scholarly journals New human renin inhibitory peptides. Angiotensinogen transition-state analogues containing novel Leu-Val replacement and a retro-inverso amide bond.

1988 ◽  
Vol 36 (6) ◽  
pp. 2278-2281 ◽  
Author(s):  
Kinji Iizuka ◽  
Tetsuhide Kamijo ◽  
Hiromu Harada ◽  
Kenji Akahane ◽  
Tetsuhiro Kubota ◽  
...  
Keyword(s):  
Transition State ◽  
Amide Bond ◽  
Inhibitory Peptides ◽  
Transition State Analogues ◽  
Human Renin

scholarly journals Synthesis of human renin inhibitory peptides, angiotensinogen transition-state analogs containing a Retro-inverso amide bond.

1990 ◽  
Vol 38 (11) ◽  
pp. 3042-3047 ◽  
Author(s):  
Hiromu HARADA ◽  
Kinji IIZUKA ◽  
Tetsuhide KAMIJO ◽  
Kenji AKAHANE ◽  
Ryoji YAMAMOTO ◽  
...  
Keyword(s):  
Transition State ◽  
Amide Bond ◽  
Inhibitory Peptides ◽  
Transition State Analogs ◽  
Human Renin

scholarly journals Tight Binding of Transition-State Analogues to a Peptidyl-Aminoacyl-L/D-Isomerase from Frog Skin

ChemBioChem ◽  
2011 ◽  
Vol 12 (13) ◽  
pp. 1996-2000 ◽  
Author(s):  
Verena Gehmayr ◽  
Christa Mollay ◽  
Lorenz Reith ◽  
Norbert Müller ◽  
Alexander Jilek
Keyword(s):  
Transition State ◽  
Frog Skin ◽  
Tight Binding ◽  
Transition State Analogues

scholarly journals Polyvalent transition-state analogues of sialyl substrates strongly inhibit bacterial sialidases.

2020 ◽  
Author(s):  
coralie assailly ◽  
clarisse bridot ◽  
amélie saumonneau ◽  
paul lottin ◽  
Benoit Roubinet ◽  
...  
Keyword(s):  
Transition State ◽  
Important Class ◽  
Inhibitory Potency ◽  
Polymeric Scaffolds ◽  
Transition State Analogues

<div>Conjugation of the transitionstate-cation analogue DANA to polymeric scaffolds led to highly potent inhibitors of bacterial sialidases. Each clustered DANA on the polymers saw its inhibitory potency for S. pneumoniae or B. thetaiotaomicron sialidases improved by more than four orders of magnitude. This extends the multivalent concept to this important class of enzymes.</div><div><br></div>

scholarly journals Transition-State Analogues of Phenylethanolamine N-Methyltransferase

2020 ◽  
Vol 142 (33) ◽  
pp. 14222-14233 ◽  
Author(s):  
Niusha Mahmoodi ◽  
Rajesh K. Harijan ◽  
Vern L. Schramm
Keyword(s):  
Transition State ◽  
Transition State Analogues

scholarly journals Crystal Structures ofStaphylococcus aureusKetol-Acid Reductoisomerase in Complex with Two Transition State Analogues that Have Biocidal Activity

2017 ◽  
Vol 23 (72) ◽  
pp. 18289-18295 ◽  
Author(s):  
Khushboo M. Patel ◽  
David Teran ◽  
Shan Zheng ◽  
Ajit Kandale ◽  
Mario Garcia ◽  
...  
Keyword(s):  
Transition State ◽  
Crystal Structures ◽  
Biocidal Activity ◽  
Transition State Analogues

scholarly journals Metallo-β-Lactamase Inhibitors Inspired on Snapshots from the Catalytic Mechanism

Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 854 ◽  
Author(s):  
Antonela R. Palacios ◽  
María-Agustina Rossi ◽  
Graciela S. Mahler ◽  
Alejandro J. Vila
Keyword(s):  
Transition State ◽  
Broad Spectrum ◽  
Catalytic Mechanism ◽  
Structural Diversity ◽  
Resistance Mechanisms ◽  
Amide Bond ◽  
Similar Reaction ◽  
Hydrolysis Process ◽  
Common Strategy ◽  
Low Toxicity

β-Lactam antibiotics are the most widely prescribed antibacterial drugs due to their low toxicity and broad spectrum. Their action is counteracted by different resistance mechanisms developed by bacteria. Among them, the most common strategy is the expression of β-lactamases, enzymes that hydrolyze the amide bond present in all β-lactam compounds. There are several inhibitors against serine-β-lactamases (SBLs). Metallo-β-lactamases (MBLs) are Zn(II)-dependent enzymes able to hydrolyze most β-lactam antibiotics, and no clinically useful inhibitors against them have yet been approved. Despite their large structural diversity, MBLs have a common catalytic mechanism with similar reaction species. Here, we describe a number of MBL inhibitors that mimic different species formed during the hydrolysis process: substrate, transition state, intermediate, or product. Recent advances in the development of boron-based and thiol-based inhibitors are discussed in the light of the mechanism of MBLs. We also discuss the use of chelators as a possible strategy, since Zn(II) ions are essential for substrate binding and catalysis.

scholarly journals Synthesis and structure-activity relationships of human renin inhibitors designed from angiotensinogen transition state.

1990 ◽  
Vol 38 (9) ◽  
pp. 2487-2493 ◽  
Author(s):  
Kinji IIZUKA ◽  
Tetsuhide KAMIJO ◽  
Hiromu HARADA ◽  
Kenji AKAHANE ◽  
Tetsuhiro KUBOTA ◽  
...  
Keyword(s):  
Transition State ◽  
Renin Inhibitors ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Human Renin
Sign in / Sign up

Export Citation Format

Share Document