Results 81 to 90 of about 25,555 (231)

Disarming the Hsp70–Bim Alliance: Small‐Molecule and Peptidic Disruptors of a Chaperone‐Apoptotic Switch in Cancer

open access: yesChemistryOpen, EarlyView.
Targeting a nucleotide‐sensitive groove on Hsp70 that binds the Bim BH3 helix, we integrate structures, biophysics, and SAR from peptides, fragments, and phenalene‐dicarbonitrile “wedges.” These disrupt the Hsp70–Bim complex with sub‐µM cellular engagement and in vivo activity while sparing Hsp90/mortalin.
Emadeldin M. Kamel   +5 more
wiley   +1 more source

Computational Evaluation of Statin Analogs Targeting HMG‐CoA Reductase for Coronary Artery Disease Treatment

open access: yesChemistryOpen, EarlyView.
Molecular dynamics analysis of novel statin analogs shows that binding induces superior stabilization of HMG‐CoA reductase. As shown by the solvent‐accessible surface area profile, ligand‐induced rigidity offers a new, effective strategy for drug design. Cardiovascular diseases remain a leading cause of global mortality.
Yoshua B. Mtulo   +4 more
wiley   +1 more source

Peptidic product derived from trypsin autolysis modulates insect digestive proteases and supports plant biochemical defense

open access: yesPest Management Science, EarlyView.
XXXX Abstract BACKGROUND Spodoptera frugiperda, commonly known as the fall armyworm, is a highly economically significant pest that affects various crops, resulting in substantial losses in productivity. Managing this pest primarily relies on chemical insecticides; however, the repeated development of resistance to these chemicals has rendered them ...
Daniel Guimarães Silva Paulo   +9 more
wiley   +1 more source

The continuing significance of chiral agrochemicals

open access: yesPest Management Science, Volume 81, Issue 4, Page 1697-1716, April 2025.
In the time frame 2018–2023, around 43% of the 35 chiral agrochemicals introduced to the market (herbicides, fungicides, insecticides, acaricides, and nematicides) contain one or more stereogenic centers in the molecule, and almost 69% of them have been marketed as racemic mixtures of enantiomers or stereoisomers.
Peter Jeschke
wiley   +1 more source

Amentoflavone, a Preferentially TGF‐β Receptor 1 Inhibitor, Alleviates Cardiac Remodeling and Dysfunction Through Modulating the TGF‐β/Smad and MAPK Signaling Pathways

open access: yesPhytotherapy Research, EarlyView.
Amentoflavone, a preferentially TGF‐ββ receptor 1 inhibitor, attenuates transverse aortic constriction (TAC)‐triggered cardiac hypertrophy, fibrosis, and dysfunction by suppressing downstream Smad and MAPK signaling cascades in cardiomyocytes and cardiac fibroblasts.
Jiangjiao Wu   +10 more
wiley   +1 more source

Reversible Small Molecule Inhibitors of MAO A and MAO B with Anilide Motifs

open access: yesDrug Design, Development and Therapy, 2020
Jens Hagenow,1 Stefanie Hagenow,1 Kathrin Grau,1 Mohammad Khanfar,1– 3 Lena Hefke,4 Ewgenij Proschak,4 Holger Stark1 1Heinrich Heine University Düsseldorf, Institute of Pharmaceutical and Medicinal Chemistry, Duesseldorf 40225, Germany ...
Hagenow J   +6 more
doaj  

Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists

open access: yesBritish Journal of Pharmacology, EarlyView.
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

How to Identify a Pharmacophore

open access: yesChemistry & Biology, 2008
The inhibition of chitinases by argifin and progressively dissected analogs had been studied by a combination of kinetic and crystallographic methods (Andersen et al., 2008). This work also leads to a general understanding of structure-activity relationships for inhibitors with one distinct pharmacophor.
openaire   +3 more sources

Are we hallucinating or can psychedelic drugs modulate the immune system to control inflammation?

open access: yesBritish Journal of Pharmacology, EarlyView.
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

In Silico Analysis for Exploring the Potential Inhibitors Against Breast Cancer (MCF7) Using Curcumin Analogue Compounds

open access: yesJurnal Kimia Sains dan Aplikasi
Breast cancer is one of the most problematic diseases in the world. Currently, there are no potential vaccines for the treatment of this disease. Therefore, finding effective compounds, such as curcumin analogs, is crucial to inhibit breast cancer. Forty-
Neni Frimayanti, Adel Zamri, Yum Eryanti
doaj   +1 more source

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