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Literature DB >> 23214419

Stapled peptides with improved potency and specificity that activate p53.

Christopher J Brown¹, Soo T Quah, Janice Jong, Amanda M Goh, Poh C Chiam, Kian H Khoo, Meng L Choong, May A Lee, Larisa Yurlova, Kourosh Zolghadr, Thomas L Joseph, Chandra S Verma, David P Lane.

Abstract

By using a phage display derived peptide as an initial template, compounds have been developed that are highly specific against Mdm2/Mdm4. These compounds exhibit greater potency in p53 activation and protein-protein interaction assays than a compound derived from the p53 wild-type sequence. Unlike Nutlin, a small molecule inhibitor of Mdm2/Mdm4, the phage derived compounds can arrest cells resistant to p53 induced apoptosis over a wide concentration range without cellular toxicity, suggesting they are highly suitable for cyclotherapy.

Entities: Chemical Disease Gene

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Year: 2012 PMID： 23214419 DOI： 10.1021/cb3005148

Source DB: PubMed Journal: ACS Chem Biol ISSN： 1554-8929 Impact factor: 5.100

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Cited

63 in total

1. A stapled peptide antagonist of MDM2 carried by polymeric micelles sensitizes glioblastoma to temozolomide treatment through p53 activation.

Authors: Xishan Chen; Lingyu Tai; Jie Gao; Jianchang Qian; Mingfei Zhang; Beibei Li; Cao Xie; Linwei Lu; Wuyuan Lu; Weiyue Lu
Journal: J Control Release Date: 2015-09-30 Impact factor: 9.776

2. Identification of a Structural Determinant for Selective Targeting of HDMX.

Authors: Yael Ben-Nun; Hyuk-Soo Seo; Edward P Harvey; Zachary J Hauseman; Thomas E Wales; Catherine E Newman; Ann M Cathcart; John R Engen; Sirano Dhe-Paganon; Loren D Walensky
Journal: Structure Date: 2020-04-30 Impact factor: 5.006

Review 3. Hitting Undruggable Targets: Viewing Stabilized Peptide Development through the Lens of Quantitative Systems Pharmacology.

Authors: Lydia Atangcho; Tejas Navaratna; Greg M Thurber
Journal: Trends Biochem Sci Date: 2018-12-15 Impact factor: 13.807

Review 4. An enhanced functional interrogation/manipulation of intracellular signaling pathways with the peptide 'stapling' technology.

Authors: Y He; D Chen; W Zheng
Journal: Oncogene Date: 2015-03-23 Impact factor: 9.867

5. A critical assessment of the synthesis and biological activity of p53/human double minute 2-stapled peptide inhibitors.

Authors: Rike Wallbrecher; Patrick Chène; Stephan Ruetz; Therese Stachyra; Thomas Vorherr; Roland Brock
Journal: Br J Pharmacol Date: 2017-07-06 Impact factor: 8.739

Stapled peptides with improved potency and specificity that activate p53.

1. A stapled peptide antagonist of MDM2 carried by polymeric micelles sensitizes glioblastoma to temozolomide treatment through p53 activation.

2. Identification of a Structural Determinant for Selective Targeting of HDMX.

Review 3. Hitting Undruggable Targets: Viewing Stabilized Peptide Development through the Lens of Quantitative Systems Pharmacology.

Review 4. An enhanced functional interrogation/manipulation of intracellular signaling pathways with the peptide 'stapling' technology.

5. A critical assessment of the synthesis and biological activity of p53/human double minute 2-stapled peptide inhibitors.

6. Structure of the EmrE multidrug transporter and its use for inhibitor peptide design.

7. Cell death and the mitochondria: therapeutic targeting of the BCL-2 family-driven pathway.

Review 8. Pathological unfoldomics of uncontrolled chaos: intrinsically disordered proteins and human diseases.

9. Bridged Analogues for p53-Dependent Cancer Therapy Obtained by S-Alkylation.

Review 10. Drugging the p53 pathway: understanding the route to clinical efficacy.