J
Juan I. Luengo
Researcher at GlaxoSmithKline
Publications - 76
Citations - 2612
Juan I. Luengo is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Receptor & FKBP. The author has an hindex of 27, co-authored 74 publications receiving 2355 citations.
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Journal ArticleDOI
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Juan I. Luengo,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Melody Diamond,Patricia A. Elkins,Christine M. Gardiner,Eric Garver,Seth A. Gilbert,Richard R. Gontarek,Jeffrey R. Jackson,Kevin L. Kershner,Lusong Luo,Kaushik Raha,Christian S. Sherk,Chiu-Mei Sung,David Sutton,Peter J. Tummino,Ronald Wegrzyn,Kurt R. Auger,Dashyant Dhanak +30 more
TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
Journal ArticleDOI
Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist.
Connie L. Erickson-Miller,Evelyne Delorme,Shin-Shay Tian,Christopher B. Hopson,Amy J. Landis,Elizabeth I. Valoret,Teresa S. Sellers,Jon Rosen,Stephen G. Miller,Juan I. Luengo,Kevin J. Duffy,Julian Jenkins +11 more
TL;DR: In conclusion, eltrombopag interacts selectively with the TpoR without competing with Tpo, leading to the increased proliferation and differentiation of human bone marrow progenitor cells into megakaryocytes and increased platelet production.
ComponentDOI
Design, synthesis, and kinetic evaluation of high-affinity fkbp ligands and the x-ray crystal-structures of their complexes with fkbp12.
Dennis A. Holt,Juan I. Luengo,Dennis S. Yamashita,Hye-Ja Oh,Arda L. Konialian,H.‐K. Yen,Leonard W. Rozamus,Martin Brandt,Mary J. Bossard,Mark Alan Levy,Drake S. Eggleston,Jun Liang,L.W Schultz,T.J Stout,Jon Clardy +14 more
TL;DR: In this article, the design and synthesis of high affinity FKBP12 ligands is described, which can inhibit the cis-trans-peptidylprolyl isomerase (rotamase) activity with an inhibition constant as low as 1 nM, yet they possess remarkable structural simplicity relative to FK506 and rapamycin.
Journal ArticleDOI
A small, nonpeptidyl mimic of granulocyte-colony-stimulating factor
Shin Shay Tian,Peter J. Lamb,Andrew G. King,Stephen G. Miller,Linda Kessler,Juan I. Luengo,Laurie Averill,Randall K. Johnson,John G. Gleason,Louis M. Pelus,Susan B. Dillon,Jon Rosen +11 more
TL;DR: A nonpeptidyl small molecule SB 247464, capable of activating granulocyte-colony-stimulating factor (G-CSF) signal transduction pathways, was identified in a high-throughput assay in cultured cells.
Journal ArticleDOI
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.
Kevin J. Duffy,Michael G. Darcy,Evelyne Delorme,Susan B. Dillon,Daniel F. Eppley,Connie L. Erickson-Miller,Leslie Giampa,Christopher B. Hopson,Yifang Huang,Richard M. Keenan,Peter Lamb,Lynnette Leong,Nannan Liu,Stephen G. Miller,Price Alan T,Jon Rosen,Rakhi Shah,Tony Shaw,Heather Smith,Kenneth C. Stark,Shin-Shay Tian,Curtis M. Tyree,Kenneth Wiggall,Lily Zhang,Juan I. Luengo +24 more
TL;DR: Modification of the core structure and adjustment of unwanted functionality resulted in the development of (5-oxo-1,5-dihydropyrazol-4-ylidene)hydrazines which exhibited efficacies equivalent to those of TPO in several cell-based assays designed to measure thrombopoietic activity.