Results 51 to 60 of about 19,491 (256)

Cholestenoic acid, an endogenous cholesterol metabolite, is a potent γ-secretase modulator. [PDF]

open access: yes, 2015
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

Telomere‐to‐Telomere Genomes Reveal that Multiscale Evolution Shapes the Largest Metabolic Arsenal of Diaporthe Fungi

open access: yesAdvanced Science, EarlyView.
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]

open access: yes, 2017
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

Metabologenomic Hallmark‐Based Discovery of Bacterial Thioamides as a New Lead against Drug‐Resistant Pancreatic Cancer

open access: yesAdvanced Science, EarlyView.
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]

open access: yesBioorganic & Medicinal Chemistry Letters, 2020
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

open access: yesNatural Product Communications, 2008
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]

open access: yes, 2008
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

open access: yesAdvanced Science, EarlyView.
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]

open access: yes, 1983
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

Modular Rh‐Catalyzed Synthesis and Biological Profiling of Diverse Pentafluorobenzenesulfonamide Reactive Fragments

open access: yesChemistry – A European Journal, EarlyView.
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

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