D
Dennis S. Yamashita
Researcher at GlaxoSmithKline
Publications - 49
Citations - 2549
Dennis S. Yamashita is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Cathepsin K & Cathepsin O. The author has an hindex of 23, co-authored 49 publications receiving 2453 citations. Previous affiliations of Dennis S. Yamashita include Yale University.
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Patent
Inhibitors of akt activity
Mark A. Seefeld,Meagan B. Rouse,Dirk A. Heerding,Simon Peace,Dennis S. Yamashita,Mcnulty Kenneth C +5 more
TL;DR: In this article, the use of heterocyclic carboxamide compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis was discussed, and the authors proposed a method to synthesize carboxamides for use as inhibitors.
Journal ArticleDOI
Selectively Engaging β-Arrestins at the Angiotensin II Type 1 Receptor Reduces Blood Pressure and Increases Cardiac Performance
Jonathan D. Violin,Scott M. DeWire,Dennis S. Yamashita,David H. Rominger,Lisa Nguyen,Kevin Schiller,Erin J. Whalen,Maxine Gowen,Michael W. Lark +8 more
TL;DR: The discovery of a potent, selective β-arrestin biased ligand of the angiotensin II type 1 receptor validated the use of biased ligands to selectively target specific receptor functions in drug discovery.
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
Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase
Dirk A. Heerding,Nelson Rhodes,Jack D. Leber,Tammy J. Clark,Richard M. Keenan,Louis V. LaFrance,Mei Li,Igor G. Safonov,Dennis T. Takata,Joseph W. Venslavsky,Dennis S. Yamashita,Anthony E. Choudhry,Robert A. Copeland,Zhihong Lai,Michael D. Schaber,Peter J. Tummino,Susan L. Strum,Edgar R. Wood,Derek R. Duckett,Derek J. Eberwein,Victoria B. Knick,Timothy J. Lansing,Randy T. McConnell,Shu-Yun Zhang,Elisabeth A. Minthorn,Nestor O. Concha,Gregory L. Warren,Rakesh Kumar +27 more
TL;DR: Lead optimization studies culminating in the discovery of compound 3g are described, which is a novel ATP competitive, pan-AKT kinase inhibitor with IC 50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively.
Journal ArticleDOI
A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys
Shaji Kumar,Lauren Dare,Janice A. Vasko-Moser,Ian E. James,Simon M. Blake,David J. Rickard,S M Hwang,Thaddeus A. Tomaszek,Dennis S. Yamashita,Robert W. Marquis,H.-J. Oh,Jae U. Jeong,Daniel F. Veber,M. Gowen,M.W. Lark,George B. Stroup +15 more
TL;DR: The data indicate that SB-462795 potently inhibits human cathepsin K in osteoclasts, resulting in a rapid inhibition of bone resorption both in vitro and in vivo in the monkey, and the therapeutic potential of relacatib in the treatment of postmenopausal osteoporosis is demonstrated.