A decade update on solvent and catalyst-free neat organic reactions: a step forward towards sustainability

A Sarkar, S Santra, SK Kundu, A Hajra, GV Zyryanov… - Green …, 2016 - pubs.rsc.org
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 …

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 …

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 …

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 …

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 …

Bioactive carbohydrates and peptides in foods: An overview of sources, downstream processing steps and associated bioactivities

M Hayes, BK Tiwari - International journal of molecular sciences, 2015 - mdpi.com
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 …

[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 …

S Bleakley, M Hayes, N O'Shea, E Gallagher, T Lafarga - Foods, 2017 - mdpi.com
The renin-angiotensin-aldosterone system (RAAS) plays an important role in regulating
hypertension by controlling vasoconstriction and intravascular fluid volume. RAAS itself is …

Enzyme tunnels and gates as relevant targets in drug design

SM Marques, L Daniel, T Buryska… - Medicinal Research …, 2017 - Wiley Online Library
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 …

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 …

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 …