The current understanding of KRAS protein structure and dynamics

Tatu Pantsar1,2

  • 1Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical Sciences, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.

Insights

Targeted therapies for mutant KRAS protein, a common cancer driver, are advancing. New structural data and molecular dynamics simulations offer deeper insights into KRAS dynamics and drug development.

Area of Science:

  • Oncology
  • Structural Biology
  • Computational Biology

Background:

  • Mutant KRAS protein is a key driver in many human cancers.
  • KRAS was historically considered undruggable, but targeted therapies are emerging.
  • Recent advances have increased understanding and structural data availability for KRAS.

Purpose of the Study:

  • To provide an overview of KRAS structural data.
  • To discuss insights into KRAS conformational dynamics from experiments and simulations.
  • To identify knowledge gaps and suggest future research directions for KRAS.

Main Methods:

  • Review of publicly available KRAS structural data.
  • Analysis of experimental data on KRAS conformational dynamics.
  • Application of molecular dynamics (MD) simulations to study KRAS atomistic behavior.

Main Results:

  • Significant increase in KRAS structural data availability.
  • MD simulations provide detailed insights into KRAS protein dynamics.
  • Experimental data reveals key conformational dynamics of KRAS.

Conclusions:

  • Emerging KRAS targeted therapies show promise.
  • Integration of structural data and MD simulations enhances understanding of KRAS.
  • Further research is needed to fully decipher KRAS and guide therapeutic strategies.

Related Concept Videos

The Ras Gene02:38

The Ras Gene

The Ras-gene-encoded proteins are regulators of signaling pathways controlling cell proliferation, differentiation, or cell survival. The Ras-gene family in humans constitutes three primary members—the HRas, NRas, and KRas. These genes code for four functionally distinct yet closely related proteins—the HRas, NRas, KRas4A, and KRas4B. The involvement of mutant Ras genes in human cancer was first discovered in 1982 and is among the most common causes of human tumorigenesis.
Ras is a...
6.9K
Small GTPases - Ras and Rho01:24

Small GTPases - Ras and Rho

Ras and Rho are small monomeric GTPases that act downstream of receptor tyrosine kinase (RTK) and regulate various cellular processes. These GTPases switch between active and inactive states by binding to guanine nucleotides.
Three regulatory proteins control their activity:
5.1K
MAPK Signaling Cascades01:07

MAPK Signaling Cascades

Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
7.7K
Protein Dynamics in Living Cells01:19

Protein Dynamics in Living Cells

Different fluorescence-based techniques are used to study the protein dynamics in living cells. These techniques include FRAP, FRET, and PET.
Fluorescent recovery after photobleaching (FRAP) is a fluorescent-protein-based detection technique used to quantify protein movement rates within the cell. This method exposes a small portion of the cell to an intense laser beam. The laser beam causes permanent photobleaching of the fluorophore-tagged proteins in the exposed region. As the bleached...
2.6K
Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
17.5K
Protein Organization01:24

Protein Organization

Proteins are polymers of amino acid residues. They are versatile and responsible for different cellular functions, including DNA replication, molecular transport, catalysis, and structural support. Proteins have a hierarchical structure comprising at least three levels of organization: primary, secondary, and tertiary structure. Some large proteins have a quaternary structure where individual protein subunits are linked together.
The primary structure of a protein is its amino acid sequence....
8.8K