Results 21 to 30 of about 9,317 (205)

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

Highly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Cathepsin K (CatK) is a target for the treatment of osteoporosis, arthritis, and bone metastasis. Peptidomimetics with a cyanohydrazide warhead represent a new class of highly potent CatK inhibitors; however, their binding mechanism is unknown.
Jakub Benýšek, Michal Buša, Petra Rubešová, Jindřich Fanfrlík, Martin Lepšík, Jiří Brynda, Zuzana Matoušková, Ulrike Bartz, Martin Horn, Michael Gütschow, Michael Mareš   +10 more
doaj   +1 more source

Investigation of monoclonal antibody CSX-1004 for fentanyl overdose

Nature Communications, 2023
The opioid crisis in the United States is primarily driven by the highly potent synthetic opioid fentanyl leading to >70,000 overdose deaths annually; thus, new therapies for fentanyl overdose are urgently needed. Here, we present the first clinic-ready,
Paul T. Bremer, Emily L. Burke, Andrew C. Barrett, Rajeev I. Desai   +3 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

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

Cystic fibrosis drug ivacaftor stimulates CFTR channels at picomolar concentrations

eLife, 2019
The devastating inherited disease cystic fibrosis (CF) is caused by mutations of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) anion channel.
László Csanády, Beáta Töröcsik
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

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

Of Seven New K⁺ Channel Inhibitor Peptides of Centruroides bonito, α-KTx 2.24 Has a Picomolar Affinity for Kv1.2

Toxins, 2023
Seven new peptides denominated CboK1 to CboK7 were isolated from the venom of the Mexican scorpion Centruroides bonito and their primary structures were determined.
Kashmala Shakeel, Timoteo Olamendi-Portugal, Muhammad Umair Naseem, Baltazar Becerril, Fernando Z. Zamudio, Gustavo Delgado-Prudencio, Lourival Domingos Possani, Gyorgy Panyi   +7 more
doaj   +1 more source