scholarly journals Erratum: Simultaneous structure–activity studies and arming of natural products by C–H amination reveal cellular targets of eupalmerin acetate

2013 ◽  
Vol 5 (7) ◽  
pp. 634-634 ◽  
Author(s):  
Jing Li ◽  
Justin S. Cisar ◽  
Cong-Ying Zhou ◽  
Brunilda Vera ◽  
Howard Williams ◽  
...  
2013 ◽  
Vol 5 (6) ◽  
pp. 510-517 ◽  
Author(s):  
Jing Li ◽  
Justin S. Cisar ◽  
Cong-Ying Zhou ◽  
Brunilda Vera ◽  
Howard Williams ◽  
...  

RSC Advances ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 2453-2461
Author(s):  
Min-Che Tung ◽  
Keng-Chang Tsai ◽  
Kit-Man Fung ◽  
Ming-Jaw Don ◽  
Tien-Sheng Tseng

The cytosolic non-receptor protein kinase, spleen tyrosine kinase (SYK), is an attractive drug target in autoimmune, inflammatory disorder, and cancers indications.


2021 ◽  
Vol 28 ◽  
Author(s):  
Jiahua Cui ◽  
Jiajun Qian ◽  
Larry Ming-Cheung Chow ◽  
Jinping Jia

Background: The proposed central role of cancer stem cells (CSCs) in tumor development has been extended to explain the diverse oncologic phenomena such as multidrug resistance, metastasis and tumor recurrence in clinics. Due to the enhanced expression of ATP-binding cassette transporters and anti-apoptotic factors, stagnation on G0 phase and the strong ability of self-renewal, the CSCs were highly resistant to clinical anticancer drugs. Therefore, the discovery of new drug candidates that could effectively eradicate cancer stem cells afforded promising outcomes in cancer therapy. Introduction: Natural products and their synthetic analogues are a rich source of biologically active compounds and several of them have already been recognized as potent CSCs killers. We aim to provide a collection of recently identified natural products that suppressed the survival of the small invasive CSC populations and combated the drug resistance of these cells in chemotherapy. Results and Conclusion: These anti-CSCs natural products included flavonoids, stilbenes, quinones, terpenoids, polyketide antibiotics, steroids and alkaloids. In the present review, we highlighted the therapeutic potential of natural products and their derivatives against the proliferation and drug resistance of CSCs, their working mechanisms and related structure-activity relationships. Meanwhile, in this survey, several natural products with diverse cellular targets such as the naphthoquinone shikonin and the stilbene resveratrol were characterized as promising lead compounds for future development.


Marine Drugs ◽  
2018 ◽  
Vol 17 (1) ◽  
pp. 3 ◽  
Author(s):  
Takehiro Matsubara ◽  
Masashi Yokoya ◽  
Natchanun Sirimangkalakitti ◽  
Naoki Saito

A general protocol for the asymmetric synthesis of 3-N-arylmethylated right-half model compounds of renieramycins was developed, which enabled structure–activity relationship (SAR) study of several 3-N-arylmethyl derivatives. The most active compound (6a) showed significant cytotoxic activity against human prostate cancer DU145 and colorectal cancer HCT116 cell lines (IC50 = 11.9, and 12.5 nM, respectively).


2016 ◽  
Vol 33 (5) ◽  
pp. 626-636 ◽  
Author(s):  
Andrew M. Piggott ◽  
Peter Karuso

A description of the T7 phage biopanning procedure is provided with tips and advice suitable for setup in a chemistry laboratory.


2018 ◽  
Vol 12 (02.1) ◽  
pp. 24S
Author(s):  
Jennifer Herrmann

Introduction: Natural products are the source of a large fraction of the current pharmaceutics available against human disease. However, the discovery of novel compounds with new mechanisms of action is becoming increasingly challenging. We focused our work on soil-dwelling Myxobacteria from highly diverse samples, which are more and more recognized as an important natural product source. Methodology: Our discovery pipeline combines traditional whole cell-based activity screens with state-of-the-art analytical techniques and a comprehensive dereplication process. Having identified an antimicrobial compound we aim at elucidating its target, MOA and MOR in diverse microbiological screens and by applying ‘omic’ technologies. Results: Two case studies of currently investigated compound classes will be highlighted. Cystobactamids are novel topoisomerase inhibitors that display very pronounced activity on Gram-positive and Gram-negative bacteria. Telomycins from Streptomyces canus bind to cardiolipin and our studies revealed other putative cellular targets. Conclusion: We were able to isolate several new natural products with potent and selective activity against clinically relevant pathogens. Interestingly, underlying MOAs often differ from those of already described antimicrobial agents.


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