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Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6.
J Med Chem. 2014.
PMID: 24432909
Free article.
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP.
Johnson TW, et al. Among authors: lingardo l.
J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3.
J Med Chem. 2014.
PMID: 24819116
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Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH.
Murphy ST, et al. Among authors: lingardo l.
J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23.
J Med Chem. 2011.
PMID: 22040023
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Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays.
Hofler A, Nichols T, Grant S, Lingardo L, Esposito EA, Gridley S, Murphy ST, Kath JC, Cronin CN, Kraus M, Alton G, Xie Z, Sutton S, Gehring M, Ermolieff J.
Hofler A, et al. Among authors: lingardo l.
Anal Biochem. 2011 Jul 15;414(2):179-86. doi: 10.1016/j.ab.2011.03.013. Epub 2011 Mar 12.
Anal Biochem. 2011.
PMID: 21402045
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Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery.
Johnson MC, Hu Q, Lingardo L, Ferre RA, Greasley S, Yan J, Kath J, Chen P, Ermolieff J, Alton G.
Johnson MC, et al. Among authors: lingardo l.
J Comput Aided Mol Des. 2011 Jul;25(7):689-98. doi: 10.1007/s10822-011-9456-7. Epub 2011 Jul 22.
J Comput Aided Mol Des. 2011.
PMID: 21779981
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Development of hepatitis C virus chimeric replicons for identifying broad spectrum NS3 protease inhibitors.
Binder J, Tetangco S, Weinshank M, Maegley K, Lingardo L, Diehl W, Love R, Patick AK, Smith GJ 3rd.
Binder J, et al. Among authors: lingardo l.
Antiviral Res. 2011 Aug;91(2):102-11. doi: 10.1016/j.antiviral.2011.05.007. Epub 2011 May 19.
Antiviral Res. 2011.
PMID: 21620899
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Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1).
Pearce LR, Alton GR, Richter DT, Kath JC, Lingardo L, Chapman J, Hwang C, Alessi DR.
Pearce LR, et al. Among authors: lingardo l.
Biochem J. 2010 Oct 15;431(2):245-55. doi: 10.1042/BJ20101024.
Biochem J. 2010.
PMID: 20704563
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The crystal structure of the RNA-dependent RNA polymerase from human rhinovirus: a dual function target for common cold antiviral therapy.
Love RA, Maegley KA, Yu X, Ferre RA, Lingardo LK, Diehl W, Parge HE, Dragovich PS, Fuhrman SA.
Love RA, et al. Among authors: lingardo lk.
Structure. 2004 Aug;12(8):1533-44. doi: 10.1016/j.str.2004.05.024.
Structure. 2004.
PMID: 15296746
Free article.
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