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Related Concept Videos

RNA Splicing01:32

RNA Splicing

Splicing is the process by which eukaryotic RNA is edited before its translation into protein. The RNA strand transcribed from eukaryotic DNA is called the primary transcript. The primary transcripts that become mRNAs are called precursor messenger RNAs (pre-mRNAs). Eukaryotic pre-mRNA contains alternating sequences of exons and introns. Exons are nucleotide sequences that code for proteins, whereas introns are the non-coding regions. In RNA splicing, introns are removed and exons are bonded...
RNA Splicing01:32

RNA Splicing

Splicing is the process by which eukaryotic RNA is edited before its translation into protein. The RNA strand transcribed from eukaryotic DNA is called the primary transcript. The primary transcripts that become mRNAs are called precursor messenger RNAs (pre-mRNAs). Eukaryotic pre-mRNA contains alternating sequences of exons and introns. Exons are nucleotide sequences that code for proteins, whereas introns are the non-coding regions. In RNA splicing, introns are removed and exons are bonded...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Alternative RNA Splicing02:18

Alternative RNA Splicing

Alternative RNA splicing is the regulated splicing of exons and introns to produce different mature mRNAs from a single pre-mRNA. Unlike in constitutive splicing where a single gene produces a single type of mRNA, alternative splicing allows an organism to produce multiple proteins from a single gene and plays an important role in protein diversity.
There are five types of alternative RNA splicing that vary in the ways the pre-mRNA segments are removed or retained in the mature mRNA. The first...
Induced Pluripotent Stem Cells01:06

Induced Pluripotent Stem Cells

Stem cells are undifferentiated cells that divide and produce different cell types. Ordinarily, cells that have differentiated into a specific cell type are terminally differentiated; however, scientists have found a way to reprogram these mature cells so that they dedifferentiate and return to an unspecialized, proliferative state. These cells are pluripotent like embryonic stem cells—able to produce all cell types—and are called induced pluripotent stem cells (iPSCs).
Somatic cells are...

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Engineering Artificial Factors to Specifically Manipulate Alternative Splicing in Human Cells
10:06

Engineering Artificial Factors to Specifically Manipulate Alternative Splicing in Human Cells

Published on: April 26, 2017

Remediating cancer via splicing modulation.

Mark S Butler1

  • 1Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland , St. Lucia, Brisbane, 4072, Australia.

Journal of Medicinal Chemistry
|August 29, 2013
PubMed
Summary
This summary is machine-generated.

Researchers developed new cancer drugs by modifying spliceosome modulators. They created more stable and potent analogs of FD-895, enhancing anticancer drug development.

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Area of Science:

  • Medicinal Chemistry
  • Cancer Therapeutics
  • Molecular Biology

Background:

  • Spliceosome modulators offer novel cancer treatment mechanisms.
  • Microbial compounds provide a basis for new anticancer drug discovery.

Purpose of the Study:

  • To improve the stability and potency of the spliceosome modulator FD-895.
  • To develop next-generation spliceosome-modulating anticancer drugs.

Main Methods:

  • Structure-activity relationship (SAR) study of FD-895.
  • Synthesis and evaluation of novel analogs for stability and activity.

Main Results:

  • Identified (17S)-FD-895 (1) with enhanced potency and stability.
  • Developed a highly stable cyclopropane analog 2 undergoing preclinical evaluation.

Conclusions:

  • Modified spliceosome modulators show promise for cancer treatment.
  • Analogs of FD-895 serve as templates for future anticancer drug design.