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Related Concept Videos

Peptide Bonds02:43

Peptide Bonds

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A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
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Encoding01:19

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Information enters the brain through encoding, which is the input of information into the memory system. Once sensory information is received from the environment, the brain labels or codes it. The information is then organized with similar information and connected to existing concepts. Encoding occurs through automatic processing and effortful processing.
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Speciation is the evolutionary process resulting in the formation of new, distinct species—groups of reproductively isolated populations.
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Among all the organelles in an animal cell, only mitochondria have their own independent genomes. Animal mitochondrial DNA is a double-stranded, closed-circular molecule with around 20,000 base pairs. Mitochondrial DNA is unique in that one of its two strands, the heavy, or H, -strand is guanine rich, whereas the complementary strand is cytosine rich and called the light, or L, -strand. Compared to nuclear DNA, mitochondrial DNA has a very low percentage of non-coding regions and is marked by...
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Stereoisomerism of Cyclic Compounds02:33

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In this lesson, we delve into the role of ring conformation and its stability, which determines the spatial arrangement and, consequently, the molecular symmetry and stereoisomerism of cyclic compounds. 1,2-Dimethylcyclohexane is used as a case study to evaluate the possible number of stereoisomers. Here, given the multiple (n = 2) chiral centers, there are 2n = 4 possible configurations that lack a plane of symmetry, as the ring skeleton exists in a non-planar chair conformation. In addition,...
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A population is composed of members of the same species that simultaneously live and interact in the same area. When individuals in a population breed, they pass down their genes to their offspring. Many of these genes are polymorphic, meaning that they occur in multiple variants. Such variations of a gene are referred to as alleles. The collective set of all the alleles within a population is known as the gene pool.
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Genetically Encoded Cyclic Peptide Libraries: From Hit to Lead and Beyond.

Jacob Valentine1, Ali Tavassoli1

  • 1School of Chemistry, University of Southampton, Southampton, United Kingdom.

Methods in Enzymology
|November 5, 2018
PubMed
Summary

Cyclic peptides offer diverse, robust scaffolds for drug discovery, excelling in identifying leads for challenging targets like protein-protein interactions. Their unique properties enhance biological activity and resistance to degradation, making them valuable in high-throughput screening.

Keywords:
Cyclic peptidesHit to leadProtein–protein interaction inhibitorsSICLOPPSmRNA display

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Biochemistry

Background:

  • High-throughput screening (HTS) demands diverse chemical libraries for effective lead identification.
  • Cyclic peptides offer advantages over traditional peptides, including enhanced proteolysis resistance and biological activity due to conformational locking.
  • They are increasingly important for tackling complex drug targets such as protein-protein interactions.

Purpose of the Study:

  • To highlight the value of cyclic peptide libraries in modern drug discovery.
  • To discuss the advantages and challenges associated with generating and screening large cyclic peptide libraries.
  • To emphasize the potential of cyclic peptides in overcoming limitations of small molecule approaches.

Main Methods:

  • Review of existing techniques for cyclic peptide library generation and screening.
  • Analysis of the structural properties and biological advantages of cyclic peptides.
  • Discussion of structure-activity relationship (SAR) challenges and opportunities.

Main Results:

  • Cyclic peptides provide a versatile scaffold with high diversity and specificity.
  • They demonstrate improved pharmacokinetic properties and efficacy compared to linear peptides.
  • Their conformational rigidity aids in targeting challenging biological interactions.

Conclusions:

  • Cyclic peptide libraries are essential for advancing drug discovery, particularly for complex targets.
  • Robust design and screening systems are crucial for managing library diversity and complexity.
  • Further exploration of modifications can lead to highly tuned therapeutic leads.