A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy

2019 ◽  
Vol 3 (1) ◽  
pp. 145-150 ◽  
Author(s):  
Yinzhu Jin ◽  
Zhenhao Tian ◽  
Xiangge Tian ◽  
Lei Feng ◽  
Jingnan Cui ◽  
...  
Keyword(s):  
Cell Wall ◽  
Real Time ◽  
Fluorescent Probe ◽  
High Throughput ◽  
High Throughput Screening ◽  
Molecular Target ◽  
Cell Wall Synthesis ◽  
Key Enzyme ◽  
Tuberculosis Therapy ◽  
Natural Inhibitors

Fluorescent probeARHBis developed for detecting in various bacteria the activity ofN-acetyltransferase 2 (NAT2), a key enzyme in cell wall synthesis and widely considered to be a molecular target for anti-mycobacterial therapy.

scholarly journals Correction: A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy

2019 ◽  
Vol 3 (10) ◽  
pp. 2190-2190
Author(s):  
Yinzhu Jin ◽  
Zhenhao Tian ◽  
Xiangge Tian ◽  
Lei Feng ◽  
Jingnan Cui ◽  
...  
Keyword(s):  
Real Time ◽  
Fluorescent Probe ◽  
High Throughput ◽  
High Throughput Screening ◽  
Real Time Imaging ◽  
Tuberculosis Therapy ◽  
Natural Inhibitors

Correction for ‘A highly selective fluorescent probe for real-time imaging of bacterial NAT2 and high-throughput screening of natural inhibitors for tuberculosis therapy’ by Yinzhu Jin et al., Mater. Chem. Front., 2019, 3, 145–150.

scholarly journals A High Throughput Screen for Inhibitors of Fungal Cell Wall Synthesis

2002 ◽  
Vol 7 (4) ◽  
pp. 359-366 ◽  
Author(s):  
Jonathan M. Evans ◽  
Phillip G. Zaworski ◽  
Christian N. Parker
Keyword(s):  
Cell Wall ◽  
Cell Growth ◽  
High Throughput ◽  
High Throughput Screening ◽  
Osmotic Shock ◽  
Fungal Cell Wall ◽  
Cell Wall Synthesis ◽  
Fungal Cell ◽  
Unique Nature ◽  
Pharmacologically Active

Fungal cell wall synthesis is essential for viability, requiring the activity of genes involved in environmental sensing, precursor synthesis, transport, secretion, and assembly. This multitude of potential targets, the availability of known agents targeting this pathway, and the unique nature of fungal cell wall synthesis make this pathway an appealing target for drug discovery. Here we describe the adaptation of an assay monitoring cell wall synthesis for high-throughput screening. The assay requires fungal cell growth, in the presence of the test compound, for 3 h before the cells are subjected to osmotic shock in the presence of a dye that stains DNA. Miniaturization of the assay to a 384-well plate format and removing a mechanical transfer led to subtle changes in the assay characteristics. Validation of the assay with a library of known pharmacologically active agents has identified a number of different classes of compounds that are active in this assay, causing aberrant cell wall morphology and in many cases the inhibition of fungal cell growth.

Differential Assay for High-Throughput Screening of Antibacterial Compounds

2007 ◽  
Vol 12 (8) ◽  
pp. 1102-1108 ◽  
Author(s):  
Shaun P. Falk ◽  
Andrew T. Ulijasz ◽  
Bernard Weisblum
Keyword(s):  
Cell Wall ◽  
High Throughput ◽  
High Throughput Screening ◽  
Immediate Release ◽  
Cell Wall Synthesis ◽  
Compound Library ◽  
Fluorogenic Substrate ◽  
Cell Wall Disruption ◽  
Surfactant Activity ◽  
High Throughput Assay

The previously described Bacillus subtilis reporter strain BAU-102 is capable of detecting cell wall synthesis inhibitors that act at all stages of the cell wall synthesis pathway. In addition, this strain is capable of detecting compounds with hydrophobic/ surfactant activity and alternative mechanisms of cell wall disruption. BAU-102 sequesters preformed β-gal in the periplasm, suggesting leakage of β-gal as the means by which this assay detects compound activities. A model is proposed according to which β-gal release by BAU-102 reflects activation of pathways leading to autolysis. The authors also report a simplified high-throughput assay using BAU-102 combined with the fluorogenic substrate N-methylumbelliferyl-β-D-galactoside as a single reagent. Cell wall inhibitors release β-gal consistently only after 60 min of incubation, whereas compounds with surfactant activity show an almost immediate release. A high-throughput screen of a 480-compound library of known bioactives yielded 8 compounds that cause β-gal release. These results validate the BAU-102 assay as an effective tool in antimicrobial drug discovery. ( Journal of Biomolecular Screening 2007:1102-1108)

scholarly journals Visualization of penicillin G acylase in bacteria and high-throughput screening of natural inhibitors using a ratiometric fluorescent probe

2020 ◽  
Vol 56 (34) ◽  
pp. 4640-4643 ◽  
Author(s):  
Lu Li ◽  
Lei Feng ◽  
Ming Zhang ◽  
Xin He ◽  
Shengqiao Luan ◽  
...  
Keyword(s):  
Fluorescent Probe ◽  
High Throughput ◽  
High Throughput Screening ◽  
Penicillin G Acylase ◽  
Penicillin G ◽  
Natural Inhibitors ◽  
Ratiometric Fluorescent Probe

A ratiometric fluorescent probe (PNA) has been developed to sense and image bacterial penicillin G acylase in addition to the high-throughput screening of PGA inhibitors.

scholarly journals A Near‐Infrared Organic Fluorescent Probe for Broad Applications for Blood Vessels Imaging by High‐Throughput Screening via 3D‐Blood Vessel Models (Small Methods 8/2021)

Small Methods ◽  
2021 ◽  
Vol 5 (8) ◽  
pp. 2170036
Author(s):  
Muhammad Asri Abdul Sisak ◽  
Fiona Louis ◽  
Ichio Aoki ◽  
Sun Hyeok Lee ◽  
Young‐Tae Chang ◽  
...  
Keyword(s):  
Blood Vessel ◽  
Blood Vessels ◽  
Fluorescent Probe ◽  
High Throughput ◽  
High Throughput Screening ◽  
Near Infrared

Volume Cytometry:  Microfluidic Sensor for High-Throughput Screening in Real Time

2005 ◽  
Vol 77 (5) ◽  
pp. 1290-1294 ◽  
Author(s):  
Daniel A. Ateya ◽  
Frederick Sachs ◽  
Philip A. Gottlieb ◽  
Steve Besch ◽  
Susan Z. Hua
Keyword(s):  
Real Time ◽  
High Throughput ◽  
High Throughput Screening

scholarly journals A Staphylococcus aureus clpX Mutant Used as a Unique Screening Tool to Identify Cell Wall Synthesis Inhibitors that Reverse β-Lactam Resistance in MRSA

2021 ◽  
Vol 8 ◽  
Author(s):  
Kristoffer T. Bæk ◽  
Camilla Jensen ◽  
Maya A. Farha ◽  
Tobias K. Nielsen ◽  
Ervin Paknejadi ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Wall ◽  
High Throughput Screening ◽  
Bacterial Infections ◽  
Screening Tool ◽  
Acquired Resistance ◽  
Teichoic Acid ◽  
Acid Synthesis ◽  
Biologically Active ◽  
Cell Wall Synthesis

Staphylococcus aureus is a leading cause of bacterial infections world-wide. Staphylococcal infections are preferentially treated with β-lactam antibiotics, however, methicillin-resistant S. aureus (MRSA) strains have acquired resistance to this superior class of antibiotics. We have developed a growth-based, high-throughput screening approach that directly identifies cell wall synthesis inhibitors capable of reversing β-lactam resistance in MRSA. The screen is based on the finding that S. aureus mutants lacking the ClpX chaperone grow very poorly at 30°C unless specific steps in teichoic acid synthesis or penicillin binding protein (PBP) activity are inhibited. This property allowed us to exploit the S. aureus clpX mutant as a unique screening tool to rapidly identify biologically active compounds that target cell wall synthesis. We tested a library of ∼50,000 small chemical compounds and searched for compounds that inhibited growth of the wild type while stimulating growth of the clpX mutant. Fifty-eight compounds met these screening criteria, and preliminary tests of 10 compounds identified seven compounds that reverse β-lactam resistance of MRSA as expected for inhibitors of teichoic acid synthesis. The hit compounds are therefore promising candidates for further development as novel combination agents to restore β-lactam efficacy against MRSA.

High-Throughput Screening for the Discovery of Iron Homeostasis Modulators Using an Extremely Sensitive Fluorescent Probe

ACS Sensors ◽  
2020 ◽  
Vol 5 (9) ◽  
pp. 2950-2958
Author(s):  
Tasuku Hirayama ◽  
Masato Niwa ◽  
Shusaku Hirosawa ◽  
Hideko Nagasawa
Keyword(s):  
Fluorescent Probe ◽  
High Throughput ◽  
High Throughput Screening ◽  
Iron Homeostasis
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