Results 11 to 20 of about 9,317 (205)

A potent alpaca-derived nanobody that neutralizes SARS-CoV-2 variants

iScience, 2022
Summary: The spike glycoprotein of SARS-CoV-2 engages with human ACE 2 to facilitate infection. Here, we describe an alpaca-derived heavy chain antibody fragment (VHH), saRBD-1, that disrupts this interaction by competitively binding to the spike protein
Jules B. Weinstein, Timothy A. Bates, Hans C. Leier, Savannah K. McBride, Eric Barklis, Fikadu G. Tafesse   +5 more
doaj   +1 more source

A potent bispecific nanobody protects hACE2 mice against SARS-CoV-2 infection via intranasal administration

Cell Reports, 2021
Summary: The dramatically expanding coronavirus disease 2019 (COVID-19) needs multiple effective countermeasures. Neutralizing nanobodies (Nbs) are a potential therapeutic strategy for treating COVID-19.
Xilin Wu, Lin Cheng, Ming Fu, Bilian Huang, Linjing Zhu, Shijie Xu, Haixia Shi, Doudou Zhang, Huanyun Yuan, Waqas Nawaz, Ping Yang, Qinxue Hu, Yalan Liu, Zhiwei Wu   +13 more
doaj   +1 more source

Glycosylated Neurotensin Analogues Exhibit Sub‐picomolar Anticonvulsant Potency in a Pharmacoresistant Model of Epilepsy [PDF]

ChemMedChem, 2009
AbstractThe glycosylation of neuroactive peptides is a promising strategy to treat neurological and psychiatric disorders. Herein we investigated the effects of site‐specific glycosylation of neurotensin (NT). The glycosylated analogues have low‐nanomolar affinities and agonist activities toward NTS1, and suppress seizures with sub‐picomolar potency ...
Hee-Kyoung, Lee, Liuyin, Zhang, Misty D, Smith, H Steve, White, Grzegorz, Bulaj   +4 more
openaire   +2 more sources

Design and Synthesis of Novel Bis-Imidazolyl Phenyl Butadiyne Derivatives as HCV NS5A Inhibitors

Pharmaceuticals, 2022
In today’s global plan to completely eradicate hepatitis C virus (HCV), the essential list of medications used for HCV treatment are direct-acting antivirals (DAAs), as interferon-sparing regimens have become the standard-of-care (SOC) treatment.
Jehad Hamdy, Nouran Emadeldin, Mostafa M. Hamed, Efseveia Frakolaki, Sotirios Katsamakas, Niki Vassilaki, Grigoris Zoidis, Anna K. H. Hirsch, Mohammad Abdel-Halim, Ashraf H. Abadi   +9 more
doaj   +1 more source

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

Journal of Biological Chemistry, 2014
Fynomers are small binding proteins derived from the human Fyn SH3 domain. Using phage display technology, Fynomers were generated inhibiting the activity of the proinflammatory cytokine interleukin-17A (IL-17A). One specific Fynomer called 2C1 inhibited human IL-17A in vitro with an IC50 value of 2.2 nm.
Silacci, Michela, Baenziger-Tobler, Nadja, Lembke, Wibke, Zha, Wenjuan, Batey, Sarah, Bertschinger, Julian, Grabulovski, Dragan   +6 more
openaire   +2 more sources

Bivalent Llama Single-Domain Antibody Fragments against Tumor Necrosis Factor Have Picomolar Potencies due to Intramolecular Interactions [PDF]

Frontiers in Immunology, 2017
The activity of tumor necrosis factor (TNF), a cytokine involved in inflammatory pathologies, can be inhibited by antibodies or trap molecules. Herein, llama-derived variable heavy-chain domains of heavy-chain antibody (VHH, also called Nanobodies™) were generated for the engineering of bivalent constructs, which antagonize the binding of TNF to its ...
Els Beirnaert, Aline Desmyter, Aline Desmyter, Silvia Spinelli, Silvia Spinelli, Marc Lauwereys, Lucien Aarden, Torsten Dreier, Remy Loris, Remy Loris, Karen Silence, Caroline Pollet, Christian Cambillau, Christian Cambillau, Hans de Haard   +14 more
openaire   +6 more sources

Sulfated Polysaccharides from Macroalgae Are Potent Dual Inhibitors of Human ATP-Hydrolyzing Ectonucleotidases NPP1 and CD39

Marine Drugs, 2021
Extracellular ATP mediates proinflammatory and antiproliferative effects via activation of P2 nucleotide receptors. In contrast, its metabolite, the nucleoside adenosine, is strongly immunosuppressive and enhances tumor proliferation and metastasis.
Vittoria Lopez, Laura Schäkel, H. J. Maximilian Schuh, Michael S. Schmidt, Salahuddin Mirza, Christian Renn, Julie Pelletier, Sang-Yong Lee, Jean Sévigny, Susanne Alban, Gerd Bendas, Christa E. Müller   +11 more
doaj   +1 more source

Structure-based evaluation of C5 derivatives in the catechol diether series targeting HIV-1 reverse transcriptase [PDF]

, 2014
Using a computationally driven approach, a class of inhibitors with picomolar potency known as the catechol diethers were developed targeting the non-nucleoside-binding pocket of HIV-1 reverse transcriptase.
Anderson, Karen S., Bollini, Mariela, Frey, Kathleen M., Gallardo Macias, Ricardo, Gray, William T., Jorgensen, William L., Spasov, Krasimir A.   +6 more
core   +1 more source

Development of PF-06671008, a Highly Potent Anti-P-cadherin/Anti-CD3 Bispecific DART Molecule with Extended Half-Life for the Treatment of Cancer

Antibodies, 2016
Bispecific antibodies offer a promising approach for the treatment of cancer but can be challenging to engineer and manufacture. Here we report the development of PF-06671008, an extended-half-life dual-affinity re-targeting (DART®) bispecific molecule ...
Adam R. Root, Wei Cao, Bilian Li, Peter LaPan, Caryl Meade, Jocelyn Sanford, Macy Jin, Cliona O’Sullivan, Emma Cummins, Matthew Lambert, Alfredo D. Sheehan, Weijun Ma, Scott Gatto, Kelvin Kerns, Khetemenee Lam, Aaron M. D’Antona, Lily Zhu, William A. Brady, Susan Benard, Amy King, Tao He, Lisa Racie, Maya Arai, Dianah Barrett, Wayne Stochaj, Edward R. LaVallie, James R. Apgar, Kristine Svenson, Lidia Mosyak, Yinhua Yang, Gurunadh R. Chichili, Liqin Liu, Hua Li, Steve Burke, Syd Johnson, Ralph Alderson, William J. J. Finlay, Laura Lin, Stéphane Olland, William Somers, Ezio Bonvini, Hans-Peter Gerber, Chad May, Paul A. Moore, Lioudmila Tchistiakova, Laird Bloom   +45 more
doaj   +1 more source

NF449, a novel picomolar potency antagonist at human P2X1 receptors

European Journal of Pharmacology, 2003
The antagonistic effects of the novel suramin analogue 4,4',4",4"'-(carbonylbis(imino-5,1,3-benzenetriylbis(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid (NF449) were analyzed at homomeric human P2X(1) and P2X(7) receptor subtypes (hP2X(1) and hP2X(7)) heterologously expressed in Xenopus oocytes using the two-microelectrode voltage-clamp ...
Hülsmann, Martin, Nickel, Peter, Kassack, Matthias, Schmalzing, Günther, Lambrecht, Günter, Markwardt, Fritz   +5 more
openaire   +3 more sources