Results 151 to 160 of about 37,292 (264)
3D-QSAR and pharmacophore model study on aryl diphenolic azoles as estrogen receptor-b ligands
3D-QSAR and pharmacophore model study on aryl diphenolic azoles as estrogen receptor-b ...
Jun-Zhi Wang +4 more
core
Unusual backfolded binding poses of BAZ2A bromodomain binders
We identified BAZ2A‐binding compounds assuming a peculiar, almost enclosed, conformation. These molecules pose a basis for the development of potent BAZ2A macrocyclic inhibitors, as performed for other bromodomains.BAZ2A is a large multidomain protein overexpressed in aggressive prostate cancer, where it potentiates migration and invasion of other ...
Andrea Dalle Vedove +5 more
wiley +1 more source
The selective nature through which coumarin compounds produced by different species of plants target PQS signalling in Pseudomonas aeruginosa and select for distinct phenotypic responses in key pathogenic organisms adds to the growing evidence of their utility as natural virulence suppressors. ABSTRACT Cell‐to‐cell communication in microbial systems is
Dylan Boon +8 more
wiley +1 more source
Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists
Psychedelic drugs such as LSD and psilocin were once relegated to the fringes of medical research because of their association with counterculture movements and a perceived concern about harm through recreational use, and their consequent legal prohibition in the early 1970s.
Trevor Sharp, Aurelija Ippolito
wiley +1 more source
Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?
Psychedelic drugs that activate 5‐HT2A receptors have been long used for cultural, medicinal and recreational purposes. Interest in psychedelics for treating psychiatric disorders has resurged recently and is well documented; less well recognised are their anti‐inflammatory properties. Growing evidence now demonstrates that psychedelics modulate immune
Omar Qureshi +10 more
wiley +1 more source
3D pharmacophore models describe the ligand’s chemical interactions in their bioactive conformation. They offer a simple but sophisticated approach to decipher the chemically encoded ligand information, making them a valuable tool in Drug Design.
Ngoc-Vi Nguyen, Tran +7 more
core +1 more source
Defining AV2‐1 as a novel pharmacological probe to target human and rodent TRPV2
Abstract Background and Purpose Transient receptor potential vanilloid 2 (TRPV2) is a non‐selective cation channel implicated in immune cell functions. However, progress in understanding TRPV2 has been limited by a lack of potent and selective pharmacological tools, particularly those targeting the human variant. We aimed to identify and characterise a
Andrea Leipe +6 more
wiley +1 more source
DNA gyrase B is one of the enzyme targets for antimicrobial drug development, and its absence in mammals makes it a suitable target for the creation of safe antibacterial drugs. We identified six novel hits as DNA gyrase B inhibitors in the present study
Samia A. Elseginy (11595739) +1 more
core +1 more source
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren +8 more
wiley +1 more source
Dearomative homocoupling of quinolines into 1,1',2,2',3,3',4,4'‐octahydro‐4,4'‐biquinoline (OHBQ) is reported. The photoexcited boron complex, in situ generated from quinoline, HB(pin), and KOtBu, enables the unprecedented homocoupling of tetrahydroquinolines that is challenging in the ground state, expanding the chemical diversity of OHBQ derivatives.
Mone Suzuki +2 more
wiley +1 more source

