Slow-binding inhibitors of acetylcholinesterase of medical interest

Structural Studies on Mitotic Spindle Fibres

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100070345 ◽

1978 ◽

Vol 36 (3) ◽

pp. 615-626

Author(s):

J.R. Mcintosh

Keyword(s):

Chemical Composition ◽

Mitotic Spindle ◽

Structural Studies ◽

Mitotic Apparatus ◽

Chemical Studies ◽

Medical Interest ◽

Spindle Fibres

The mitotic apparatus is a structure of obvious biological and medical interest, but it has proved to be a difficult cellular machine to understand. The chemical composition of the spindle is only slightly elucidated, largely because of the difficulties in preparing useful isolates of the structure. Chemical studies of the mitotic spindle have been reviewed elsewhere (Mcintosh, 1977), and will not be discussed further here. One would think that structural studies on the mitotic apparatus (MA) in situ would be straightforward, but even with this approach there is some disagreement in the results obtained with various methods and by different investigators. In this paper I will review briefly the approaches which have been used in structural studies of the MA, pointing out the strengths and problems of each approach. I will summarize the principal findings of the different methods, and identify what seem to be fruitful avenues for further work.

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Science Teaching Excites Medical Interest: A Qualitative Inquiry of Science Education during the 2020 COVID-19 Pandemic

Education Sciences ◽

10.3390/educsci11040148 ◽

2021 ◽

Vol 11 (4) ◽

pp. 148

Author(s):

Xiaoshan Z. Gordy ◽

Wesley Sparkmon ◽

Hyllore Imeri ◽

Andrew Notebaert ◽

Marie Barnard ◽

...

Keyword(s):

Distance Learning ◽

Science Teaching ◽

Science Teachers ◽

Online Teaching ◽

Structured Interview ◽

School Science ◽

Qualitative Inquiry ◽

High School Science ◽

Technology In Teaching ◽

Medical Interest

The national or local lockdowns in response to COVID-19 forced education systems to rapidly shift from in-person to distance learning. The hasty transition undoubtedly imposed tremendous challenges on teachers, students and distance learning infrastructure. The purpose of this study was to investigate how high school science teachers who had previously been trained in flipped-learning and advanced educational technology through the Science Teaching Excites Medical Interest (STEMI) program perceived their transition to distance learning during this pandemic. In this study eleven teachers were interviewed with a semi-structured interview guide. Data were analyzed using the deductive-inductive content analytic approach. Our results indicated that teachers reported having more confidence in using technology for teaching online due in part to their participation in the STEMI program. They also reported internet access as one of the most significant barriers, both for students and teachers. While some teachers thought that students may feel more in control of learning due to absence of time and place limits with distance learning, others may struggle to stay engaged without the classroom support they would normally have received. Teachers generally experienced increased workloads and harder work–life balance with online teaching. In spite of the unforeseen challenges, the pandemic situation afforded teachers with opportunities to adopt different technology in teaching and foresee the need for technology integration in order to better prepare for the unexpected in the future.

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Identification of SARS-CoV-2 Receptor Binding Inhibitors by In Vitro Screening of Drug Libraries

Molecules ◽

10.3390/molecules26113213 ◽

2021 ◽

Vol 26 (11) ◽

pp. 3213

Author(s):

Alon Ben David ◽

Eran Diamant ◽

Eyal Dor ◽

Ada Barnea ◽

Niva Natan ◽

...

Keyword(s):

Receptor Binding ◽

High Throughput Screening ◽

Cell Attachment ◽

Drug Repurposing ◽

Heparin Sodium ◽

Compound Libraries ◽

Global Pandemic ◽

Ic50 Values ◽

Binding Inhibitors

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for the coronavirus disease 2019 (COVID-19) global pandemic. The first step of viral infection is cell attachment, which is mediated by the binding of the SARS-CoV-2 receptor binding domain (RBD), part of the virus spike protein, to human angiotensin-converting enzyme 2 (ACE2). Therefore, drug repurposing to discover RBD-ACE2 binding inhibitors may provide a rapid and safe approach for COVID-19 therapy. Here, we describe the development of an in vitro RBD-ACE2 binding assay and its application to identify inhibitors of the interaction of the SARS-CoV-2 RBD to ACE2 by the high-throughput screening of two compound libraries (LOPAC®1280 and DiscoveryProbeTM). Three compounds, heparin sodium, aurintricarboxylic acid (ATA), and ellagic acid, were found to exert an effective binding inhibition, with IC50 values ranging from 0.6 to 5.5 µg/mL. A plaque reduction assay in Vero E6 cells infected with a SARS-CoV-2 surrogate virus confirmed the inhibition efficacy of heparin sodium and ATA. Molecular docking analysis located potential binding sites of these compounds in the RBD. In light of these findings, the screening system described herein can be applied to other drug libraries to discover potent SARS-CoV-2 inhibitors.

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