Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy

By Yong S. Chang, B. Graves, V. Guerlavais, C. Tovar, K. Packman, K. To, K. Olson, K. Kesavan, P. Gangurde, A. Mukherjee and 16 more. Proceedings of the National Academy of Sciences of the United States of America, 2013

609 citations recorded by the source corpus.

Subfields: Molecular Biology, Oncology, Organic Chemistry

View Paper: https://www.semanticscholar.org/paper/778c4c293841a05b33dad1eb8e27b34cfb3bcb3f

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In Molecular Biology

1. Wenyi Wei
2. Ji-Hong Hong
3. Lei Chen
4. Kum Khanna
5. Andy Chi-Lung Lee
6. J. Harris
7. T. Meng
8. Ping Wang

In Oncology

1. Nicole J. Yang
2. Marlon J. Hinner

Citations in the corpus

• Getting Across the Cell Membrane: An Overview for Small Molecules, Peptides, and Proteins (2015, background): “Immunoprecipitation demonstrating the intended disruption of intracellular protein–protein interactions has also been presented as evidence of permeation [22, 23].”
• A Comprehensive Review on Current Advances in Peptide Drug Development and Design (2019, background): “This side-chain cyclized α-helical (stapled) peptide is able to selectively bind to and inhibit MDM2/MDMX, thus activating p53-dependent tumor suppression [6].”
• The role of ubiquitination in tumorigenesis and targeted drug discovery (2020, background): “ATSP-7041, a dual inhibitor, can induce p53dependent tumor growth suppression.(394) NSC207895, targeting Mdmx specifically, can act additively with nutlin-3a to activate p53 and induce apoptosis (Fig.”
• Recent advances in the development of protein–protein interactions modulators: mechanisms and clinical trials (2020, background): “Chang et al.74 reported a class of potent MDM2 peptide inhibitors ATSP (Table 3), among which the IC50 value of ATSP-7041 reached 0.9 nM, and the reported Ki values Signal Transduction and Targeted Therapy (2020) 5:213 of the ATSP series peptides reached the nanomolar level.”