Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-depende...
Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
About this item
Full title
Author / Creator
Chang, Yong S. , Graves, Bradford , Guerlavais, Vincent , Tovar, Christian , Packman, Kathryn , To, Kwong-Him , Olson, Karen A. , Kesavan, Kamala , Gangurde, Pranoti , Mukherjee, Aditi , Baker, Theresa , Darlak, Krzysztof , Elkin, Carl , Filipovic, Zoran , Qureshi, Farooq Z. , Cai, Hongliang , Berry, Pamela , Feyfant, Eric , Shi, Xiangguo E. , Horstick, James , Annis, D. Allen , Manning, Anthony M. , Fotouhi, Nader , Nash, Huw , Vassilev, Lyubomir T. and Sawyer, Tomi K.
Publisher
United States: National Academy of Sciences
Journal title
Language
English
Formats
Publication information
Publisher
United States: National Academy of Sciences
Subjects
More information
Scope and Contents
Contents
Stapled α−helical peptides have emerged as a promising new modality for a wide range of therapeutic targets. Here, we report a potent and selective dual inhibitor of MDM2 and MDMX, ATSP-7041, which effectively activates the p53 pathway in tumors in vitro and in vivo. Specifically, ATSP-7041 binds both MDM2 and MDMX with nanomolar affinities, shows...
Alternative Titles
Full title
Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
Authors, Artists and Contributors
Author / Creator
Graves, Bradford
Guerlavais, Vincent
Tovar, Christian
Packman, Kathryn
To, Kwong-Him
Olson, Karen A.
Kesavan, Kamala
Gangurde, Pranoti
Mukherjee, Aditi
Baker, Theresa
Darlak, Krzysztof
Elkin, Carl
Filipovic, Zoran
Qureshi, Farooq Z.
Cai, Hongliang
Berry, Pamela
Feyfant, Eric
Shi, Xiangguo E.
Horstick, James
Annis, D. Allen
Manning, Anthony M.
Fotouhi, Nader
Nash, Huw
Vassilev, Lyubomir T.
Sawyer, Tomi K.
Identifiers
Primary Identifiers
Record Identifier
TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3767549
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3767549
Other Identifiers
ISSN
0027-8424
E-ISSN
1091-6490
DOI
10.1073/pnas.1303002110
