Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.

Literature DB >> 23170954

Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.

Jonathan E Bock¹, Jason Gavenonis¹, Joshua A Kritzer¹.

Abstract

Chemical biologists commonly seek out correlations between the physicochemical properties of molecules and their behavior in biological systems. However, a new paradigm is emerging for peptides in which conformation is recognized as the primary determinant of bioactivity and bioavailability. This review highlights an emerging body of work that directly addresses how a peptide's conformation controls its biological effects, cell penetration, and intestinal absorption. Based on this work, the dream of mimicking the potency and bioavailability of natural product peptides is getting closer to reality.

Entities: CellLine Chemical Disease Gene Mutation Species

Mesh：

Substances：
Peptides

Year: 2012 PMID： 23170954 PMCID： PMC4847942 DOI： 10.1021/cb300515u

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

124 in total

1. Improvement of oral peptide bioavailability: Peptidomimetics and prodrug strategies.

Authors:
Journal: Adv Drug Deliv Rev Date: 1997-09-15 Impact factor: 15.470

2. Probing the alpha-helical structural stability of stapled p53 peptides: molecular dynamics simulations and analysis.

Authors: Zuojun Guo; Udayan Mohanty; Justin Noehre; Tomi K Sawyer; Woody Sherman; Goran Krilov
Journal: Chem Biol Drug Des Date: 2010-04 Impact factor: 2.817

3. Conformational flexibility, internal hydrogen bonding, and passive membrane permeability: successful in silico prediction of the relative permeabilities of cyclic peptides.

Authors: Taha Rezai; Jonathan E Bock; Mai V Zhou; Chakrapani Kalyanaraman; R Scott Lokey; Matthew P Jacobson
Journal: J Am Chem Soc Date: 2006-11-01 Impact factor: 15.419

Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.

1. Improvement of oral peptide bioavailability: Peptidomimetics and prodrug strategies.

2. Probing the alpha-helical structural stability of stapled p53 peptides: molecular dynamics simulations and analysis.

3. Conformational flexibility, internal hydrogen bonding, and passive membrane permeability: successful in silico prediction of the relative permeabilities of cyclic peptides.

Review 4. The design of guanidinium-rich transporters and their internalization mechanisms.

5. Conformationally restricted bicyclic analogs of somatostatin.

Review 6. The exploration of macrocycles for drug discovery--an underexploited structural class.

Review 7. Peptidomimetics, a synthetic tool of drug discovery.

8. Alpha-conotoxin Vc1.1 alleviates neuropathic pain and accelerates functional recovery of injured neurones.

9. All-atom model for stabilization of alpha-helical structure in peptides by hydrocarbon staples.

10. Mammalian cell penetration, siRNA transfection, and DNA transfection by supercharged proteins.

1. Highly Constrained Bicyclic Scaffolds for the Discovery of Protease-Stable Peptides via mRNA Display.

2. Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.

3. EPSA: A Novel Supercritical Fluid Chromatography Technique Enabling the Design of Permeable Cyclic Peptides.

Review 4. Getting across the cell membrane: an overview for small molecules, peptides, and proteins.

Review 5. Biosynthesis and Chemical Applications of Thioamides.

6. Stapled peptides: How to be quick on the uptake.

7. Preface.

8. Conformational Restriction of Peptides Using Dithiol Bis-Alkylation.

9. Biosynthesis: Methylating mushrooms.

Review 10. Peptidomimetic therapeutics: scientific approaches and opportunities.