Výsledky vyhledávání

Manipulating turn residues on de novo designed β-hairpin peptides for selectivity against drug-resistant bacteria

Autor: Peter J. Bond, Devika Mukherjee, Pui Lai Rachel Ee, Jeanette W. P. Teo, Jan K. Marzinek, Jun-Jie Koh, Vanitha Selvarajan, Nhan D.T. Tram, Zi-Chen Jiang, Bernadette Cheng, Pascal Goh, Alister Boags

Publikováno v: Acta Biomaterialia. 135:214-224

Synthetic β-hairpin antimicrobial peptides (AMPs) offer a useful source for the development of novel antimicrobial agents. β-hairpin peptides generally consist of two side strands bridged by a reverse turn. In literature, most studies focused on th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5147fb328057b93e4a839ccf6c040257
https://doi.org/10.1016/j.actbio.2021.09.004

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Design and synthesis of oligo-lipidated arginyl peptide (OLAP) dimers with enhanced physicochemical activity, peptide stability and their antimicrobial actions against MRSA infections

Autor: Roger W. Beuerman, Do Yun Jung, Zhi Hao Ng, Shuimu Lin, Wendy Wan Ling Sin, Shouping Liu, Jun-Jie Koh

Publikováno v: Amino Acids. 50:1329-1345

Multi-drug resistant pathogens have been of increasing concern today. There is an urgent need for the discovery of more potent antibiotics. Cationic antimicrobial peptides (CAMPs) are known to be effective antimicrobial agents against resistant patho

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3e54a8f06c1d89a1af0a2ae08982b96
https://doi.org/10.1007/s00726-018-2607-6

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Semisynthesis and Biological Evaluation of Xanthone Amphiphilics as Selective, Highly Potent Antifungal Agents to Combat Fungal Resistance

Autor: Roger W. Beuerman, Wan Ling Wendy Sin, Fanghui Lim, Shouping Liu, Shuimu Lin, Lin Wang, Li Ren, Derong Cao, Jun-Jie Koh

Publikováno v: Journal of Medicinal Chemistry. 60:10135-10150

New efficient antifungal agents are urgently needed to treat drug-resistant fungal infections. Here, we designed and synthesized a series of cationic xanthone amphiphilics as antifungal agents from natural α-mangostin to combat fungal resistance. Th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3696c056c21ca8bbf302e58e80e8334f
https://doi.org/10.1021/acs.jmedchem.7b01348

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Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA)

Autor: Roger W. Beuerman, Jun-Jie Koh, Derong Cao, Wan Ling Wendy Sin, Lei Zhou, Rajamani Lakshminarayanan, Fanghui Lim, Lin Wang, Li Ren, Shuimu Lin, Thet Tun Aung, Donald T.H. Tan, Shouping Liu

Publikováno v: Journal of Medicinal Chemistry. 60:6152-6165

A new series of semisynthetic flavone-based small molecules mimicking antimicrobial peptides has been designed from natural icaritin to combat drug-resistant Gram-positive bacterial infections. Compound 6 containing two arginine residues exhibited ex

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f081177de682740fe52ee05ecd5a8b6
https://doi.org/10.1021/acs.jmedchem.7b00380

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Symmetrically Substituted Xanthone Amphiphiles Combat Gram-Positive Bacterial Resistance with Enhanced Membrane Selectivity

Autor: Derong Cao, Jianguo Li, Li Ren, Fanghui Lim, Roger W. Beuerman, Thet Tun Aung, Donald T.H. Tan, Jun-Jie Koh, Shuimu Lin, Rajamani Lakshminarayanan, Shouping Liu, Lin Wang, Chandra S. Verma, Yingjun Wang, Hanxun Zou

Publikováno v: Journal of Medicinal Chemistry. 60:1362-1378

This is the first report of the design of a new series of symmetric xanthone derivatives that mimic antimicrobial peptides using a total synthesis approach. This novel design is advantageous because of its low cost, synthetic simplicity and versatili

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1488fc7a3cee0fb2ca380fd6c4ed387
https://doi.org/10.1021/acs.jmedchem.6b01403

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Nonpeptidic Amphiphilic Xanthone Derivatives: Structure–Activity Relationship and Membrane-Targeting Properties

Autor: Derong Cao, Jianguo Li, Wee Luan Koh, Donald T.H. Tan, Chandra S. Verma, Rui Ting Soh, Shouping Liu, Rajamani Lakshminarayanan, Roger W. Beuerman, Hanxun Zou, Shuimu Lin, Huifen Lin, Fang Hui Lim, Jun-Jie Koh

Publikováno v: Journal of Medicinal Chemistry. 59:171-193

We recently reported the bioinspired synthesis of a highly potent nonpeptidic xanthone, 2c (AM-0016), with potent antibacterial activity against MRSA. Herein, we report a thorough structure-activity relationship (SAR) analysis of a series of nonpepti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78f9ed07584e9c499deef437f85920f8
https://doi.org/10.1021/acs.jmedchem.5b01500

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Antimicrobial activity profiles of Amphiphilic Xanthone derivatives are a function of their molecular Oligomerization

Autor: Shuimu Lin, Verma Chandra, Roger W. Beuerman, Jianguo Li, Wendy Wan Ling Sin, Thet Tun Aung, Jun-Jie Koh, Konstantin Pervushin, Shouping Liu, Yang Bai

Publikováno v: Biochimica et biophysica acta. Biomembranes. 1860(11)

Currently, membrane-targeting small antimicrobial peptidomimetics (SAP) are important in antibiotic development because bacteria appear to develop resistance to these surface-active compounds less readily. However, the molecular membrane-targeting ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0032df0aa5b3287cad2d322b31f62e64
https://pubmed.ncbi.nlm.nih.gov/29782818

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N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization

Autor: Donald T.H. Tan, Rajamani Lakshminarayanan, Shouping Liu, Huifen Lin, Ai Ling Tan, Li Mei Pang, Yu Siang Chew, Vonny Caroline, Chandra S. Verma, Jun-Jie Koh, Thet Tun Aung, Roger W. Beuerman, Jianguo Li

Publikováno v: Journal of Medicinal Chemistry. 58:6533-6548

Treating infections caused by multidrug-resistant Gram-negative pathogens is challenging, and there is concern regarding the toxicity of the most effective antimicrobials for Gram-negative pathogens. We hypothesized that conjugating a fatty acid moie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efe2d22c83ef73758bc2182af813badc
https://doi.org/10.1021/acs.jmedchem.5b00628

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A novel fragment based strategy for membrane active antimicrobials against MRSA

Autor: Shouping Liu, Jianguo Li, Yang Bai, Jun-Jie Koh, Roger W. Beuerman, Konstantin Pervushin, Rajamani Lakshminarayanan, Hanxun Zou, Chandra S. Verma, Lei Zhou

Publikováno v: Biochimica et Biophysica Acta (BBA) - Biomembranes. 1848:1023-1031

Membrane active antimicrobials are a promising new generation of antibiotics that hold the potential to avert antibiotic resistance. However, poor understanding of the action mechanism and the lack of general design principles have impeded their deve

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e0aa3fa18093d610de3ccfaafc0c19f
https://doi.org/10.1016/j.bbamem.2015.01.001

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