Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin‐1 binding of small molecules
Sign Up to like & getrecommendations! Published in 2020 at "Drug Development Research"
DOI: 10.1002/ddr.21641
Abstract: Neuropilin‐1 (NRP1) is emerging as an important molecule in immune signaling where it has been shown to modulate the actions of TGF‐β1 in macrophages and regulatory T cells. The development of cost‐effective and reliable assays… read more here.
Keywords: novel fluorescent; small molecules; fluorescent chemical; probe suitable ... See more keywords
Synthesis of d-desthiobiotin-AI-2 as a novel chemical probe for autoinducer-2 quorum sensing receptors.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103200
Abstract: In processes regulated by quorum sensing (QS) bacteria respond to the concentration of autoinducers in the environment to engage in group behaviours. Autoinducer-2 (AI-2) is unique as it can foster interspecies communication. Currently, two AI-2… read more here.
Keywords: probe; desthiobiotin; quorum sensing; chemical ... See more keywords
Micro-mixing measurement by chemical probe in homogeneous and isotropic turbulence
Sign Up to like & getrecommendations! Published in 2017 at "Chemical Engineering Journal"
DOI: 10.1016/j.cej.2016.12.001
Abstract: Abstract The chemical probe is commonly used to evaluate the performance of chemical reactors. By a localized injection of chemical reagents, it is possible to measure the local micro-mixing, which is readily related to the… read more here.
Keywords: micro mixing; model; chemical; chemical probe ... See more keywords
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01174
Abstract: STK17B is a member of the death-associated protein kinase family and has been genetically linked to the development of diverse diseases. However, the role of STK17B in normal and disease pathology is poorly defined. Here,… read more here.
Keywords: loop conformation; stk17b; unique loop; dark kinase ... See more keywords
Structure-Based Design of a Chemical Probe Set for the 5-HT5A Serotonin Receptor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02031
Abstract: The 5-HT5A receptor (5-HT5AR), for which no selective agonists and a few antagonists exist, remains the least understood serotonin receptor. A single commercial antagonist, SB-699551, has been widely used to investigate the 5-HT5AR function in… read more here.
Keywords: chemical probe; probe; structure based; serotonin receptor ... See more keywords
Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00697
Abstract: From a designed library of indolyl pyrimidinamines, we identified a highly potent and cell-active chemical probe (17) that inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve). Comprehensive evaluation of inhibitor selectivity confirmed that this PIKfyve probe demonstrates excellent kinome-wide… read more here.
Keywords: roles pikfyve; chemical probe; lifecycle coronaviruses; identification utilization ... See more keywords
SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00399
Abstract: Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members,… read more here.
Keywords: aak1 bmp2k; sgc aak1; bmp2k; chemical probe ... See more keywords
Virtual Screening in Search for a Chemical Probe for Angiotensin-Converting Enzyme 2 (ACE2)
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26247584
Abstract: We elaborate new models for ACE and ACE2 receptors with an excellent prediction power compared to previous models. We propose promising workflows for working with huge compound collections, thereby enabling us to discover optimized protocols… read more here.
Keywords: chemical probe; angiotensin converting; screening search; search chemical ... See more keywords