Discovery of naphthalimide conjugates as fluorescent probes for α_1-adrenoceptors

α1-Adrenoceptors（α1-ARs）, including at least three subtypes, α（1A）, α（1B） and α（1D）, which play essential roles in G protein-coupled receptors（GPCRs）, can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes（1a-1f） for α1-ARs, including two parts, a pharmacophore（quinazoline and phenylpiperazine） for α1-AR recognition and a fluorophore（naphthalimide） for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors,which were used successfully for in vitro visualization of α1-adrenoceptors.

Diagnostic Techniques for COVID-19:A Mini-review of Early Diagnostic Methods

The outbreak of severe pneumonia at the end of 2019 was proved to be caused by the SARS-CoV-2 virus spreading out the world.And COVID-19 spread rapidly through a terrible transmission way by human-to-human,which led to many suspected cases waiting to be diagnosed and huge daily samples needed to be tested by an eff ective and rapid detection method.With an increasing number of COVID-19 infections,medical pressure is severe.Therefore,more e fficient and accurate diagnosis methods were keen urgently established.In this review,we summarized several methods that can rapidly and sensitively identify COVID-19;some of them are widely used as the diagnostic techniques for SARS-CoV-2 in various countries,some diagnostic technologies refer to SARS(Severe Acute Respiratory Syndrome)or/and MERS(Middle East Respiratory Syndrome)detection,which may provide potential diagnosis ideas.

Luminescence of coelenterazine derivatives with C-8 extended electronic conjugation

Replacement of the methylene group at the C-8 position with an extended electronic conjugation is a new promising method to develop red-shifted coelenterazine derivatives. In this paper, we have described an oxygen-containing coelenterazine derivative with a significant red-shifted（63 nm）bioluminescence signal maximum relative to coelenterazine 400a（Deep Blue C^（TM）, 1）. In cell imaging, the sulfur-containing coelenterazine derivative displayed a significantly（1.77 ± 0.09;P≤0.01） higher luminescence signal compared to coelenterazine 400 a and the oxygen-containing coelenterazine derivative exhibited a slightly（0.74 ± 0.08; P≤0.05） lower luminescence signal. It is beneficial to understand further the underlying mechanisms of bioluminescence.

A bestatin-based fluorescent probe for aminopeptidase N cell imaging

Aminopeptidase N （APN） is an important drug target and biomarker for various tumors. The current work characterizes a novel APN-targeted fluorescent probe （Bes-Green, 2） that manifests comparable inhibitory activity with Bestatin. This probe has capacity of tightly binding to the APN for imaging endogenous APN in living human ovarian clear cell carcinoma cells （ES-2） and has potential application in biological study of cellular APN.

BioLeT: A new design strategy for functional bioluminogenic probes

By integrating photoinduced electron transfer（PET） into the design of functional bioluminogenic probes,Urano and his coworkers recently developed a new rational design strategy, BioLeT. It is expected that this BioLeT strategy will enable us to design and develop new bioluminescence probes for detecting various biomolecules with no catalytic or reactive activity.