F
Francis X. Sullivan
Publications - 11
Citations - 765
Francis X. Sullivan is an academic researcher. The author has contributed to research in topics: Transketolase & Cancer. The author has an hindex of 8, co-authored 11 publications receiving 504 citations.
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Journal ArticleDOI
A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.
Alexander Drilon,Alexander Drilon,Ramamoorthy Nagasubramanian,James F. Blake,Nora Ku,Brian B. Tuch,Kevin Ebata,Steve Smith,Veronique Lauriault,Kolakowski Gabrielle R,Barbara J. Brandhuber,Paul D. Larsen,Karyn Bouhana,Shannon L. Winski,R. Hamor,Wen-I Wu,Andrew Parker,Tony Morales,Francis X. Sullivan,Walter E. DeWolf,Lance Wollenberg,Paul Gordon,Dorothea N. Douglas-Lindsay,Maurizio Scaltriti,Ryma Benayed,Sandeep Raj,Bethany Hanusch,Alison M. Schram,Philip Jonsson,Michael F. Berger,Michael F. Berger,Jaclyn F. Hechtman,Jaclyn F. Hechtman,Barry S. Taylor,Steve Andrews,S. Michael Rothenberg,David M. Hyman,David M. Hyman +37 more
TL;DR: LOXO-195 abrogated resistance in TRK fusion-positive cancers that acquired kinase domain mutations, a shared liability with all existing TRK TKIs, establishes a role for sequential treatment by demonstrating continued TRK dependence and validates a paradigm for the accelerated development of next-generation inhibitors against validated oncogenic targets.
Journal ArticleDOI
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
Fell Jay Bradford,John P. Fischer,Brian R. Baer,James F. Blake,Karyn Bouhana,David Briere,Karin D. Brown,Laurence E. Burgess,Aaron C. Burns,Michael Burkard,Harrah Chiang,Mark Joseph Chicarelli,Cook Adam,John Gaudino,Jill Hallin,Lauren Hanson,Dylan P. Hartley,Hicken Erik James,Gary P. Hingorani,Ronald Jay Hinklin,Macedonio J. Mejia,Peter Olson,Jennifer N. Otten,Susan P. Rhodes,Martha Rodriguez,Pavel Y. Savechenkov,Darin Smith,Niranjan Sudhakar,Francis X. Sullivan,Tony Pisal Tang,Guy Vigers,Lance Wollenberg,James G. Christensen,Matthew A. Marx +33 more
TL;DR: The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRASG12C is described.
Journal ArticleDOI
Chk1 inhibition and Wee1 inhibition combine synergistically to impede cellular proliferation.
Kurtis D. Davies,P LouAnn Cable,Jennifer Garrus,Francis X. Sullivan,Ira von Carlowitz,Yvan Le Huerou,Eli M. Wallace,Richard Woessner,Stefan D. Gross +8 more
TL;DR: The clinical combination of a Chk1 inhibitor and a Wee1 inhibitor holds promise as an effective treatment strategy for cancer.
Journal ArticleDOI
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors
Allen A. Thomas,Y. Le Huerou,J. De Meese,Gunawardana Indrani W,Tomas Kaplan,Todd Romoff,Stephen S. Gonzales,Kevin Ronald Condroski,Boyd Steven A,Josh Ballard,Bryan Bernat,Walter E. DeWolf,May Han,Patrice Lee,Christine Lemieux,Robin Pedersen,Jed Pheneger,Greg Poch,Darin Smith,Francis X. Sullivan,Solly Weiler,S. Kirk Wright,Jie Lin,Barb Brandhuber,Guy Vigers +24 more
TL;DR: Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes alpha-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogen enzyme.
Journal ArticleDOI
Non-charged thiamine analogs as inhibitors of enzyme transketolase.
Allen A. Thomas,J. De Meese,Y. Le Huerou,Boyd Steven A,Todd Romoff,Steven S. Gonzales,Gunawardana Indrani W,Tomas Kaplan,Francis X. Sullivan,Kevin Ronald Condroski,Joseph P. Lyssikatos,Thomas Daniel Aicher,Josh Ballard,Bryan Bernat,Walter E. DeWolf,May Han,Christine Lemieux,Darin Smith,Solly Weiler,S. Kirk Wright,Guy Vigers,Barb Brandhuber +21 more
TL;DR: It is sought to make neutral thiazolium replacements that would be substrates for TPPK, while not necessarily needing thiamine transporters (ThTr1 and ThTr2) for cell penetration.