- 4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases🔍
- 4|Oxo|β|Lactams as Novel Inhibitors for Rhomboid Proteases🔍
- 4|Oxo|β|lactams as Covalent Inhibitors of the Mitochondrial ...🔍
- 4‐Oxo‐β‐Lactams as Inhibitors for Rhomboid Proteases🔍
- Inhibition profile of 4|Oxo|β|Lactams.🔍
- 4‑Oxo|β|lactams as Covalent Inhibitors of the Mitochondrial ...🔍
- Benzoxazin|4|ones as novel🔍
- Monocyclic β|Lactams Are Selective🔍
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases - 2023
We report 4-oxo-β-lactams as a novel scaffold for inhibition of rhomboids. We show that they covalently react with the active site and that the covalent bond ...
4-Oxo-β-Lactams as Novel Inhibitors for Rhomboid Proteases
Intramembrane serine proteases (rhomboid proteases) are involved in a variety of biological processes and are implicated in several diseases ...
4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial ...
Rhomboid proteases play a variety of physiological roles, but rhomboid protease inhibitors have been mostly developed for the E. coli model ...
4‐Oxo‐β‐Lactams as Inhibitors for Rhomboid Proteases
The team discovered 4-oxo-β-lactams (example pictured) that can serve as rhomboid protease inhibitors.
4-Oxo-β-Lactams as Novel Inhibitors for Rhomboid Proteases - Lirias
Here, we report 4-oxo-β-lactams as a novel scaffold for inhibition of rhomboids. We show that they covalently react with the active site and ...
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases
Request PDF | 4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases | Intramembrane serine proteases (rhomboid proteases) are involved ...
Inhibition profile of 4-Oxo-β-Lactams. - ResearchGate
Here, we report 4‐oxo‐β‐lactams as a novel scaffold for inhibition of rhomboids. We show that they covalently react with the active site and that the covalent ...
4‑Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial ...
Rhomboid proteases play a variety of physiological roles, but rhomboid protease inhibitors have been mostly developed for the E. coli model ...
Benzoxazin-4-ones as novel, easily accessible inhibitors for ...
We demonstrate that an alkoxy substituent at the 2-position is crucial for potency and results in low micromolar inhibitors of rhomboid proteases. Hence, we ...
Monocyclic β-Lactams Are Selective, Mechanism-Based Inhibitors of ...
Although rhomboids are weakly inhibited by some broad-spectrum serine protease inhibitors, no potent and specific inhibitors have been ...
Chemoproteomics-Enabled Identification of 4-Oxo-β-Lactams as ...
Chemoproteomics-Enabled Identification of 4-Oxo-β-Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9 · Abstract · Publication types · MeSH ...
Activity-based probes for rhomboid proteases discovered in a mass ...
We have identified isocoumarin inhibitors and developed activity-based probes for rhomboid proteases. The probes can distinguish between active and inactive ...
Covalent activity-based probes for imaging of serine proteases
... oxo-lactams as in rhomboid GlpG-targeting probe 13 [58] ... S.H.L.. (. 2023. ) 4-Oxo-β-lactams as novel inhibitors for rhomboid proteases.
Design, synthesis and biological evaluation of rhomboid protease ...
N-aryl sulfonyl substituted β-lactam (4) was the most potent inhibitor with an ... beta-lactams are selective, mechanism-based inhibitors of rhomboid ...
Covalent activity-based probes for imaging of serine proteases - OUCI
4-Oxo-β-lactams as novel inhibitors for rhomboid proteases, ChemBioChem, № 24, с. e202300418 https://doi.org/10.1002/cbic.202300418; In vitro and in situ ...
... inhibitor pre-incubation. Figure 5. Serine protease ABPs with different reactive electrophiles, including oxo-lactams as in rhomboid GlpG-targeting probe 13 ...
Universidade de Lisboa Faculdade de Farmácia 3-Oxo-β-Sultams ...
The 4-Oxo-β-Lactam is a novel chemotype for DPP8 and DPP9 ... We intend on continuing the study of 4-Oxo-β-Lactams as inhibitors of the DPP enzymes,.
Novel Mechanism of Inhibition of Elastase by β-Lactams Is Defined ...
Novel Mechanism of Inhibition of Elastase by β-Lactams Is Defined by Two Inhibitor Crystal Complexes ... Автори: Paul Taylor; Violet Anderson; Malcolm D.
Rhomboid proteases in human disease
In the case of β-lactams, the inhibitor is slowly turned over by the protease, probably explaining why β-lactams are unable to inhibit rhomboid proteases fully ...
2023 - Table of Contents page: Journal of Biological Chemistry
Abstract 1223: High-throughput Virtual Screening of Potential Novel Inhibitors for DXP Reductoisomerase in Helicobacter pylori ... β-lactams. Duhyun Ko ...