Source 1review2015ChemMedChem
Toolkit/macrocyclic peptides
macrocyclic peptides
Taxonomy: Mechanism Branch / Architecture. Workflows sit above the mechanism and technique branches rather than replacing them.
Summary
Herein we review various classes of cyclic and macrocyclic peptides as chemical probes of protein surfaces and modulators of PPIs.
Usefulness & Problems
Why this is useful
Macrocyclic peptides are reviewed as chemical probes of protein surfaces and as modulators of protein–protein interactions. The abstract positions them as peptide-like molecules with targeting potential in this space.; recognizing protein surfaces; probing protein–protein interactions; modulating protein–protein interactions
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Macrocyclic peptides are reviewed as chemical probes of protein surfaces and as modulators of protein–protein interactions. The abstract positions them as peptide-like molecules with targeting potential in this space.
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recognizing protein surfaces
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probing protein–protein interactions
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modulating protein–protein interactions
Problem solved
They are proposed as a way to specifically target protein–protein interactions that are otherwise difficult to address. This is especially relevant for protein surfaces lacking deep pockets.; providing peptide-like molecules that can specifically target protein–protein interactions
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They are proposed as a way to specifically target protein–protein interactions that are otherwise difficult to address. This is especially relevant for protein surfaces lacking deep pockets.
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providing peptide-like molecules that can specifically target protein–protein interactions
Problem links
providing peptide-like molecules that can specifically target protein–protein interactions
LiteratureThey are proposed as a way to specifically target protein–protein interactions that are otherwise difficult to address. This is especially relevant for protein surfaces lacking deep pockets.
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They are proposed as a way to specifically target protein–protein interactions that are otherwise difficult to address. This is especially relevant for protein surfaces lacking deep pockets.
Taxonomy & Function
Primary hierarchy
Mechanism Branch
Architecture: A reusable architecture pattern for arranging parts into an engineered system.
Mechanisms
conformational constraint via cyclisationprotein–protein interaction modulationprotein surface recognitionTechniques
Structural CharacterizationTarget processes
No target processes tagged yet.
Input: Chemical
Implementation Constraints
cofactor dependency: cofactor requirement unknownencoding mode: genetically encodedimplementation constraint: context specific validationoperating role: actuator
A macrocyclic peptide scaffold is required, but the abstract does not provide details on synthesis, display, or delivery methods. No specific assay or platform is named in the anchor abstract.; requires macrocyclic peptide design; the abstract does not specify synthesis or discovery prerequisites
The abstract does not establish that macrocyclic peptides alone solve intracellular stability, permeability, or clearance challenges. It also does not specify which subclasses work best in which settings.; the abstract does not distinguish macrocyclic-peptide-specific limitations from general peptide liabilities
Validation
Cell-freeBacteriaMammalianMouseHumanTherapeuticIndep. Replication
Supporting Sources
Ranked Claims
Cyclisation can improve peptide properties by constraining the secondary structure of linear peptides.
Recent advances support the potential of peptide-like molecules to specifically target protein–protein interactions.
Peptides have limited biological application because of low intracellular stability, low permeability, and high in vivo clearance.
Peptides are suitable candidates for targeting protein surfaces because they can closely mimic structural features of protein interfaces.
Approval Evidence
1 source4 linked approval claimsfirst-pass slug macrocyclic-peptides
Herein we review various classes of cyclic and macrocyclic peptides as chemical probes of protein surfaces and modulators of PPIs.
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engineering strategysupports
Cyclisation can improve peptide properties by constraining the secondary structure of linear peptides.
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field potentialsupports
Recent advances support the potential of peptide-like molecules to specifically target protein–protein interactions.
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limitation statementsupports
Peptides have limited biological application because of low intracellular stability, low permeability, and high in vivo clearance.
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modality rationalesupports
Peptides are suitable candidates for targeting protein surfaces because they can closely mimic structural features of protein interfaces.
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Comparisons
Source-stated alternatives
Small molecules are the main contrasted approach in the abstract. The supplied web research summary also notes stapled peptides and bicyclic peptides as related modality classes, but the anchor abstract does not explicitly name them.
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Small molecules are the main contrasted approach in the abstract. The supplied web research summary also notes stapled peptides and bicyclic peptides as related modality classes, but the anchor abstract does not explicitly name them.
Source-backed strengths
presented as peptide-like molecules with potential to specifically target protein–protein interactions
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presented as peptide-like molecules with potential to specifically target protein–protein interactions
Compared with stapled peptides
Small molecules are the main contrasted approach in the abstract. The supplied web research summary also notes stapled peptides and bicyclic peptides as related modality classes, but the anchor abstract does not explicitly name them.
Shared frame: source-stated alternative in extracted literature
Strengths here: presented as peptide-like molecules with potential to specifically target protein–protein interactions.
Relative tradeoffs: the abstract does not distinguish macrocyclic-peptide-specific limitations from general peptide liabilities.
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Small molecules are the main contrasted approach in the abstract. The supplied web research summary also notes stapled peptides and bicyclic peptides as related modality classes, but the anchor abstract does not explicitly name them.
Ranked Citations
- 1.