scholarly journals Conformational interplay in hybrid peptide-helical aromatic foldamer macrocycles

2021 ◽  
Author(s):  
Sebastian Dengler ◽  
Pradeep Kumar Mandal ◽  
Lars Allmendinger ◽  
Céline Douat ◽  
Ivan Huc
Keyword(s):  
Important Class ◽  
Hybrid Peptide ◽  
Bioactive Substances ◽  
Macrocyclic Peptides ◽  
Macrocyclic Peptide

Macrocyclic peptides are an important class of bioactive substances. When inserting an aromatic foldamer segment in a macrocyclic peptide, the strong folding propensity of the former may influence the conformation...

scholarly journals Modulating Protein–Protein Interactions by Cyclic and Macrocyclic Peptides. Prominent Strategies and Examples

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 445
Author(s):  
Rosario González-Muñiz ◽  
María Ángeles Bonache ◽  
María Jesús Pérez de Vega
Keyword(s):  
Protein Interactions ◽  
Recent Progress ◽  
Cell Penetrating Peptides ◽  
Protein Protein Interactions ◽  
Future Mission ◽  
Protein Interfaces ◽  
Peptide Derivatives ◽  
Macrocyclic Peptides ◽  
Synthetic Methodologies ◽  
Macrocyclic Peptide

Cyclic and macrocyclic peptides constitute advanced molecules for modulating protein–protein interactions (PPIs). Although still peptide derivatives, they are metabolically more stable than linear counterparts, and should have a lower degree of flexibility, with more defined secondary structure conformations that can be adapted to imitate protein interfaces. In this review, we analyze recent progress on the main methods to access cyclic/macrocyclic peptide derivatives, with emphasis in a few selected examples designed to interfere within PPIs. These types of peptides can be from natural origin, or prepared by biochemical or synthetic methodologies, and their design could be aided by computational approaches. Some advances to facilitate the permeability of these quite big molecules by conjugation with cell penetrating peptides, and the incorporation of β-amino acid and peptoid structures to improve metabolic stability, are also commented. It is predicted that this field of research could have an important future mission, running in parallel to the discovery of new, relevant PPIs involved in pathological processes.

scholarly journals Macrocyclic peptides that inhibit Wnt signalling via interaction with Wnt3a

2020 ◽  
Vol 1 (1) ◽  
pp. 26-34
Author(s):  
Manuel E. Otero-Ramirez ◽  
Kyoko Matoba ◽  
Emiko Mihara ◽  
Toby Passioura ◽  
Junichi Takagi ◽  
...  
Keyword(s):  
De Novo ◽  
Direct Interaction ◽  
Wnt Signalling ◽  
Rapid Screening ◽  
Macrocyclic Peptides ◽  
Macrocyclic Peptide

Discovery and optimization of de novo macrocyclic peptide binders of Wnt3a through RaPID screening against an afamin-stabilized Wnt3a complex, capable of inhibiting Wnt signalling by direct interaction to the Wnt protein.

scholarly journals Structural Features and Binding Modes of Thioether-Cyclized Peptide Ligands

Biomedicines ◽  
2018 ◽  
Vol 6 (4) ◽  
pp. 116 ◽  
Author(s):  
Manuel Otero-Ramirez ◽  
Toby Passioura ◽  
Hiroaki Suga
Keyword(s):  
Structural Information ◽  
Structural Features ◽  
Crystallographic Analysis ◽  
Peptide Ligands ◽  
Binding Modes ◽  
High Potency ◽  
Affinity Ligands ◽  
Macrocyclic Peptides ◽  
Target Binding ◽  
Macrocyclic Peptide

Macrocyclic peptides are an emerging class of bioactive compounds for therapeutic use. In part, this is because they are capable of high potency and excellent target affinity and selectivity. Over the last decade, several biochemical techniques have been developed for the identification of bioactive macrocyclic peptides, allowing for the rapid isolation of high affinity ligands to a target of interest. A common feature of these techniques is a general reliance on thioether formation to effect macrocyclization. Increasingly, the compounds identified using these approaches have been subjected to x-ray crystallographic analysis bound to their respective targets, providing detailed structural information about their conformation and mechanism of target binding. The present review provides an overview of the target bound thioether-closed macrocyclic peptide structures that have been obtained to date.

Gold liposomes

1996 ◽  
Vol 54 ◽  
pp. 898-899
Author(s):  
James F. Hainfeld
Keyword(s):  
Direct Methods ◽  
Important Class ◽  
Double Bonds ◽  
Membrane Phospholipids ◽  
Essential Ingredient ◽  
Lipid Structures

Lipids are an important class of molecules, being found in membranes, HDL, LDL, and other natural structures, serving essential roles in structure and with varied functions such as compartmentalization and transport. Synthetic liposomes are also widely used as delivery and release vehicles for drugs, cosmetics, and other chemicals; soap is made from lipids. Lipids may form bilayer or multilammellar vesicles, micelles, sheets, tubes, and other structures. Lipid molecules may be linked to proteins, carbohydrates, or other moieties. EM study of this essential ingredient of life has lagged, due to lack of direct methods to visualize lipids without extensive alteration. OsO4 reacts with double bonds in membrane phospholipids, forming crossbridges. This has been the method of choice to both fix and stain membranes, thus far. An earlier work described the use of tungstate clusters (W11) attached to lipid moieties to form lipid structures and lipid probes.

COMPARATIVE ANALYSIS OF BIOACTIVE SUBSTANCES CONTENT IN THE LEAVES AND FRUITS OF A ROWAN-TREE (SORBUS AUCUPARIA FRUCTUS) AND ASSESSMENT OF PROSPECTS IN MEDICINE AND PHARMACY

2020 ◽  
pp. 58-62
Author(s):  
Chernichkina A.D.
Keyword(s):  
Raw Materials ◽  
Wide Distribution ◽  
Biologically Active ◽  
Bioactive Substances ◽  
Plant Raw Materials ◽  
Mountain Ash ◽  
The Russian Federation ◽  
Materials Used ◽  
Active Substances ◽  
Pectin Substances

A large number of biologically active substances, organic acids, tannins, and pectin substances were detected during the study of fruits, leaves, and pulp of the fruits of mountain Ash. The content of these substances in leaves and pulp will significantly expand the arsenal of medicinal plant raw materials used. Given the wide distribution of mountain Ash in the territory of the Russian Federation, harvesting leaves from the same plants after harvesting the fruit and using pulp will make it possible to obtain new phytopreparations.

PERAN AIR REBUSAN DAUN SALAM (SYZGIUM POLYANTHUM) DALAM MENURUNKAN KADAR ASAM URAT

2016 ◽  
Vol 5 (2) ◽  
pp. 83-91
Author(s):  
Miftafu Darussalam ◽  
Dwi Kartika Rukmi
Keyword(s):  
Uric Acid ◽  
Vascular Inflammation ◽  
Vascular Lesion ◽  
Wilcoxon Test ◽  
Test Time ◽  
Control Group ◽  
Target Area ◽  
Bioactive Substances ◽  
Control Group Design ◽  
Boiled Water

Background: Uric acid is a final product or a waste that is resulted from the metabolism of purines. A high level of uric acid (hyperuricemia) will cause several health problems, such as vascular inflammation, smooth muscle proliferation, and vascular lesion in kidneys. The syzygium polyanthum leaves contain bioactive substances that may affect the level of uric acid in blood. Objective: This study aimed to determine the influence of boiled water of syzygium polyanthum leaves to the changes of uric acid levels in the target area of Puskesmas Pandak 1 Bantul. Methods: This study employed pre- and post-test without control group design. The population consisted of all patients with hyperuricemia in the target area of Puskesmas Pandak 1 Bantul. Sample was selected with a concecutive sampling, gaining a total number of 24 respondents. Data were analyzed with the Wilcoxon test. The dose of boiled water of syzygium polyanthum leaves intake was 0.36g/ KgBW, once a day for 14 days. Result: This research showed that the boiled water of syzygium polyanthum leaves decreased hyperuricemia (uric acid levels), along with the significancy value of 0.009 (p <0.05). At the pre-test time, the average level of uric acid reached 7.279 mg/dl, and after the treatment, it decreased to 6.76 mg/dl. Conclusion: This study has established evidence that the boiled water of syzygium polyanthum leaves is able to decrease hyperuricemia (uric acid level in blood). Keywords: syzygium polyanthum, boiled water of syzygium polyanthum leaves, hyperuricemia

ANTI-CANCER COMPOUNDS ISOLATED FROM SOFT CORAL SINULARIA CRUCIATA - ALCYONIIDAE

2012 ◽  
pp. 84-89
Author(s):  
Quoc Hung Vo ◽  
Nguyen Phuong Nhi Doan ◽  
Dinh Quynh Phu Nguyen ◽  
Thi Dieu Tram Ho ◽  
Thi Hoai Nguyen
Keyword(s):  
Mass Spectrometry ◽  
Soft Coral ◽  
Normal Phase ◽  
Ionization Mass ◽  
Medical Field ◽  
Bioactive Substances ◽  
Anti Cancer ◽  
The World ◽  
Pure Compounds ◽  
Layer Chromatography

Objectives: Nowadays, bioactive substances isolated from marine organisms which are abundant and varied in Vietnamese sea attracted more and more the attention of scientists in the world and Vietnam as well. We have studied on soft coral Sinularia cruciata – Alcyoniidae, which has never been studied in Vietnam before, to find substances which are useful in medical field, especially in anti-cancer therapy. Materials and method: Specimens of soft coral Sinularia cruciata were collected from Con Co, Quang Tri province in May 2011. Pure compounds were isolated by using Thin Layer Chromatography; Column Chromatography normal phase and inverse phase; Shephadex LH 20. Structures of them were determined by spectral data of Nuclear Magnetic Resonance (NMR), Electrospray Ionization Mass Spectrometry (ESI-MS). Results & Conclusion: Structures of 4 compounds were identified: (1) 5.8-epidioxycholest-6-en-3-ol (2) Cholesterol (3) 1-O-hexadecyl-glycerol (Chimyl alcohol) (4) Glycerol 1-O-octadecyl ether (Batyl alcohol). The substance (1) was demonstrated to have strong anti-cancer effects in previous study. Key words Sinularia cruciata, Alcyoniidae, 5,8-epidioxycholest-6-en-3-ol, soft coral, cancer.

Sign in / Sign up

Export Citation Format

Share Document