Related Experiment Video

Updated: Jun 6, 2026

PIP-on-a-chip: A Label-free Study of Protein-phosphoinositide Interactions
10:58

PIP-on-a-chip: A Label-free Study of Protein-phosphoinositide Interactions

Published on: July 27, 2017

Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein

Christina Juli1, Martin Sippel, Jens Jäger

  • 1Institute of Pharmacy and Food Chemistry, University of Würzburg, Würzburg, Germany.

Journal of Medicinal Chemistry
|December 15, 2010
PubMed

Insights

Researchers identified new potential inhibitors for the macrophage infectivity potentiator (MIP) protein, a key factor in Legionnaires

Area of Science:

  • Microbiology and Infectious Diseases
  • Drug Discovery and Medicinal Chemistry

Background:

  • Legionella pneumophila causes Legionnaires' disease, with the macrophage infectivity potentiator (MIP) protein identified as a major virulence factor.
  • MIP is an FK506-binding protein (FKBP) crucial for L. pneumophila's intracellular survival and dissemination within lung tissue.

Purpose of the Study:

  • To discover novel small-molecule inhibitors targeting the MIP protein.
  • To explore pipecolic acid derivatives as potential scaffolds for MIP inhibition, starting from known FKBP12 ligands.

Main Methods:

  • Computational analysis of FKBP12 ligands to guide inhibitor design.
  • Chemical synthesis of novel pipecolic acid derivatives.
  • Biological testing to evaluate the inhibitory activity of synthesized compounds against MIP.

Main Results:

  • Identification of a promising chemical scaffold based on pipecolic acid derivatives.
  • Demonstrated potential for these derivatives to inhibit the macrophage infectivity potentiator (MIP) protein.

Conclusions:

  • Pipecolic acid derivatives represent a viable starting point for developing new inhibitors of the MIP protein.
  • This research opens avenues for novel therapeutic strategies against Legionnaires' disease by targeting MIP.

More Related Videos

Legionella pneumophila Outer Membrane Vesicles: Isolation and Analysis of Their Pro-inflammatory Potential on Macrophages08:34

Legionella pneumophila Outer Membrane Vesicles: Isolation and Analysis of Their Pro-inflammatory Potential on Macrophages

Published on: February 22, 2017

Use of Galleria mellonella as a Model Organism to Study Legionella pneumophila Infection12:30

Use of Galleria mellonella as a Model Organism to Study Legionella pneumophila Infection

Published on: November 22, 2013

Related Concept Videos

Inhibitors of Gram-positive Cell Wall Synthesis01:23

Inhibitors of Gram-positive Cell Wall Synthesis

Bacterial cell walls are typically rigid structures composed mainly of peptidoglycan, a mesh-like polymer that provides mechanical strength and maintains cell shape. The synthesis of peptidoglycan is a crucial process in bacterial growth and serves as a primary target for many antibiotics.Mechanism of Action of Beta-Lactam AntibioticsBeta-lactam antibiotics, such as penicillin, inhibit peptidoglycan synthesis in actively growing cells. These antibiotics share a characteristic four-membered...
Inhibitors of Bacterial Protein Synthesis01:25

Inhibitors of Bacterial Protein Synthesis

Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
Phosphoinositides and PIPs01:42

Phosphoinositides and PIPs

Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Atypical Pneumonia01:14

Atypical Pneumonia

Atypical pneumonia, often caused by Mycoplasma pneumoniae, is a form of pulmonary infection that differs from the classical presentation of bacterial pneumonia in both its cause and clinical symptoms. Mycoplasma pneumoniae is a pleomorphic bacterium notable for its lack of a rigid cell wall. This structural characteristic imparts resistance to beta-lactam antibiotics and significantly influences the bacterium’s behavior within the human host.Other pathogens responsible for the disease include...
Gene Regulation in Microbial Communities: Quorum Sensing01:28

Gene Regulation in Microbial Communities: Quorum Sensing

Quorum sensing is a mechanism of bacterial communication that enables coordinated gene expression in response to changes in population density. This facilitates collective behaviors that enhance survival, resource acquisition, and ecological adaptation. This process relies on small signaling molecules called autoinducers that accumulate as bacterial populations grow. When a critical threshold concentration of autoinducers is reached, bacterial cells collectively modify gene expression,...