- 4|Oxo|β|lactams as Covalent Inhibitors of the Mitochondrial ...🔍
- 4‑Oxo|β|lactams as Covalent Inhibitors of the Mitochondrial ...🔍
- Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity🔍
- Peptide‐based covalent inhibitors of protein–protein interactions🔍
- 4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases🔍
- Chemical inhibition of mitochondrial fission via targeting the DRP1 ...🔍
- Design of next|generation covalent inhibitors🔍
- Development of covalent inhibitors🔍
4|Oxo|β|lactams as Covalent Inhibitors of the Mitochondrial ...
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 Covalent Inhibitors of the Mitochondrial ...
4‑Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL.
Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity - NCBI
... β, and ‐γ, respectively) are known. The isoforms show a high ... mitochondrial hexokinase, and Akt3 is co‐localized with the nucleus.3 ...
Peptide‐based covalent inhibitors of protein–protein interactions
Chemical structure of the tested acrylamide modifiers (x = 3 or 4) is provided. (B) Crystal structure of covalent inhibitor BI‐107F7 bound to SIAH C130 (pdb: ...
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases - Lirias
[9,11]. These efforts enabled inhibitor development resulting in the discovery of various covalent electrophilic scaffolds for rhomboid inhibition: 4- chloro- ...
Chemical inhibition of mitochondrial fission via targeting the DRP1 ...
... inhibitors and have developed a covalent compound, mitochondrial division inhibitor (MIDI). ... 4 compounds induced mitochondrial ...
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases
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 ...
Design of next-generation covalent inhibitors: Targeting residues ...
1, 2, 3, 4 Additional to the opportunities of developing selective inhibitors ... In mitochondrial F1-ATPase, a nucleotide-driven motor, both Tyr368 and ...
Development of covalent inhibitors: Principle, design, and ...
5 Covalent dipeptidyl peptidase-4 (DPP-4) inhibitors. DPP-4 is a ... mitochondrial F1-ATPase and found that FSBA predominantly modified ...
Small molecule inhibitors of the mitochondrial ClpXP protease ...
In addition, both Hsp60 and ClpP protein expression were reduced in Jurkat cells (Fig. 4d), suggesting that ClpXP inhibition could promote an ...
Advancements, challenges, and future frontiers in covalent inhibitors ...
... (4) [164], an inhibitor of NF-kB activation. The chemical structures of these ... Ramil Gómez, et al. MO712: involvement of mitochondrial dysfunction in ...
Recent advances in targeting the “undruggable” proteins: from drug ...
Similarly, they successfully developed KRASG12R covalent inhibitors, G12R inhibitor-4 ... mitochondrial proteins (Table 4). Mechanistic ...
Reversible Covalent Inhibition Desired Covalent Adduct Formation ...
... Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. ... mitochondrial, and microsomal GSTs, the latter now ...
Development of covalent inhibitors: Principle, design, and ...
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. ... mitochondrial F1-ATPase by 5′-p-fluorosulfonylbenzoyladenosine.
Covalent inhibition by a natural product-inspired latent electrophile
portin-4 (IPO4), C906 of mitochondrial monofunctional C1-tet- rahydrofolate synthase (MTHFD1L, also known as formyltetra- hydrofolate ...
Inhibition of mitochondrial division through covalent modification of ...
Dive into the research topics of 'Inhibition of mitochondrial division through covalent modification of Drp1 protein by 15 deoxy-Δ12,14-prostaglandin J2'.
Covalent inhibitors of EGFR family protein kinases induce ... - Science
... inhibitor for 4 hours. All whole-cell lysates were generated with ... mitochondrial fragmentation and apoptosis. Cell. Death. Dis. 8 ...
β-Lactone covalent inhibitors of ClpP. - ResearchGate
Given ClpP proteolysis is essential to maintain mitochondrial proteome homeostasis and determine cell fate under cellular stress, targeting mitochondrial ...
Inhibiting androgen receptor splice variants with cysteine-selective ...
Inhibiting androgen receptor splice variants with cysteine-selective irreversible covalent inhibitors to treat prostate cancer ... 4 °C and then with UT-143 ...
Recent Advances in Selective and Irreversible Covalent Ligand ...
mine (acetylcholinesterase inhibitor), and saxagliptin (dipeptidyl peptidase-4 inhibitor). ... covalent inhibitors. This strategy was ...