Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Combined Effects of Drugs: Synergism01:27

Combined Effects of Drugs: Synergism

4.7K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
4.7K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Revealing the Biological Effect of the <i>N</i>-glycosylation of High-Mobility Group Box 1 (HMGB1) Facilitated by Chemical Protein Synthesis.

Journal of the American Chemical Society·2026
Same author

Structure-Guided Designed [<sup>18</sup>F]-labeled FAPI for Enhanced Hydrophilicity: From Preclinical to First-In-Human Study.

Journal of medicinal chemistry·2026
Same author

Total Chemical Synthesis of Interleukin-15 and Interleukin-2: Taming Protein Hydrophobicity and Aggregation by a Versatile Solubilizing Strategy.

Angewandte Chemie (International ed. in English)·2026
Same author

Pyridium-π interaction preserves N,S-benzylidene thioacetals in acidolysis enabling efficient protein chemical synthesis.

Nature communications·2026
Same author

A Catalyst-Free, Tyrosine-Selective Bioconjugation Strategy via Triazine-Pyridine Chemistry for Antibodies.

Organic letters·2026
Same author

Signal Peptide Engineering and Codon Optimization to Enhance α-Gal A Activity for rAAV Gene Therapy of Fabry Disease.

Journal of inherited metabolic disease·2026

Related Experiment Video

Updated: Sep 6, 2025

Author Spotlight: Scalable Drug Screening Protocol for Efficient Discovery of M. abscessus Treatments
07:50

Author Spotlight: Scalable Drug Screening Protocol for Efficient Discovery of M. abscessus Treatments

Published on: October 25, 2024

2.0K

Studies on daptomycin lactam-based analogues.

Hoi Yee Chow1, Kathy Hiu Laam Po2, Sheng Chen2

  • 1Department of Chemistry, State Key Lab of Synthetic Chemistry, The University of Hong Kong, Pok Fu Lam, Hong Kong.

Journal of Peptide Science : an Official Publication of the European Peptide Society
|June 29, 2022
PubMed
Summary
This summary is machine-generated.

A modified daptomycin lactam analogue showed an eightfold increase in antibacterial activity against MRSA. However, further modifications reduced activity, suggesting structural changes impact daptomycin's active conformation.

Keywords:
antibioticscyclic peptidedaptomycinstructure-activity relationship studies

More Related Videos

Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection
11:56

Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection

Published on: October 25, 2013

14.3K
Visualization of Bacterial Resistance using Fluorescent Antibiotic Probes
08:23

Visualization of Bacterial Resistance using Fluorescent Antibiotic Probes

Published on: March 2, 2020

12.9K

Related Experiment Videos

Last Updated: Sep 6, 2025

Author Spotlight: Scalable Drug Screening Protocol for Efficient Discovery of M. abscessus Treatments
07:50

Author Spotlight: Scalable Drug Screening Protocol for Efficient Discovery of M. abscessus Treatments

Published on: October 25, 2024

2.0K
Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection
11:56

Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection

Published on: October 25, 2013

14.3K
Visualization of Bacterial Resistance using Fluorescent Antibiotic Probes
08:23

Visualization of Bacterial Resistance using Fluorescent Antibiotic Probes

Published on: March 2, 2020

12.9K

Area of Science:

  • Medicinal Chemistry
  • Antibiotic Drug Discovery
  • Microbiology

Background:

  • Daptomycin is a crucial lipopeptide antibiotic for treating Gram-positive bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA).
  • Structure-activity relationship (SAR) studies are vital for optimizing antibiotic efficacy and overcoming resistance mechanisms.

Purpose of the Study:

  • To synthesize and evaluate novel daptomycin lactam-based analogues for enhanced antibacterial activity.
  • To investigate the impact of specific structural modifications on daptomycin's antibacterial potency and mechanism.

Main Methods:

  • Synthesis of a series of daptomycin lactam analogues with single and multiple modifications.
  • Determination of minimum inhibitory concentrations (MICs) against methicillin-resistant Staphylococcus aureus (MRSA).

Main Results:

  • A daptomycin analogue with a singly modified lactam demonstrated an eightfold increase in MIC against MRSA compared to native daptomycin.
  • Analogues with multiple modifications, particularly replacement of the n-decanoyl group with a rigid 4-(phenylethynyl)benzoyl moiety, exhibited significantly reduced antibacterial activity.
  • The reduced activity in multiply modified analogues suggests a deviation from the optimal active conformation.

Conclusions:

  • Single lactam modification can enhance daptomycin's activity against MRSA.
  • Complex structural modifications can disrupt the active conformation, leading to loss of antibacterial efficacy.
  • Further research into daptomycin's active conformation is essential for rational drug design and development of new antibiotics.