Drugging an undruggable pocket on KRAS

Kessler, Dirk; Gmachl, Michael; Mantoulidis, Andreas; J. Martin, Laetitia; Zoephel, Andreas; Mayer, Moriz; Gollner, Andreas; Covini, David; Fischer, Silke; Gerstberger, Thomas; Gmaschitz, Teresa; M. Goodwin, Craig; Greb, Peter; Häring, Daniela; Hela, Wolfgang; Hoffmann, Johann; Karolyi‐Oezguer, Jale; Knesl, Petr; Kornigg, Stefan; Koegl, Manfred; Kousek, Roland; Lamarre, Lyne; Moser, Franziska; Munico-Martinez, Silvia; Peinsipp, Christoph; Phan, Jason; Rinnenthal, Jörg; Sai, Jiqing; Salamon, Christian; Scherbantin, Yvonne; Schipany, Katharina; Schnitzer, Renate; Schrenk, Andreas; Sharps, Bernadette; Siszler, Gabriella; Sun, Qi; G. Waterson, Alex; Wolkerstorfer, B.; Zeeb, Markus; Pearson, Mark; W. Fesik, Stephen; B. McConnell, Darryl

doi:10.1073/pnas.1904529116

Public

Drugging an undruggable pocket on KRAS

Published in Proceedings of the National Academy of Sciences • Jul 22, 2019

Authors:

Dirk Kessler

Michael Gmachl

Andreas Mantoulidis

Abstract

The 3 human RAS genes, KRAS, NRAS, and HRAS, encode 4 different RAS proteins which belong to the protein family of small GTPases that function as binary molecular switches involved in cell signaling. Activating mutations in RAS are among the most common oncogenic drivers in human cancers, with KRAS ...

Subject

KRAS

HRAS

Neuroblastoma RAS viral oncogene homolog

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