A decade update on solvent and catalyst-free neat organic reactions: a step forward towards sustainability
Particular success has been achieved in the synthesis of new products and in processes
since the twelve principles of “green chemistry” were formulated in the 1990s. These …
since the twelve principles of “green chemistry” were formulated in the 1990s. These …
Development of covalent inhibitors: Principle, design, and application in cancer
L Zheng, Y Li, D Wu, H **ao, S Zheng… - MedComm …, 2023 - Wiley Online Library
Covalent inhibitors have been a rapidly growing field in drug discovery due to their
therapeutic potential and unique advantages in cancer therapy. As opposed to noncovalent …
therapeutic potential and unique advantages in cancer therapy. As opposed to noncovalent …
Ang II (angiotensin II) conversion to angiotensin-(1-7) in the circulation is POP (prolyloligopeptidase)-dependent and ACE2 (angiotensin-converting enzyme 2) …
P Serfozo, J Wysocki, G Gulua, A Schulze, M Ye… - …, 2020 - ahajournals.org
The Ang II (Angiotensin II)-Angiotensin-(1-7) axis of the Renin Angiotensin System
encompasses 3 enzymes that form Angiotensin-(1-7)[Ang-(1-7)] directly from Ang II: ACE2 …
encompasses 3 enzymes that form Angiotensin-(1-7)[Ang-(1-7)] directly from Ang II: ACE2 …
Translational imaging of the fibroblast activation protein (FAP) using the new ligand [68Ga]Ga-OncoFAP-DOTAGA
P Backhaus, F Gierse, MC Burg, F Büther… - European Journal of …, 2022 - Springer
Purpose The fibroblast activation protein (FAP) is an emerging target for molecular imaging
and therapy in cancer. OncoFAP is a novel small organic ligand for FAP with very high …
and therapy in cancer. OncoFAP is a novel small organic ligand for FAP with very high …
Fibroblast activation protein-α: a key modulator of the microenvironment in multiple pathologies
T Kelly, Y Huang, AE Simms, A Mazur - … review of cell and molecular biology, 2012 - Elsevier
Fibroblast activation protein-α (FAP) is a serine protease that can provide target specificity to
therapeutic agents because in adults its expression is restricted to pathologic sites, including …
therapeutic agents because in adults its expression is restricted to pathologic sites, including …
Bioactive carbohydrates and peptides in foods: An overview of sources, downstream processing steps and associated bioactivities
Bioactive peptides and carbohydrates are sourced from a myriad of plant, animal and
insects and have huge potential for use as food ingredients and pharmaceuticals. However …
insects and have huge potential for use as food ingredients and pharmaceuticals. However …
[HTML][HTML] Predicted Release and Analysis of Novel ACE-I, Renin, and DPP-IV Inhibitory Peptides from Common Oat (Avena sativa) Protein Hydrolysates Using in Silico …
The renin-angiotensin-aldosterone system (RAAS) plays an important role in regulating
hypertension by controlling vasoconstriction and intravascular fluid volume. RAAS itself is …
hypertension by controlling vasoconstriction and intravascular fluid volume. RAAS itself is …
Enzyme tunnels and gates as relevant targets in drug design
Many enzymes contain tunnels and gates that are essential to their function. Gates
reversibly switch between open and closed conformations and thereby control the traffic of …
reversibly switch between open and closed conformations and thereby control the traffic of …
Rapid measurement of inhibitor binding kinetics by isothermal titration calorimetry
JM Di Trani, S De Cesco, R O'Leary, J Plescia… - Nature …, 2018 - nature.com
Although drug development typically focuses on binding thermodynamics, recent studies
suggest that kinetic properties can strongly impact a drug candidate's efficacy. Robust …
suggest that kinetic properties can strongly impact a drug candidate's efficacy. Robust …
5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein–Protein Interaction-Derived Functions
HT Patsi, TP Kilpelainen, M Jumppanen… - Journal of Medicinal …, 2024 - ACS Publications
A series of novel 5-aminothiazole-based ligands for prolyl oligopeptidase (PREP) comprise
selective, potent modulators of the protein–protein interaction (PPI)-mediated functions of …
selective, potent modulators of the protein–protein interaction (PPI)-mediated functions of …