerates SAR (5 days instead several weeks) while nanomole amounts reagents. Lastly, it avoids laborious solvent-demanding mixtures, thus making economical more sustainable finding.

Language: Английский

Citations

2
A review of volumetric titration as an efficient method for the quantification of ions and compounds in lithium-ion battery components DOI
M. Loghavi,

Mohsen Babaiee,

Rahim Eqra

et al.

Chemical Papers, Journal Year: 2023, Volume and Issue: 77(12), P. 7395 - 7408

Published: Sept. 21, 2023

Language: Английский

Citations

2