Elsevier
Bioorganic and Medicinal Chemistry Letters
,  volume 20 ,  issue 23 ,  pages 7085-7091

Small molecule inhibitors of hantavirus infection

Publication type: Journal Article
Publication date: 2010-12-01
Elsevier
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Hantaviruses use α(v)β(3) integrins on the surface of human host cells as a gateway to invasion, hence compounds that target this receptor may be used as antiviral agents. To accomplish this aim, new peptidomimetic compounds were selected based on similarity to a cyclic peptide known to bind the α(v)β(3) receptor. This first round of biological screening identified peptidomimetic molecules which were effective hantavirus inhibitors in the low micromolar range, two thousand times more potent than the original cyclic peptide. Pharmacophore models were built to broaden the structural diversity of the second set of compounds screened. Structure-activity relationships (SAR) were drawn from the entire dataset. Further characterization by dose-response studies revealed that three compounds had potency in the nanomolar range. Selectivity assays with a panel of hantaviruses supported the mechanism of inhibition by targeting the α(v)β(3) receptor, through the β(3) integrin.
Found 
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GOST |
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GOST Copy
HALL P. et al. Small molecule inhibitors of hantavirus infection // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 23. pp. 7085-7091.
GOST all authors (up to 50) Copy
HALL P., Leitão A., Ye C., Kilpatrick K., HJELLE B., Oprea T. I., Larson R. S. Small molecule inhibitors of hantavirus infection // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 23. pp. 7085-7091.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.bmcl.2010.09.092
UR - https://doi.org/10.1016/j.bmcl.2010.09.092
TI - Small molecule inhibitors of hantavirus infection
T2 - Bioorganic and Medicinal Chemistry Letters
AU - HALL, PAMELA
AU - Leitão, Andrei
AU - Ye, Chunyan
AU - Kilpatrick, Kathleen
AU - HJELLE, BRIAN
AU - Oprea, Tudor I.
AU - Larson, Richard S.
PY - 2010
DA - 2010/12/01
PB - Elsevier
SP - 7085-7091
IS - 23
VL - 20
PMID - 20951038
SN - 0960-894X
SN - 1464-3405
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2010_HALL,
author = {PAMELA HALL and Andrei Leitão and Chunyan Ye and Kathleen Kilpatrick and BRIAN HJELLE and Tudor I. Oprea and Richard S. Larson},
title = {Small molecule inhibitors of hantavirus infection},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/j.bmcl.2010.09.092},
number = {23},
pages = {7085--7091},
doi = {10.1016/j.bmcl.2010.09.092}
}
MLA
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MLA Copy
HALL, PAMELA, et al. “Small molecule inhibitors of hantavirus infection.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 23, Dec. 2010, pp. 7085-7091. https://doi.org/10.1016/j.bmcl.2010.09.092.