Results 21 to 30 of about 212,806 (232)

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   +2 more sources

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis

Bioorganic & Medicinal Chemistry Letters, 2007
Conformational analysis of trans-1,2-disubstituted cyclohexane CCR3 antagonist 2 revealed that the cyclohexane linker could be replaced by an acyclic syn-alpha-methyl-beta-hydroxypropyl linker. Synthesis and biological evaluation of mono- and disubstituted propyl linkers support this conformational correlation.
Joseph B. Santella, Daniel S. Gardner, Wenqing Yao, Chongsheng Shi, Prabhakar Reddy, Andrew J. Tebben, George V. Delucca, Dean A. Wacker, Paul S. Watson, Patricia K. Welch, Eric Wadman, Paul Davies, Kimberly A. Solomon, Dani M. Graden, Swamy Yeleswaram, Sandhya Mandlekar, Ilona Kariv, Carl P. Decicco, Soo S. Ko, Percy H. Carter, John V. Duncia   +20 more
semanticscholar   +4 more sources

Engineering a “muco‐trapping” ACE2‐immunoglobulin hybrid with picomolar affinity as an inhaled, pan‐variant immunotherapy for COVID‐19

Bioengineering & Translational Medicine
Soluble angiotensin‐converting enzyme 2 (ACE2) can act as a decoy molecule that neutralizes severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) by blocking spike (S) proteins on virions from binding ACE2 on host cells.
Karthik Tiruthani, Carlos Cruz‐Teran, Jasper F. W. Chan, Alice Ma, Morgan McSweeney, Whitney Wolf, Shoufeng Yuan, Vincent K. M. Poon, Chris C. S. Chan, Lakshmi Botta, Brian Farrer, Ian Stewart, Alison Schaefer, Jasmine Edelstein, Priya Kumar, Harendra Arora, Jeff T. Hutchins, Anthony J. Hickey, Kwok‐Yung Yuen, Samuel K. Lai   +19 more
doaj   +2 more sources

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   +2 more sources

Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy

Journal of Enzyme Inhibition and Medicinal Chemistry
PLK1 is essential for cell cycle regulation and proliferation, and its elevated expression in prostate cancer is associated with high tumour grade. Therefore, PLK1 inhibition is considered a promising strategy for the treatment of prostate cancer.
Zhen Xu, Lixia Guan, Yuting Wang, Miao-Miao Niu, Yashi Ruan, Cen Xu, Li Yang   +6 more
doaj   +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

Enhanced Plasma Stability and Potency of Aryl/Acyloxy Prodrugs of a BTN3A1 Ligand. [PDF]

ACS Med Chem Lett
While ester-based phosphonate prodrugs excel at delivering payloads into cells, their instability in plasma is a hurdle for their advancement. Here, we synthesized new aryl/acyloxy prodrugs of a phosphonate BTN3A1 ligand.
Singh U, Pawge G, Rani S, Hsiao CC, Wiemer DF, Wiemer AJ.   +5 more
europepmc   +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, Silvia Spinelli, Marc Lauwereys, Lucien A. Aarden, Torsten Dreier, Remy Loris, Karen Silence, Caroline Pollet, Christian Cambillau, Hans de Haard   +10 more
openalex   +7 more sources

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Journal of Medicinal Chemistry, 2017
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic "readers" and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases.
Bing Zhou, Jiantao Hu, Fuming Xu, Zhuo Chen, Longchuan Bai, Ester Fernández‐Salas, Mei Lin, Liu Liu, Chao‐Yie Yang, Yujun Zhao, Donna McEachern, Sally Przybranowski, Bo Wen, Duxin Sun, Shaomeng Wang   +14 more
openalex   +4 more sources

Long‐Circulating Nanobody Confers Durable Prophylaxis against Severe Acute Respiratory Syndrome Coronavirus 2 Omicron Infection [PDF]

Advanced NanoBiomed Research
Breakthrough infections in vaccinated population and continuous emergence of severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) variants make it imperative to develop more efficacious medical countermeasures.
Geetha Jyothi Vaskuri, Gang Ye, Fan Bu, Dong Yang, Colleen B. Jonsson, Hailey Turner‐Hubbard, Sydney Winecke, Alise Mendoza, Fang Li, Chalet Tan   +9 more
doaj   +2 more sources