Douglas S. Auld
Novartis
119 Papers
666 Citations
Douglas S. Auld is an academic researcher from Novartis. The author has contributed to research in topics: Luciferase & Pyruvate kinase. The author has an hindex of 41, co-authored 115 publications. Previous affiliations of Douglas S. Auld include National Institutes of Health.
Chat about Author
Papers
Inhibition of Pyruvate Kinase M2 by Reactive Oxygen Species Contributes to Cellular Antioxidant Responses
Dimitrios Anastasiou,Dimitrios Anastasiou,George Poulogiannis,George Poulogiannis,John M. Asara,John M. Asara,Matthew B. Boxer,Jian-kang Jiang,Min Shen,Gary Bellinger,Gary Bellinger,Atsuo T. Sasaki,Atsuo T. Sasaki,Jason W. Locasale,Jason W. Locasale,Douglas S. Auld,Craig J. Thomas,Matthew G. Vander Heiden,Matthew G. Vander Heiden,Lewis C. Cantley,Lewis C. Cantley +20 more
TL;DR: In this paper, the authors showed that acute increases in intracellular concentrations of reactive oxygen species (ROS) caused inhibition of the glycolytic enzyme pyruvate kinase M2 (PKM2) through oxidation of Cys358.
•Journal Article
Inhibition of Pyruvate Kinase M2 by Reactive Oxygen Species Contributes to Cellular Antioxidant Responses
Matthew G. Vander Heiden,Dimitrios Anastasiou,George Poulogiannis,John M. Asara,Matthew B. Boxer,Jian-kang Jiang,Min Shen,Bellinger Gary,Atsuo T. Sasaki,Jason W. Locasale,Douglas S. Auld,Craig J. Thomas,Lewis C. Cantley,Gary Bellinger +13 more
TL;DR: In human lung cancer cells, acute increases in intracellular concentrations of ROS caused inhibition of the glycolytic enzyme pyruvate kinase M2 (PKM2) through oxidation of Cys358, which is required to divert glucose flux into the pentose phosphate pathway and generate sufficient reducing potential for detoxification of ROS.
953
Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries.
James Inglese,Douglas S. Auld,Ajit Jadhav,Ronald L. Johnson,Anton Simeonov,Adam Yasgar,Wei Zheng,Christopher P. Austin +7 more
TL;DR: The feasibility of qHTS for accurately profiling every compound in large chemical libraries (>10(5) compounds) is demonstrated, thereby providing a platform for chemical genomics and accelerating the identification of leads for drug discovery.
824
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Dimitrios Anastasiou,Yimin Yu,William J. Israelsen,Jian-kang Jiang,Matthew B. Boxer,Bum Soo Hong,Wolfram Tempel,Svetoslav Dimov,Min Shen,Abhishek K. Jha,Hua Yang,Katherine R. Mattaini,Christian M. Metallo,Brian P. Fiske,Kevin D. Courtney,Scott E. Malstrom,Tahsin M. Khan,Charles Kung,Amanda P. Skoumbourdis,Henrike Veith,Noel Southall,Martin J. Walsh,Kyle R. Brimacombe,William Leister,Sophia Y. Lunt,Zachary R. Johnson,Katharine E. Yen,Kaiko Kunii,Shawn M. Davidson,Heather R. Christofk,Christopher P. Austin,James Inglese,Marian H. Harris,John M. Asara,Gregory Stephanopoulos,Francesco G. Salituro,Shengfang Jin,Lenny Dang,Douglas S. Auld,Hee-Won Park,Lewis C. Cantley,Craig J. Thomas,Matthew G. Vander Heiden,Matthew G. Vander Heiden +43 more
TL;DR: It is shown that expression of PKM1, the pyruvate kinase isoform with high constitutive activity, or exposure to published small molecule PKM2 activators inhibit growth of xenograft tumors and support the notion that small molecule activation ofPKM2 can interfere with anabolic metabolism.
High-throughput screening assays for the identification of chemical probes
James Inglese,Ronald L. Johnson,Anton Simeonov,Menghang Xia,Wei Zheng,Christopher P. Austin,Douglas S. Auld +6 more
TL;DR: High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology as mentioned in this paper, including signal transduction pathways and complex networks functioning in cellular environments.
619