Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction
1
Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
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2
Department of Therapeutic Discovery, Amgen Inc., 360 Binney Street Cambridge, Massachusetts 02142, United States
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Publication type: Journal Article
Publication date: 2012-05-09
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
22524527
Drug Discovery
Molecular Medicine
Abstract
Structure-based rational design led to the discovery of novel inhibitors of the MDM2-p53 protein-protein interaction. The affinity of these compounds for MDM2 was improved through conformational control of both the piperidinone ring and the appended N-alkyl substituent. Optimization afforded 29 (AM-8553), a potent and selective MDM2 inhibitor with excellent pharmacokinetic properties and in vivo efficacy.
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Metrics
143
Total citations:
143
Citations from 2025:
6
(4.2%)
Cite this
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MLA
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GOST
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Rew Y. et al. Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction // Journal of Medicinal Chemistry. 2012. Vol. 55. No. 11. pp. 4936-4954.
GOST all authors (up to 50)
Copy
Rew Y., Huang D., Long A. M., Schneider S., Yakowec P. Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction // Journal of Medicinal Chemistry. 2012. Vol. 55. No. 11. pp. 4936-4954.
Cite this
RIS
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TY - JOUR
DO - 10.1021/jm300354j
UR - https://doi.org/10.1021/jm300354j
TI - Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction
T2 - Journal of Medicinal Chemistry
AU - Rew, Yosup
AU - Huang, David
AU - Long, Alexander M.
AU - Schneider, Steve
AU - Yakowec, Peter
PY - 2012
DA - 2012/05/09
PB - American Chemical Society (ACS)
SP - 4936-4954
IS - 11
VL - 55
PMID - 22524527
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2012_Rew,
author = {Yosup Rew and David Huang and Alexander M. Long and Steve Schneider and Peter Yakowec},
title = {Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction},
journal = {Journal of Medicinal Chemistry},
year = {2012},
volume = {55},
publisher = {American Chemical Society (ACS)},
month = {may},
url = {https://doi.org/10.1021/jm300354j},
number = {11},
pages = {4936--4954},
doi = {10.1021/jm300354j}
}
Cite this
MLA
Copy
Rew, Yosup, et al. “Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction.” Journal of Medicinal Chemistry, vol. 55, no. 11, May. 2012, pp. 4936-4954. https://doi.org/10.1021/jm300354j.