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Teixobactin

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https://www.readbyqxmd.com/read/27704270/new-structural-templates-for-clinically-validated-and-novel-targets-in-antimicrobial-drug-research-and-development
#1
Philipp Klahn, Mark Brönstrup
The development of bacterial resistance against current antibiotic drugs necessitates a continuous renewal of the arsenal of efficacious drugs. This imperative has not been met by the output of antibiotic research and development of the past decades for various reasons, including the declining efforts of large pharma companies in this area. Moreover, the majority of novel antibiotics are chemical derivatives of existing structures that represent mostly step innovations, implying that the available chemical space may be exhausted...
October 5, 2016: Current Topics in Microbiology and Immunology
https://www.readbyqxmd.com/read/27550357/dual-targeting-of-cell-wall-precursors-by-teixobactin-leads-to-cell-lysis
#2
Tomoyuki Homma, Austin Nuxoll, Autumn Brown Gandt, Patrick Ebner, Ina Engels, Tanja Schneider, Friedrich Götz, Kim Lewis, Brian P Conlon
Teixobactin represents the first member of a newly discovered class of antibiotics that acts through inhibition of cell wall synthesis. Teixobactin binds multiple bactoprenol-coupled cell wall precursors, inhibiting both peptidoglycan and teichoic acid synthesis. Here we show that the impressive bactericidal activity of teixobactin is due to the synergistic inhibition of both targets, resulting in cell wall damage, delocalization of autolysins, and subsequent cell lysis. We also find that teixobactin does not bind mature peptidoglycan further increasing its activity at high cell densities and against vancomycin intermediate resistant (VISA) isolates with thickened peptidoglycan layers...
August 22, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27484680/total-synthesis-of-teixobactin
#3
Kang Jin, Iek Hou Sam, Kathy Hiu Laam Po, Du'an Lin, Ebrahim H Ghazvini Zadeh, Sheng Chen, Yu Yuan, Xuechen Li
To cope with the global bacterial multidrug resistance, scientific communities have devoted significant efforts to develop novel antibiotics, particularly those with new modes of actions. Teixobactin, recently isolated from uncultured bacteria, is considered as a promising first-in-class drug candidate for clinical development. Herein, we report its total synthesis by a highly convergent Ser ligation approach and this strategy allows us to prepare several analogues of the natural product.
2016: Nature Communications
https://www.readbyqxmd.com/read/27388768/new-found-hope-for-antibiotic-discovery-lipid-ii-inhibitors
#4
REVIEW
Vivian Ng, Weng C Chan
Research into antibacterial agents has recently gathered pace in light of the disturbing crisis of antimicrobial resistance. The development of modern tools offers the opportunity of reviving the fallen era of antibacterial discovery through uncovering novel lead compounds that target vital bacterial cell components, such as lipid II. This paper provides a summary of the role of lipid II as well as an overview and insight into the structural features of macrocyclic peptides that inhibit this bacterial cell wall component...
August 26, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27232661/elucidation-of-the-teixobactin-pharmacophore
#5
Hyunjun Yang, Kevin H Chen, James S Nowick
This paper elucidates the teixobactin pharmacophore by comparing the arginine analogue of teixobactin Arg10-teixobactin to seven homologues with varying structure and stereochemistry. The roles of the guanidinium group at position 10, the stereochemistry of the macrolactone ring, and the "tail" comprising residues 1-5 are investigated. The guanidinium group is not necessary for activity; Lys10-teixobactin is more active than Arg10-teixobactin against Gram-positive bacteria in minimum inhibitory concentration (MIC) assays...
July 15, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/27191730/total-synthesis-of-teixobactin
#6
Andrew M Giltrap, Luke J Dowman, Gayathri Nagalingam, Jessica L Ochoa, Roger G Linington, Warwick J Britton, Richard J Payne
The first total synthesis of the cyclic depsipeptide natural product teixobactin is described. Synthesis was achieved by solid-phase peptide synthesis, incorporating the unusual l-allo-enduracididine as a suitably protected synthetic cassette and employing a key on-resin esterification and solution-phase macrolactamization. The synthetic natural product was shown to possess potent antibacterial activity against a range of Gram-positive pathogenic bacteria, including a virulent strain of Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus (MRSA)...
June 3, 2016: Organic Letters
https://www.readbyqxmd.com/read/27168676/combating-tuberculosis-infection-a-forbidding-challenge
#7
REVIEW
Tejal Rawal, Shital Butani
After 50 years drought, several drugs are looming from the pipeline to combat tuberculosis. They will serve as a boon to the field that has been burdened with primitive, inadequate treatments and drug-resistant bacterial strains. From the decades, due to lack of interest and resources, the field has suffered a lot. Learning from the flaws, scientists have renovated their approaches to the finding of new antitubercular drugs. The first line drugs take about six months or more for the entire treatment. The second line remedy for resistant-tuberculosis requires daily injections which carry severe side effects...
January 2016: Indian Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27120596/new-is-old-and-old-is-new-recent-advances-in-antibiotic-based-antibiotic-free-and-ethnomedical-treatments-against-methicillin-resistant-staphylococcus-aureus-wound-infections
#8
REVIEW
Jian-Lin Dou, Yi-Wei Jiang, Jun-Qiu Xie, Xiao-Gang Zhang
Staphylococcus aureus is the most common pathogen of wound infections. Thus far, methicillin-resistant S. aureus (MRSA) has become the major causative agent in wound infections, especially for nosocomial infections. MRSA infections are seldom eradicated by routine antimicrobial therapies. More concerning, some strains have become resistant to the newest antibiotics of last resort. Furthermore, horizontal transfer of a polymyxin resistance gene, mcr-1, has been identified in Enterobacteriaceae, by which resistance to the last group of antibiotics will likely spread rapidly...
2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/26984316/efficient-total-syntheses-and-biological-activities-of-two-teixobactin-analogues
#9
Anish Parmar, Abhishek Iyer, Charlotte S Vincent, Dorien Van Lysebetten, Stephen H Prior, Annemieke Madder, Edward J Taylor, Ishwar Singh
The discovery of the new antibiotic teixobactin has been timely in the race for unearthing novel antibiotics wherein the emergence of drug resistant bacteria poses a serious threat worldwide. Herein, we present the total syntheses and biological activities of two teixobactin analogues. This approach is simple, efficient and has several advantages: it uses commercially available building blocks (except AllocHN-d-Thr-OH), has a single purification step and a good recovery (22%). By using this approach we have synthesised two teixobactin analogues and established that the d-amino acids are critical for the antimicrobial activity of these analogues...
April 26, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/26683668/the-mechanism-of-action-of-lysobactin
#10
Wonsik Lee, Kaitlin Schaefer, Yuan Qiao, Veerasak Srisuknimit, Heinrich Steinmetz, Rolf Müller, Daniel Kahne, Suzanne Walker
Lysobactin, also known as katanosin B, is a potent antibiotic with in vivo efficacy against Staphylococcus aureus and Streptococcus pneumoniae. It was previously shown to inhibit peptidoglycan (PG) biosynthesis, but its molecular mechanism of action has not been established. Using enzyme inhibition assays, we show that lysobactin forms 1:1 complexes with Lipid I, Lipid II, and Lipid II(A)(WTA), substrates in the PG and wall teichoic acid (WTA) biosynthetic pathways. Therefore, lysobactin, like ramoplanin and teixobactin, recognizes the reducing end of lipid-linked cell wall precursors...
January 13, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/26654835/synthesis-and-biological-evaluation-of-a-teixobactin-analogue
#11
Yahya E Jad, Gerardo A Acosta, Tricia Naicker, Melissa Ramtahal, Ayman El-Faham, Thavendran Govender, Hendrik G Kruger, Beatriz G de la Torre, Fernando Albericio
The first synthesis and biological activity of a teixobactin analogue is reported. Substitution of the unusual L-allo-enduracididine residue by the naturally occurring L-arginine was achieved, and the analogue gave an activity trend similar to that of teixobactin (against Gram-postive bacteria) and meropenem, which was approved by the FDA in 1996. The synthetic route used allows for the synthesis of the natural product as well as the development of a program of medicinal chemistry.
December 18, 2015: Organic Letters
https://www.readbyqxmd.com/read/26551990/streptomyces-wadayamensis-mppp-is-a-pyridoxal-5-phosphate-dependent-l-arginine-%C3%AE-deaminase-%C3%AE-hydroxylase-in-the-enduracididine-biosynthetic-pathway
#12
Lanlan Han, Alan W Schwabacher, Graham R Moran, Nicholas R Silvaggi
L-Enduracididine (L-End) is a nonproteinogenic amino acid found in a number of bioactive peptides, including the antibiotics teixobactin, enduracidin, and mannopeptimycin. The potent activity of these compounds against antibiotic-resistant pathogens like MRSA and their novel mode of action have garnered considerable interest for the development of these peptides into clinically relevant antibiotics. This goal has been hampered, at least in part, by the fact that L-End is difficult to synthesize and not currently commercially available...
December 1, 2015: Biochemistry
https://www.readbyqxmd.com/read/26475603/-new-antibacterial-agents-on-the-market-and-in-the-pipeline
#13
REVIEW
W V Kern
After some years of stagnation there have been several new successful developments in the field of antibacterial agents. Most of these new developments have been in conventional antibacterial classes. New drugs among the beta-lactam agents are methicillin-resistant Staphylococcus aureus (MRSA) active cephalosporins (ceftaroline and ceftobiprole) and new combinations of beta-lactam with beta-lactamase inhibitors (ceftolozane/tazobactam, ceftazidime/avibactam, imipenem/relebactam and meropenem/RPX7009). New developments can also be observed among oxazolidinones (tedizolid, radezolid, cadazolid and MRX-I), macrolides/ketolides (modithromycin and solithromycin), aminoglycosides (plazomicin), quinolones (nemonoxacin, delafloxacin and avarofloxacin), tetracyclines (omadacycline and eravacycline) as well as among glycopeptides and lipopeptides (oritavancin, telavancin, dalbavancin and surotomycin)...
November 2015: Der Internist
https://www.readbyqxmd.com/read/26102049/-new-horizont-in-the-fight-against-bacterial-resistance
#14
EDITORIAL
Eduardo Sánchez de Badajoz
No abstract text is available yet for this article.
June 2015: Archivos Españoles de Urología
https://www.readbyqxmd.com/read/26089440/teixobactin-the-first-of-a-new-class-of-antibiotics-discovered-by-ichip-technology
#15
REVIEW
Laura J V Piddock
Teixobactin is a recently described antibiotic of a new class produced by a hitherto undescribed soil microorganism (provisionally named Eleftheria terrae). It was isolated with a new tool, the iChip, that allowed the environmental bacterium to grow and for the antibiotic it produced to be isolated and subsequently identified. Teixobactin has activity against Gram-positive (but not Gram-negative) organisms and mycobacteria and a novel mode of action inhibiting peptidoglycan biosynthesis. In vitro no teixobactin-resistant Staphylococcus aureus or Mycobacterium tuberculosis were selected...
October 2015: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/25968231/multiple-attack-on-bacteria-by-the-new-antibiotic-teixobactin
#16
Franz von Nussbaum, Roderich D Süssmuth
No abstract text is available yet for this article.
June 1, 2015: Angewandte Chemie
https://www.readbyqxmd.com/read/25954620/teixobactin-a-novel-antibiotic-in-treatment-of-gram-positive-bacterial-infections
#17
Arunava Kali
No abstract text is available yet for this article.
March 2015: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/25832105/antibiotic-discovery-goes-underground-the-discovery-of-teixobactin-could-revitalise-the-search-for-new-antibiotics-based-on-the-novel-method-the-researchers-used-to-identify-the-compound
#18
LETTER
https://www.readbyqxmd.com/read/25561178/a-new-antibiotic-kills-pathogens-without-detectable-resistance
#19
Losee L Ling, Tanja Schneider, Aaron J Peoples, Amy L Spoering, Ina Engels, Brian P Conlon, Anna Mueller, Till F Schäberle, Dallas E Hughes, Slava Epstein, Michael Jones, Linos Lazarides, Victoria A Steadman, Douglas R Cohen, Cintia R Felix, K Ashley Fetterman, William P Millett, Anthony G Nitti, Ashley M Zullo, Chao Chen, Kim Lewis
Antibiotic resistance is spreading faster than the introduction of new compounds into clinical practice, causing a public health crisis. Most antibiotics were produced by screening soil microorganisms, but this limited resource of cultivable bacteria was overmined by the 1960s. Synthetic approaches to produce antibiotics have been unable to replace this platform. Uncultured bacteria make up approximately 99% of all species in external environments, and are an untapped source of new antibiotics. We developed several methods to grow uncultured organisms by cultivation in situ or by using specific growth factors...
January 22, 2015: Nature
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