Results 1 to 10 of about 212,806 (232)

Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel. [PDF]

Sci Adv, 2020
We identified a small molecule that, at picomolar concentrations, rescues mutant CFTR chloride channel from protein degradation. F508del, the most frequent mutation causing cystic fibrosis (CF), results in mistrafficking and premature degradation of the ...
Pedemonte N, Bertozzi F, Caci E, Sorana F, Di Fruscia P, Tomati V, Ferrera L, Rodríguez-Gimeno A, Berti F, Pesce E, Sondo E, Gianotti A, Scudieri P, Bandiera T, Galietta LJV.   +14 more
europepmc   +8 more sources

Reinvestigation of Mycothiazole Reveals the Penta-2,4-dien-1-ol Residue Imparts Picomolar Potency and 8S Configuration. [PDF]

ACS Med Chem Lett, 2020
Reinvestigation of mycothiazole (1) revealed picomolar potency (IC50 = 0.00016, 0.00027, 0.00035 μM) against pancreatic, (PANC-1), liver (HepG2), and colon (HCT-116) tumor cell lines. Reevaluation of 1 provided [α]D data indicating Vanuatu specimens of C.
Johnson TA, Morris JD, Coppage DA, Cook CV, Persi LN, Ogarrio MA, Garcia TC, McIntosh NL, McCauley EP, Media J, Maheshwari M, Valeriote FA, Shaw J, Crews P.   +13 more
europepmc   +7 more sources

An Extended Structure-Activity Relationship of Nondioxin-Like PCBs Evaluates and Supports Modeling Predictions and Identifies Picomolar Potency of PCB 202 Towards Ryanodine Receptors. [PDF]

Toxicol Sci, 2017
Nondioxin-like polychlorinated biphenyls (NDL PCBs) activate ryanodine-sensitive Ca2+ channels (RyRs) and this activation has been associated with neurotoxicity in exposed animals. RyR-active congeners follow a distinct structure-activity relationship and a quantitative structure-activity relationship (QSAR) predicts that a large number of PCBs likely ...
Holland EB, Feng W, Zheng J, Dong Y, Li X, Lehmler HJ, Pessah IN.   +6 more
europepmc   +8 more sources

Bispecific antibodies directed to CD4 domain 2 and HIV envelope exhibit exceptional breadth and picomolar potency against HIV-1. [PDF]

Proc Natl Acad Sci U S A, 2013
In the absence of an effective HIV-1 vaccine, passive immunization using broadly neutralizing Abs or Ab-like molecules could provide an alternative to the daily administration of oral antiretroviral agents that has recently shown promise as preexposure prophylaxis.
Pace CS, Song R, Ochsenbauer C, Andrews CD, Franco D, Yu J, Oren DA, Seaman MS, Ho DD.   +8 more
europepmc   +6 more sources

Nonreducing Sugar Scaffold Enables the Development of Immunomodulatory TLR4‐specific LPS Mimetics with Picomolar Potency [PDF]

Angewandte Chemie International Edition
Innate immune defense mechanisms against infection and cancer encompass the modulation of pattern recognition receptor (PRR)-mediated inflammation, including upregulation of various transcription factors and the activation of pro-inflammatory pathways ...
Sebastian Strobl, Daniele Zucchetta, Tomáš Vašíček, Alessandro Monti, Alessandro Ruda, Göran Widmalm, Holger Heine, Alla Zamyatina   +7 more
semanticscholar   +5 more sources

Discovery of a Non-competitive TNFR1 Antagonist Affibody with Picomolar Monovalent Potency That Does Not Affect TNFR2 Function [PDF]

Molecular Pharmaceutics, 2023
Tumor necrosis factor (TNF) is a key regulator of immune responses and plays a significant role in the initiation and maintenance of inflammation. Upregulation of TNF expression leads to several inflammatory diseases, such as Crohn's, ulcerative colitis,
Nagamani Vunnam, MaryJane Been, Evan Huber, Carolyn N. Paulson, Sophia Szymonski, Benjamin J. Hackel, Jonathan N. Sachs   +6 more
semanticscholar   +4 more sources

A_2B Adenosine Receptor Antagonists with Picomolar Potency

Journal of Medicinal Chemistry, 2019
The A2B adenosine receptor (A2BAR) was proposed as a novel target for the (immuno)therapy of cancer since A2BAR blockade results in antiproliferative, antiangiogenic, antimetastatic, and immunostimulatory effects. In this study, we explored the structure-
Jie Jiang, Catharina Julia Seel, Ahmed Temirak, Vigneshwaran Namasivayam, Antonella Arridu, Jakub Schabikowski, Younis Baqi, Sonja Hinz, Jörg Hockemeyer, Christa E. Müller   +9 more
semanticscholar   +4 more sources

Linker Length Matters, Fynomer-Fc Fusion with an Optimized Linker Displaying Picomolar IL-17A Inhibition Potency [PDF]

Journal of Biological Chemistry, 2014
Background: IL-17A is a proinflammatory cytokine involved in various inflammatory diseases. Results: Potent IL-17A inhibitors were generated by fusing human Fyn SH3 domain derivatives (Fynomers) to the Fc part of an antibody.
Michela Silacci, Nadja Baenziger-Tobler, Wibke Lembke, Wenjuan Zha, Sarah Batey, Julian Bertschinger, Dragan Grabulovski   +6 more
semanticscholar   +5 more sources

Trans-, cis-, and dihydro-resveratrol: a comparative study [PDF]

Chemistry Central Journal, 2011
Background Recent studies showed that moderate consumption of red or white wines increased the chances of breast cancer, while similar consumption of red wines, rich in trans-resveratrol (trans-R), decreased the rate of prostate cancer.
Anisimova Natalia YU, Kiselevsky Mikhail V, Sosnov Andrey V, Sadovnikov Sergey V, Stankov Ivan N, Gakh Andrei A   +5 more
doaj   +3 more sources

Llama-derived single domain antibodies to build multivalent, superpotent and broadened neutralizing anti-viral molecules. [PDF]

PLoS ONE, 2011
For efficient prevention of viral infections and cross protection, simultaneous targeting of multiple viral epitopes is a powerful strategy. Llama heavy chain antibody fragments (VHH) against the trimeric envelope proteins of Respiratory Syncytial Virus (
Anna Hultberg, Nigel J Temperton, Valérie Rosseels, Mireille Koenders, Maria Gonzalez-Pajuelo, Bert Schepens, Lorena Itatí Ibañez, Peter Vanlandschoot, Joris Schillemans, Michael Saunders, Robin A Weiss, Xavier Saelens, José A Melero, C Theo Verrips, Steven Van Gucht, Hans J de Haard   +15 more
doaj   +18 more sources