Article

Developing Small Molecules that Inhibit K-Ras/GTP Binding Based on New Affinity Measurements

2020-07-29

Abstract excerpt

<h4>SUMMARY</h4> RAS genes encode small GTPases essential for proliferation, differentiation, and survival of mammalian cells. RAS gene mutations are associated with approximately 30% of all human cancers. However, based on measurements reported three decades ago of Ras protein affinities to GTP in the 10-20 picomolar range, it has been accepted in the scientific and medical communities that Ras proteins are und...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: ed4e8f7f-5002-5b43-8554-4b6ecb770b6e
DOI: 10.1101/2020.07.27.218248

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Developing Small Molecules that Inhibit K-Ras/GTP Binding Based on New Affinity MeasurementsDOI 10.1101/2020.07.27.218248Read

Small-molecule modulation of Ras signaling.Semantic proximity Read

Targeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRASSemantic proximity Read

The Endeavours in RAS Inhibition - the Past, Present, and Future.Semantic proximity Read

Exploiting RAS Nucleotide Cycling as a Strategy for Drugging RAS-Driven CancersSemantic proximity Read

Ras proteins as therapeutic targets.Semantic proximity Read

Small molecule inhibitors of RAS proteins with oncogenic mutations.Semantic proximity Read

Brønsted-basic small molecules activate GTP hydrolysis in Ras Q61 mutantsSemantic proximity Read

Design of Small Molecules That Compete with Nucleotide Binding to an Engineered Oncogenic KRAS Allele.Semantic proximity Read

Crystallographic Studies of KRAS in Complex with Small Molecules and RAS-Binding Proteins.Semantic proximity Read

Probing RAS Function Using Monobody and NanoBiT Technologies.Semantic proximity Read

BRET-based RAS biosensors that show a novel small molecule is an inhibitor of RAS-effector protein-protein interactions.Semantic proximity Read

Competitive Inhibitors of Ras Effector BindingSemantic proximity Read