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Related Concept Videos

Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
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...
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

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Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
08:45

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

Published on: July 17, 2020

Druggable cancer phosphatases.

Julia P Vainonen1, Majid Momeny1, Jukka Westermarck2,3

  • 1Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland.

Science Translational Medicine
|April 8, 2021
PubMed
Summary

Targeting phosphatases, enzymes regulating protein phosphorylation, offers new cancer treatment strategies. This review highlights progress in developing drugs against oncogenic SHP2 and tumor suppressor PP2A phosphatases for improved cancer therapies.

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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Protein phosphorylation, crucial for cell signaling, is dysregulated in cancer.
  • Phosphatases, key regulators of phosphorylation, have been historically challenging drug targets.
  • Emerging strategies now focus on targeting specific phosphatases for cancer therapy.

Purpose of the Study:

  • To review therapeutic targeting of oncogenic and tumor suppressor phosphatases in cancer.
  • To discuss small molecules targeting phosphatases like SHP2 and PP2A.
  • To explore advances in clinical development and combination therapies.

Main Methods:

  • Literature review of pharmacological approaches targeting phosphatases.
  • Analysis of small molecules targeting SHP2 and PP2A.
  • Examination of clinical trial data and combination strategies.

Main Results:

  • SHP2 and PP2A are identified as druggable phosphatases with therapeutic potential.
  • Various small molecules targeting these phosphatases are in development.
  • Combination therapies show promise for enhanced efficacy.

Conclusions:

  • Targeting phosphatases represents a promising frontier in cancer drug development.
  • SHP2 and PP2A inhibitors are advancing through clinical trials.
  • Innovative pharmacological strategies are expanding treatment options for cancer patients.