Results 41 to 50 of about 212,806 (232)

Novel Cell type-specific aptamer-siRNA delivery system for HIV-1 therapy [PDF]

, 2007
The successful use of small interfering RNAs (siRNAs) for therapeutic purposes requires safe and efficient delivery to specific cells and tissues. Here we demonstrate cell type-specific delivery of anti-HIV siRNAs via fusion to an anti-gp120 aptamer. The
Haitang Li, Jiehua Zhou, John Rossi, John Zaia, Shirley Li   +4 more
core   +2 more sources

Deactivatable Bisubstrate Inhibitors of Protein Kinases

Molecules, 2022
Bivalent ligands, including bisubstrate inhibitors, are conjugates of pharmacophores, which simultaneously target two binding sites of the biomolecule. Such structures offer attainable means for the development of compounds whose ability to bind to the ...
Tanel Sõrmus, Darja Lavogina, Erki Enkvist, Asko Uri, Kaido Viht   +4 more
doaj   +1 more source

In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]

, 2018
Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta, Negri, Lucia, Rief, Silvia, Schmidhammer, Helmut, Spetea, Mariana.   +4 more
core   +2 more sources

Design and 22-step synthesis of highly potent D-ring modified and linker-equipped analogs of spongistatin 1

Nature Communications, 2018
Step-economical and efficient syntheses of Spongistatin 1 analogs are desirable for the development of potent anti-proliferative agents. Here, the authors report a 22-step synthesis of a D-ring modified Spongistatin 1 analog with retained picomolar ...
Linda M. Suen, Makeda A. Tekle-Smith, Kevin S. Williamson, Joshua R. Infantine, Samuel K. Reznik, Paul S. Tanis, Tyler D. Casselman, Dan L. Sackett, James L. Leighton   +8 more
doaj   +1 more source

Conformation specific antagonistic high affinity antibodies to the RON receptor kinase for imaging and therapy

Scientific Reports, 2022
The RON receptor tyrosine kinase is an exceptionally interesting target in oncology and immunology. It is not only overexpressed in a wide variety of tumors but also has been shown to be expressed on myeloid cells associated with tumor infiltration ...
Xin Yu Koh, Xiao Hui Koh, Diana Spiegelberg, Preeti Jha, Marika Nestor, Le-ann Hwang, Ban Xiong Tan, David Philip Lane   +7 more
doaj   +1 more source

A 1-acetamido derivative of 6-epi-valienamine: an inhibitor of a diverse group of β-N-acetylglucosaminidases [PDF]

, 2007
The synthesis of an analogue of 6-epi-valienamine bearing an acetamido group and its characterisation as an inhibitor of β-N-acetylglucosaminidases are described.
Adrian Scaffidi, Backvall, Bailey, Beer, Chen, Chretien, David J. Vocadlo, Davies, Davies, Dennis, Dong, Dorfmueller, Edward J. Taylor, Emsley, Esnouf, Fairweather, Gideon J. Davies, Horsch, Junge, Kappes, Keith A. Stubbs, Knapp, Kraulis, Legler, Lin, Liu, Liu, Macauley, Mark, Money, Murshudov, Namiki, Nicotra, Ogawa, Rana, Rao, Rebecca J. Dennis, Robert V. Stick, Salleh, Scaffidi, Shanmugasundaram, Shitara, Sigurskjold, Stubbs, Stubbs, Svensson, Tanaka, Terinek, Tews, Vocadlo   +49 more
core   +1 more source

Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting beta-amyloid, tau, and cholinesterase pathologies [PDF]

, 2014
Optimization of an essentially inactive 3,4-dihydro-2H-pyrano[3,2-c]quinoline carboxylic ester derivative as acetylcholinesterase (AChE) peripheral anionic site (PAS)-binding motif by double O → NH bioisosteric replacement, combined with molecular ...
Clos, Victòria, Di Pietro, O., Espargaró Colomé, Alba, Juárez-Jiménez, Jordi, Lavilla Grífols, Rodolfo, Luque Garriga, F. Xavier, Muñoz-Torrero López-Ibarra, Diego, Pérez Areales, Francisco Javier, Pérez Fernández, Belén, Sabaté Lagunas, Raimon   +9 more
core   +2 more sources

Fluorine and chlorine substituted adamantyl-urea as molecular tools for inhibition of human soluble epoxide hydrolase with picomolar efficacy

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Series of 1,3-disubstituted ureas and diadamantyl disubstituted diureas with fluorinated and chlorinated adamantane residues were shown to inhibit human soluble epoxide hydrolase (sEH) with inhibition potency ranging from 40 pM to 9.2 nM.
V. Burmistrov, C. Morisseau, Dmitry V. Danilov, B. Gladkikh, V. D'yachenko, N. Zefirov, O. Zefirova, G. Butov, Bruce D. Hammock   +8 more
semanticscholar   +1 more source

Potent and Selective BACE-1 Peptide Inhibitors Lower Brain Aβ Levels Mediated by Brain Shuttle Transport

EBioMedicine, 2017
Therapeutic approaches to fight Alzheimer's disease include anti-Amyloidβ (Aβ) antibodies and secretase inhibitors. However, the blood-brain barrier (BBB) limits the brain exposure of biologics and the chemical space for small molecules to be BBB ...
Nadine Ruderisch, Daniel Schlatter, Andreas Kuglstatter, Wolfgang Guba, Sylwia Huber, Carlo Cusulin, Jörg Benz, Arne Christian Rufer, Joerg Hoernschemeyer, Christophe Schweitzer, Tina Bülau, Achim Gärtner, Eike Hoffmann, Jens Niewoehner, Christoph Patsch, Karlheinz Baumann, Hansruedi Loetscher, Eric Kitas, Per-Ola Freskgård   +18 more
doaj   +1 more source

Ribosome-Inactivating Proteins: From Plant Defense to Tumor Attack

Toxins, 2010
Ribosome-inactivating proteins (RIPs) are EC3.2.32.22 N-glycosidases that recognize a universally conserved stem-loop structure in 23S/25S/28S rRNA, depurinating a single adenine (A4324 in rat) and irreversibly blocking protein translation, leading ...
Maria Serena Fabbrini, Alessio Lombardi, Rocco Caliandro, Maddalena de Virgilio   +3 more
doaj   +1 more source