Functional GLP-1R antibodies identified from a synthetic GPCR-focused library demonstrate potent blood glucose control [PDF]
mAbs, 2021 G protein-coupled receptors (GPCRs) are a group of seven-transmembrane receptor proteins that have proven to be successful drug targets. Antibodies are becoming an increasingly promising modality to target these receptors due to their unique properties ...
Qiang Liu +14 more
doaj +3 more sources
A focused library synthesis and cytotoxicity of quinones derived from the natural product bolinaquinone [PDF]
Royal Society Open Science, 2018 Bolinaquinone is a natural product that is a structurally complex, cytotoxic sesquiterpene quinone. A scaffold simplification and focused library approach using a microwave-assisted Suzuki coupling gave 32 bolinaquinone analogues with good-to-excellent ...
Azadeh Ghods +5 more
doaj +3 more sources
High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses. [PDF]
PLoS Neglected Tropical Diseases, 2013 Dengue virus is a mosquito-borne flavivirus that has a large impact in global health. It is considered as one of the medically important arboviruses, and developing a preventive or therapeutic solution remains a top priority in the medical and scientific
Deu John M Cruz +15 more
doaj +3 more sources
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators. [PDF]
J Med Chem, 2021 Whereas the PROTAC approach to target protein degradation greatly benefits from rational design, the discovery of small-molecule degraders relies mostly on phenotypic screening and retrospective target identification efforts. Here, we describe the design,
Nishiguchi G +25 more
europepmc +2 more sources
Focused library of phenyl-fused macrocyclic amidinoureas as antifungal agents. [PDF]
Mol Divers, 2022 The rise of antimicrobial-resistant phenotypes and the spread of the global pandemic of COVID-19 are worsening the outcomes of hospitalized patients for invasive fungal infections.
Balestri LJI +13 more
europepmc +2 more sources
Focused Library Approach to Discover Discrete Dipeptide Bolaamphiphiles for siRNA Delivery. [PDF]
Biomacromolecules, 2016 In this study, we report a new dipeptide functionalization strategy for developing new dendritic bolaamphiphile vectors for efficient siRNA transfection.
Eldredge AC +3 more
europepmc +2 more sources
Focused Library Generator: case of Mdmx inhibitors
Journal of Computer-Aided Molecular Design, 2019 We present a Focused Library Generator that is able to create from scratch new molecules with desired properties. After training the Generator on the ChEMBL database, transfer learning was used to switch the generator to producing new Mdmx inhibitors that are a promising class of anticancer drugs.
Zhonghua Xia +3 more
semanticscholar +5 more sources
Targeting undruggable carbohydrate recognition sites through focused fragment library design
Communications Chemistry, 2022 Carbohydrate–protein interactions are key for cell–cell and host–pathogen recognition, but their hydrophilic nature makes the development of drug-like inhibitors a challenge.
Elena Shanina +11 more
doaj +7 more sources
Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure. [PDF]
ACS Med Chem Lett, 2012 Focused libraries of enamine derivatives with a nonacidic, nonelectrophilic core structure were screened for inhibitors of dual-specificity protein phosphatases, and an o-hydroxybenzyl derivative RE44 (10d) was identified as a selective inhibitor of ...
Tsuchiya A +6 more
europepmc +2 more sources
Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity [PDF]
International Journal for Parasitology: Drugs and Drug Resistance, 2019 We report the evaluation of 265 compounds from a PDE-focused library for their antischistosomal activity, assessed in vitro using Schistosoma mansoni.
Sanaa S. Botros +19 more
doaj +2 more sources