Cholestenoic acid, an endogenous cholesterol metabolite, is a potent γ-secretase modulator. [PDF]
BackgroundAmyloid-β (Aβ) 42 has been implicated as the initiating molecule in the pathogenesis of Alzheimer's disease (AD); thus, therapeutic strategies that target Aβ42 are of great interest.
Akula, Rajender +14 more
core +3 more sources
This study presents the first telomere‐to‐telomere genomes and population resources for Diaporthe pathogens, uncovering the largest known fungal repertoire of secondary metabolite gene clusters. Structural variations and horizontal gene transfer drive cluster diversification, while specific rapidly evolving clusters control virulence, offering novel ...
Kainan Li +9 more
wiley +1 more source
A temporal comparison of sex-aggregation pheromone gland content and dynamics of release in three members of the Lutzomyia longipalpis (Diptera: Psychodidae) species complex [PDF]
Background: Lutzomyia longipalpis is the South American vector of Leishmania infantum, the etiologic agent of visceral leishmaniasis (VL). Male L. longipalpis produce a sex-aggregation pheromone that is critical in mating, yet very little is known about
Angel Guerrero +8 more
core +2 more sources
A targeted metabologenomic strategy integrating genomic and metabolomic hallmarks enabled the discovery of two new thioamides, thiogochangamides A and B, from bacteria. Their absolute configurations, previously unresolved within the thioviridamide family, were fully assigned through various chemical derivatizations and computational analysis ...
Young Eun Du +18 more
wiley +1 more source
A new chemotype with promise against Trypanosoma cruzi [PDF]
Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity ...
Wang, X. +8 more
openaire +3 more sources
Composition and Antioxidant Activity of Essential Oils of H.B.K. grown in Colombia
Microwave-assisted hydrodistillation, simultaneous distillation-solvent extraction, and supercritical fluid extraction, were used to isolate secondary metabolites from two Lippia origanoides chemotypes growing wild in Colombia.
Elena Stashenko +4 more
doaj +1 more source
Barbarea vulgaris Glucosinolate Phenotypes Differentially Affect Performance and Preference of Two Different Species of Lepidopteran Herbivores [PDF]
Contains fulltext : 90894.pdf (publisher's version ) (Closed ...
Hanneke van Leur +62 more
core +2 more sources
ESCRT‐Mimetic Nanodegrader Targets STING for Anti‐Inflammatory Therapy
A nanoplatform‐enabled targeted protein degradation strategy is presented to regulate aberrant STING signaling. STING‐ATTEC induces selective autophagic degradation of STING via formation of a STING–ATTEC–LC3 ternary complex, while the cationic FA‐LNP+ system enhances LC3 generation and targeted delivery. Together, this synergistic approach efficiently
Fuyuan Zhou +9 more
wiley +1 more source
1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M. +11 more
core +3 more sources
A modular Rh‐catalyzed synthetic approach enabled the preparation of diverse reactive fragments from available substrates. The reactive fragments modified Aurora A kinase via several distinct modification reaction classes. In a complex biological environment, the constellation of modified proteins depended critically on the reactive fragment structure.
Julian Chesti +8 more
wiley +1 more source

