K
Kyle R. Brimacombe
Researcher at National Institutes of Health
Publications - 59
Citations - 3986
Kyle R. Brimacombe is an academic researcher from National Institutes of Health. The author has contributed to research in topics: Pyruvate kinase & P-glycoprotein. The author has an hindex of 25, co-authored 58 publications receiving 2925 citations. Previous affiliations of Kyle R. Brimacombe include Cleveland Clinic Lerner College of Medicine & Cleveland Clinic.
Papers
More filters
Journal ArticleDOI
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.
Journal ArticleDOI
Remdesivir: A Review of Its Discovery and Development Leading to Emergency Use Authorization for Treatment of COVID-19
Richard T. Eastman,Jacob S. Roth,Jacob S. Roth,Kyle R. Brimacombe,Anton Simeonov,Min Shen,Samarjit Patnaik,Matthew D. Hall +7 more
TL;DR: An overview of remdesivir’s discovery, mechanism of action, and the current studies exploring its clinical effectiveness is provided.
Journal ArticleDOI
A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate
Michael E. Pacold,Kyle R. Brimacombe,Sze Ham Chan,Jason M. Rohde,Caroline A. Lewis,Lotteke J Y M Swier,Richard Possemato,Walter W. Chen,Lucas B. Sullivan,Brian P. Fiske,Steve Cho,Elizaveta Freinkman,Kıvanç Birsoy,Monther Abu-Remaileh,Yoav D. Shaul,Chieh Min Liu,Minerva Zhou,Min Jung Koh,Haeyoon Chung,Shawn M. Davidson,Alba Luengo,Amy Wang,Xin Xu,Adam Yasgar,Li Liu,Ganesha Rai,Kenneth D. Westover,Matthew G. Vander Heiden,Min Shen,Nathanael S. Gray,Matthew B. Boxer,David M. Sabatini +31 more
TL;DR: In this article, the authors used a quantitative high-throughput screen to identify small-molecule PHGDH inhibitors, which reduced the incorporation into nucleotides of one-carbon units from glucose-derived and exogenous serine.
Journal ArticleDOI
Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.
Fadi J. Najm,Mayur Madhavan,Anita Zaremba,Elizabeth Shick,Robert T. Karl,Daniel C. Factor,Tyler E. Miller,Tyler E. Miller,Zachary S. Nevin,Christopher Kantor,Alex Sargent,Kevin L. Quick,Daniela Schlatzer,Hong Tang,Ruben Papoian,Kyle R. Brimacombe,Min Shen,Matthew B. Boxer,Ajit Jadhav,Andrew P. Robinson,Joseph R. Podojil,Stephen D. Miller,Robert H. Miller,Robert H. Miller,Paul J. Tesar +24 more
TL;DR: Seven drugs function at nanomolar doses selectively to enhance the generation of mature oligodendrocytes from progenitor cells in vitro and provide a rationale for testing miconazole and clobetasol, or structurally modified derivatives, to enhance remyelination in patients.
Journal ArticleDOI
Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors
Anju Singh,Sreedhar Venkannagari,Kyu H. Oh,Ya Qin Zhang,Jason M. Rohde,Li Liu,Sridhar Nimmagadda,Kuladeep Sudini,Kyle R. Brimacombe,Sachin Gajghate,Jinfang Ma,Amy Wang,Xin Xu,Sampada A. Shahane,Menghang Xia,Juhyung Woo,George A. Mensah,Zhibin Wang,Marc Ferrer,Edward Gabrielson,Zhuyin Li,Fraydoon Rastinejad,Min Shen,Matthew B. Boxer,Shyam Biswal +24 more
TL;DR: It is concluded that targeting NRF2 may represent a promising strategy for the treatment of advanced NSCLC because of its high specificity and selectivity and its ability to bind to and inhibit its downstream target gene expression.