Classification of KRAS-Activating Mutations and the Implications for Therapeutic Intervention
C Johnson, DL Burkhart, KM Haigis - Cancer discovery, 2022 - AACR
Members of the family of RAS proto-oncogenes, discovered just over 40 years ago, were
among the first cancer-initiating genes to be discovered. Of the three RAS family members …
among the first cancer-initiating genes to be discovered. Of the three RAS family members …
The Ras switch in structural and historical perspective
R Gasper, F Wittinghofer - Biological chemistry, 2019 - degruyter.com
Since its discovery as an oncogene more than 40 years ago, Ras has been and still is in the
focus of many academic and pharmaceutical labs around the world. A huge amount of work …
focus of many academic and pharmaceutical labs around the world. A huge amount of work …
Decrypting Allostery in Membrane-Bound K-Ras4B Using Complementary In Silico Approaches Based on Unbiased Molecular Dynamics Simulations
Protein functions are dynamically regulated by allostery, which enables conformational
communication even between faraway residues, and expresses itself in many forms, akin to …
communication even between faraway residues, and expresses itself in many forms, akin to …
Catalytic Mechanism of Non-Target DNA Cleavage in CRISPR-Cas9 Revealed by Ab Initio Molecular Dynamics
CRISPR-Cas9 is a cutting-edge genome editing technology, which uses the endonuclease
Cas9 to introduce mutations at desired sites of the genome. This revolutionary tool is …
Cas9 to introduce mutations at desired sites of the genome. This revolutionary tool is …
Loop dynamics and enzyme catalysis in protein tyrosine phosphatases
Protein tyrosine phosphatases (PTPs) play an important role in cellular signaling and have
been implicated in human cancers, diabetes, and obesity. Despite shared catalytic …
been implicated in human cancers, diabetes, and obesity. Despite shared catalytic …
The CTPase activity of ParB determines the size and dynamics of prokaryotic DNA partition complexes
ParB-like CTPases mediate the segregation of bacterial chromosomes and low-copy
number plasmids. They act as DNA-sliding clamps that are loaded at parS motifs in the …
number plasmids. They act as DNA-sliding clamps that are loaded at parS motifs in the …
ATP can efficiently stabilize protein through a unique mechanism
Recent experiments suggested that ATP can effectively stabilize protein structure and inhibit
protein aggregation when its concentration is less than 10 mM, which is significantly lower …
protein aggregation when its concentration is less than 10 mM, which is significantly lower …
Arginine kinase activates Arginine for phosphorylation by pyramidalization and polarization
Arginine phosphorylation plays numerous roles throughout biology. Arginine kinase (AK)
catalyzes the delivery of an anionic phosphoryl group (PO3–) from ATP to a planar, trigonal …
catalyzes the delivery of an anionic phosphoryl group (PO3–) from ATP to a planar, trigonal …
The Ras dimer structure
T Rudack, C Teuber, M Scherlo, J Güldenhaupt… - Chemical …, 2021 - pubs.rsc.org
Oncogenic mutated Ras is a key player in cancer, but despite intense and expensive
approaches its catalytic center seems undruggable. The Ras dimer interface is a possible …
approaches its catalytic center seems undruggable. The Ras dimer interface is a possible …
Discovery of Thieno [2, 3-d] pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening
L Li, J Liu, Z Yang, H Zhao, B Deng, Y Ren… - European Journal of …, 2022 - Elsevier
A series of novel thieno [2, 3-d] pyrimidine analogs were designed and synthesized as
KRAS G12D inhibitors via combinatorial virtual screening approach. Most compounds …
KRAS G12D inhibitors via combinatorial virtual screening approach. Most compounds …