Results 131 to 140 of about 37,689 (286)

Unusual backfolded binding poses of BAZ2A bromodomain binders

Acta Crystallographica Section D, EarlyView.
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, Giulia Cazzanelli, Vito Giuseppe D'Agostino, Pablo Andres Vargas Rosales, Amedeo Caflisch, Graziano Lolli   +5 more
wiley   +1 more source

Systemic medications associate with surgically treated cataract among adults over 50 years in Finland

Acta Ophthalmologica, EarlyView.
Abstract Purpose To identify associations between systemic drugs and cataract surgery in Finland. Methods A historic cohort study based on administrative data. Endpoint event was cataract surgery. Use of drugs in question was based on redeemed prescriptions and consisted of 156 drugs.
Antti Riikonen, Jari Haukka, Tuomas Lilius, Sirpa Loukovaara   +3 more
wiley   +1 more source

Scalable Synthesis of Piperazines Enabled by Visible‐Light Irradiation and Aluminum Organometallics

, 2015
The development of more active C-H oxidation catalysts has inspired a rapid, scalable, and stereoselective assembly of multifunctional piperazines through a [3+3] coupling of azomethine ylides.
Colas, Kilian,, Samuel Suárez‐Pantiga, Suárez-Pantiga, Samuel,, Johansson, Magnus J., Magnus J. Johansson, Abraham Mendoza, Kilian Colas, Mendoza, Abraham,   +7 more
core   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

The R203W substitution drives PACS‐1 syndrome by disrupting intramolecular regulation

The FEBS Journal, EarlyView.
The middle region (MR) of PACS‐1 controls engagement with specific partner proteins. This manuscript presents the structure of the Furin binding region (FBR) and how interactions with partners are regulated through the interplay between a basic patch in the FBR and an acidic cluster in the MR.
Troy C. Krzysiak, In‐Ja L. Byeon, Ryan Ponticelli, Mary E. Lucas, Lariah Thompson, Christopher DeHaven, Gary Thomas, Angela M. Gronenborn   +7 more
wiley   +1 more source

Probing skin photoallergens in reconstructed human epidermis: An EPR spin trapping investigation

Photochemistry and Photobiology, Volume 101, Issue 2, Page 275-281, March/April 2025.
We present an original proof‐of‐concept methodology to probe radical generation from allergens in contact with photoexposed skin, using electron paramagnetic resonance and spin trapping in a reconstructed human epidermis model mimicking real‐life exposure scenarios.
Yannick Port‐Lougarre, Guillaume Voegeli, Bertrand Vileno, Elena Giménez‐Arnau   +3 more
wiley   +1 more source

Advances in organic UV filters for sunscreens over the past decade

Photochemistry and Photobiology, EarlyView.
Highlighted organic UV filter frameworks that have been described for sunscreens over the past decade divided into three groups: derivatives of or inspired by approved organic UV filters, natural product‐based compounds, and miscellaneous. Abstract Ultraviolet (UV) radiation is a major environmental factor in photoaging, erythema, and skin cancer ...
Gabriela Zanella Marcon, Maria Carolina Theisen, Andressa Motta Castro, Giovana Jones Radke, Fernando Fumagalli   +4 more
wiley   +1 more source

Synthesis, Dynamic NMR Characterization, and XRD Study of 2,4-Difluorobenzoyl-Substituted Piperazines

Chemistry
Five different 2,4-difluorobenzamide derivatives were synthesized and fully characterized by 1H/13C/19F/2D NMR spectroscopy using DMSO-d6 as solvent and MS.
Martin Köckerling, Constantin Mamat
doaj   +1 more source

Sprint‐interval training with post‐exercise blood flow restriction increases mitochondrial content and respiration

The Journal of Physiology, EarlyView.
Abstract figure legend The mechanisms underpinning improved maximal oxygen uptake following sprint interval training (SIT) with post‐exercise blood flow restriction (BFR), compared to SIT alone, remain unclear. This study examined the effects of 6 week SIT with (BFR; n = 12) or without (CON; n = 8) post‐exercise BFR on V̇O2peak${{\dot{V}}_{{{{\mathrm{O}
Donald L. Peden, Carolin Stangier, Emma A. Mitchell, Stephen J. Bailey, Richard A. Ferguson   +4 more
wiley   +1 more source

Synthesis of Some New 1-[2-(alkylthio-1-benzyl-5-imidazolyl) carbonyl]-4-[3-(isopropylamino)-2-pyridyl] piperazines as Anti-HIV [PDF]

Journal of Sciences, Islamic Republic of Iran, 2004
A few analogues of atevirdine or 1-[(5-methoxyindol-2-yl) carbonyl]-4-[3- (ethylamino)-2-pyridyl] piperazine – an anti-HIV belonging to non-nucleoside reverse transcriptase inhibitors were synthesized and evaluated for anti-HIV activity.
doaj