Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0032285 (
pneumonia
)
54,520
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The human S100 protein family contains small, dimeric and acidic proteins that contain two EF-hand motifs and bind calcium. When
S100A5
binds calcium, its conformation changes and promotes interaction with the target protein. The extracellular domain of RAGE (Receptor of Advanced Glycation End products) contain three domains: C1, C2 and V. The RAGE V domain is the target protein of
S100A5
that promotes cell survival, growth and differentiation by activating several signaling pathways. Pentamidine is an apoptotic and antiparasitic drug that is used to treat or prevent
pneumonia
. Here, we found that pentamidine interacts with
S100A5
using HSQC titration. We elucidated the interactions of
S100A5
with RAGE V domain and pentamidine using fluorescence and NMR spectroscopy. We generated two binary models-the
S100A5
-RAGE V domain and
S100A5
-Pentamidine complex-and then observed that the pentamidine and RAGE V domain share a similar binding region in mS100A5. We also used the WST-1 assay to investigate the bioactivity of
S100A5
, RAGE V domain and pentamidine. These results indicated that pentamidine blocks the binding between
S100A5
and RAGE V domain. This finding is useful for the development of new anti-proliferation drugs.
...
PMID:Pentamidine blocks the interaction between mutant S100A5 and RAGE V domain and inhibits the RAGE signaling pathway. 2729 8