Results 31 to 40 of about 212,806 (232)

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

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

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

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

Tuning CH Hydrogen Bond-Based Receptors toward Picomolar Anion Affinity via the Inductive Effect of Distant Substituents.

Angewandte Chemie, 2023
Inspired by nature, artificial hydrogen bond-based anion receptors have been developed to achieve high anion selectivity; however, their binding affinity is usually low.
Matúš Chvojka, Dominik Madea, Hennie Valkenier, V. Šindelář   +3 more
semanticscholar   +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

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