Factor XIa inhibitors in anticoagulation therapy: recent advances and perspectives

Z Xie, Z Meng, X Yang, Y Duan, Q Wang… - Journal of medicinal …, 2023 - ACS Publications
Factor XIa (FXIa) in the intrinsic pathway of the coagulation process has been proven to be
an effective and safe target for anticoagulant discovery with limited or no bleeding …

Recent advances in the discovery and development of factor XI/XIa inhibitors

RA Al‐Horani, DK Afosah - Medicinal research reviews, 2018 - Wiley Online Library
Abstract Factor XIa (FXIa) is a serine protease homodimer that belongs to the intrinsic
coagulation pathway. FXIa primarily catalyzes factor IX activation to factor IXa, which …

Vorasidenib (AG-881): a first-in-class, brain-penetrant dual inhibitor of mutant IDH1 and 2 for treatment of glioma

Z Konteatis, E Artin, B Nicolay, K Straley… - ACS Medicinal …, 2020 - ACS Publications
Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes
prevent the accumulation of the oncometabolite d-2-hydroxyglutarate (2-HG) and are under …

Biomolecular interactions of ultrasmall metallic nanoparticles and nanoclusters

AA Sousa, P Schuck, SA Hassan - Nanoscale Advances, 2021 - pubs.rsc.org
The use of nanoparticles (NPs) in biomedicine has made a gradual transition from proof-of-
concept to clinical applications, with several NP types meeting regulatory approval or …

Explicit treatment of non‐Michaelis‐Menten and atypical kinetics in early drug discovery

B Srinivasan - ChemMedChem, 2021 - Wiley Online Library
Biological systems are highly regulated. They are also highly resistant to sudden
perturbations enabling them to maintain the dynamic equilibrium essential to sustain life …

Regulation of peptidase activity beyond the active site in human health and disease

A Obaha, M Novinec - International journal of molecular sciences, 2023 - mdpi.com
This comprehensive review addresses the intricate and multifaceted regulation of peptidase
activity in human health and disease, providing a comprehensive investigation that extends …

Allosteric inhibition of α-thrombin enzymatic activity with ultrasmall gold nanoparticles

AL Lira, RS Ferreira, RJS Torquato, MLV Oliva… - Nanoscale …, 2019 - pubs.rsc.org
The catalytic activity of enzymes can be regulated by interactions with synthetic
nanoparticles (NPs) in a number of ways. To date, however, the potential use of NPs as …

Synthesis and study of new 2H-pyranoquinolin-2-one-based inhibitors of blood coagulation factors Xa and XIa

AY Potapov, BV Paponov, NA Podoplelova… - Russian Chemical …, 2021 - Springer
Abstract Condensation of 7-hydroxy-1, 2, 2, 4-tetramethylhydroquinoline-6-carbaldehydes
with various hetaryl-substituted 3-oxo esters afforded a series of hybrid hydro-6, 8, 8, 9 …

[HTML][HTML] A synthetic heparin mimetic that allosterically inhibits factor XIa and reduces thrombosis in vivo without enhanced risk of bleeding

RA Al‐Horani, EI Abdelfadiel, DK Afosah… - Journal of Thrombosis …, 2019 - Elsevier
Abstract Background Human factor XIa (FXIa) is an actively pursued target for development
of safer anticoagulants. Our long‐standing hypothesis has been that allosterism originating …

Thermodynamics, kinetics and mechanisms of noncompetitive allosteric inhibition of chymotrypsin by dihydrolipoic acid-coated gold nanoclusters

WQ Chen, MM Yin, PJ Song, XH He, Y Liu, FL Jiang - Langmuir, 2020 - ACS Publications
Enzymes are an important class of biomacromolecules which catalyze many metabolic
processes in living systems. Nanomaterials can be synthesized with tailored sizes as well as …