Development of Selective TGR5 Ligands Based on the 5,6,7,8‐Tetrahydro‐5,5,8,8‐tetramethylnaphthalene Skeleton
Sign Up to like & getrecommendations! Published in 2020 at "ChemMedChem"
DOI: 10.1002/cmdc.202000567
Abstract: TGR5, a G‐protein‐coupled receptor (GPCR), plays an important role in several physiological functions. TGR5 activation through bile acids induces an increase in energy expenditure. Therefore, synthetic TGR5 ligands could be useful for the treatment of… read more here.
Keywords: development selective; selective tgr5; skeleton; tetrahydro tetramethylnaphthalene ... See more keywords
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111952
Abstract: Cyclin-dependent kinase (CDK) family members are promising molecular targets in discovering potent inhibitors in disease settings, they function differentially. CDK2, CDK4 and CDK6, directly regulate the cell cycle, while CDK9 primarily modulates the transcription regulation.… read more here.
Keywords: degrader; development selective; protac; selective mono ... See more keywords
Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01631
Abstract: A recent study illustrated that a fluorescence polarization assay can be used to identify substrate-competitive Hsp70 inhibitors that can be isoform-selective. Herein, we use that assay in a moderate-throughput screen and report the discovery of… read more here.
Keywords: discovery development; development selective; grp78; chemistry ... See more keywords
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from Trypanosoma cruzi.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00106
Abstract: Chagas disease is a parasitic infection affecting millions of people across Latin America, imposing a dramatic socioeconomic burden. Despite the availability of drugs, nifurtimox and benznidazole, lack of efficacy and incidence of side-effects prompt the… read more here.
Keywords: development selective; phosphate dehydrogenase; glucose phosphate; cruzi ... See more keywords
Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core.
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DOI: 10.1039/c7md00281e
Abstract: A series of 18 new 5-[3-(4-aryl-1-piperazinyl)propoxy]coumarin derivatives from the corresponding bromoalkyl derivatives have been designed and synthesized by us using a microwave-assisted protocol. Radioligand binding assays of this series of compounds as well as a… read more here.
Keywords: targeting serotonin; development selective; 5ht1a receptors; serotonin 5ht1a ... See more keywords
Design and development of selective competitive fluorescent ligands for the detection and visualization of Kv7.2/7.3 in vitro.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc00372d
Abstract: A series of specific and potent fluorescent ligands were developed for labelling and visualizing Kv7.2/7.3 based molecular rotation restriction. Probes 21b and 24a were found to be safe and convenient tools to detect and visualize… read more here.
Keywords: design development; fluorescent ligands; development selective; ligands detection ... See more keywords
Trumping Development: Selective Delinking and Coercive Governmentality in US-Africa Relations
Sign Up to like & getrecommendations! Published in 2019 at "Africa Today"
DOI: 10.2979/africatoday.66.1.01
Abstract: Abstract:Globalization is one of the most important socioeconomic processes of recent decades, but it has elicited a reactionary backlash in some countries, leading to calls for reform. President Trump's rise to power in the United… read more here.
Keywords: trumping development; development selective; selective delinking; africa ... See more keywords