ArticleJournal of medicinal chemistry2012
Peptide truncation leads to a twist and an unusual increase in affinity for casitas B-lineage lymphoma tyrosine kinase binding domain.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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The trial behind it
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Who cites it
10 citing papers in PubMed.
- Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.ACS medicinal chemistry letters · 2024Article
- Article
- In Vitro Ubiquitination Platform Identifies Methyl Ellipticiniums as Ubiquitin Ligase Inhibitors.SLAS discovery : advancing life sciences R & D · 2021Article
- Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.Bioorganic & medicinal chemistry letters · 2018Article
- Preparation and optimisation of anionic liposomes for delivery of small peptides and cDNA to human corneal epithelial cells.Journal of microencapsulation · 2016Article
- Molecular pathways: cbl proteins in tumorigenesis and antitumor immunity-opportunities for cancer treatment.Clinical cancer research : an official journal of the American Association for Cancer Research · 2015Review
- Small molecule adenosine 5'-monophosphate activated protein kinase (AMPK) modulators and human diseases.Journal of medicinal chemistry · 2015Review
- Casitas B-Lineage Lymphoma RING Domain Inhibitors Protect Mice against High-Fat Diet-Induced Obesity and Insulin Resistance.PloS one · 2015Article
- The paradox of conformational constraint in the design of Cbl(TKB)-binding peptides.Scientific reports · 2013Article
- Development of a fluorescence polarization based high-throughput assay to identify Casitas B-lineage lymphoma RING domain regulators.PloS one · 2013Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
We describe truncation and SAR studies to identify a pentapeptide that binds Cbl tyrosine kinase binding domain with a higher affinity than the parental peptide. The pentapeptide has an alternative binding mode that allows occupancy of a previously uncharacterized groove. A peptide library was used to map the binding site and define the interface landscape. Our results suggest that the pentapeptide is an ideal starting point for the development of inhibitors against Cbl driven diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.