Results 1 to 10 of about 9,317 (205)

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.
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   +6 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   +4 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

A Cell-Based Potency Assay for Determining the Relative Potency of Botulinum Neurotoxin A Preparations Using Manual and Semi-Automated Procedures [PDF]

Toxins
Cell-based potency assays (CBPAs) are required for the potency testing and commercial release of botulinum neurotoxin (BoNT)-based drug products. These CBPAs must account for the toxin’s biological activities while meeting regulatory guidelines for ...
F. Mark Dunning, Sara Hendrickson, Serena Wolfe, Dan Harding, Theresa Geurs, Timothy M. Piazza, Thomas A. Little, Ward C. Tucker   +7 more
doaj   +2 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

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   +4 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   +6 more sources

Optimized ACE2-Fc fusion proteins with picomolar neutralization activity against highly evolved SARS-CoV-2 variants. [PDF]

Protein Sci
Abstract The rapid evolution of severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) has compromised the efficacy of many authorized monoclonal antibody products. This highlights the need for alternative strategies, especially for vulnerable populations such as immunocompromised individuals.
Abancó F, Tarrés-Freixas F, Lepore R, Molina-Molina E, Franco E, Boreika R, Pradenas E, Raïch-Regué D, Erkizia I, Clotet B, Valencia A, Vergara-Alert J, Segalés J, Carrillo J, Izquierdo-Useros N, Blanco J, Trinité B.   +16 more
europepmc   +2 more sources

Development of potent humanized TNFα inhibitory nanobodies for therapeutic applications in TNFα-mediated diseases [PDF]

mAbs
Tumor necrosis factor-alpha (TNFα) is a key pro-inflammatory cytokine implicated in the pathogenesis of numerous inflammatory and autoimmune diseases, including rheumatoid arthritis, inflammatory bowel disease, and neurodegenerative disorders such as ...
Tao Yin, Aubin Ramon, Matthew Greenig, Pietro Sormanni, Luciano D’Adamio   +4 more
doaj   +2 more sources

Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential

Frontiers in Physiology, 2022
In mammalian cells, 10 different adenylyl cyclases produce the ubiquitous second messenger, cyclic adenosine monophosphate (cAMP). Amongst these cAMP-generating enzymes, bicarbonate (HCO3−)-regulated soluble adenylyl cyclase (sAC; ADCY10) is uniquely ...
Thomas Rossetti, Jacob Ferreira, Lubna Ghanem, Hannes Buck, Clemens Steegborn, Robert W. Myers, Peter T. Meinke, Lonny R. Levin, Jochen Buck   +8 more
doaj   +1 more source