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Items: 27


Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer.

Wang Z, Grosskurth SE, Cheung T, Petteruti P, Zhang J, Wang X, Wang W, Gharahdaghi F, Wu J, Su N, Howard RT, Mayo M, Widzowski D, Scott DA, Johannes JW, Lamb ML, Lawson D, Dry JR, Lyne PD, Tate EW, Zinda M, Mikule K, Fawell SE, Reimer C, Chen H.

Cancer Res. 2018 Dec 1;78(23):6691-6702. doi: 10.1158/0008-5472.CAN-18-1362. Epub 2018 Oct 8.


BRD4 amplification facilitates an oncogenic gene expression program in high-grade serous ovarian cancer and confers sensitivity to BET inhibitors.

Rhyasen GW, Yao Y, Zhang J, Dulak A, Castriotta L, Jacques K, Zhao W, Gharahdaghi F, Hattersley MM, Lyne PD, Clark E, Zinda M, Fawell SE, Mills GB, Chen H.

PLoS One. 2018 Jul 23;13(7):e0200826. doi: 10.1371/journal.pone.0200826. eCollection 2018.


Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.

Gingipalli L, Block MH, Bao L, Cooke E, Dakin LA, Denz CR, Ferguson AD, Johannes JW, Larsen NA, Lyne PD, Pontz TW, Wang T, Wu X, Wu A, Zhang HJ, Zheng X, Dowling JE, Lamb ML.

Bioorg Med Chem Lett. 2018 May 1;28(8):1336-1341. doi: 10.1016/j.bmcl.2018.03.018. Epub 2018 Mar 7.


Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Yang B, Vasbinder MM, Hird AW, Su Q, Wang H, Yu Y, Toader D, Lyne PD, Read JA, Breed J, Ioannidis S, Deng C, Grondine M, DeGrace N, Whitston D, Brassil P, Janetka JW.

J Med Chem. 2018 Feb 8;61(3):1061-1073. doi: 10.1021/acs.jmedchem.7b01490. Epub 2018 Jan 19.


Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS.

Ross SJ, Revenko AS, Hanson LL, Ellston R, Staniszewska A, Whalley N, Pandey SK, Revill M, Rooney C, Buckett LK, Klein SK, Hudson K, Monia BP, Zinda M, Blakey DC, Lyne PD, Macleod AR.

Sci Transl Med. 2017 Jun 14;9(394). pii: eaal5253. doi: 10.1126/scitranslmed.aal5253. Erratum in: Sci Transl Med. 2017 Jul 26;9(400):.


Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering.

Gu C, Lamb ML, Johannes JW, Sylvester MA, Eisman MS, Harrison RA, Hu H, Kazmirski S, Mikule K, Peng B, Su N, Wang W, Ye Q, Zheng X, Lyne PD, Scott DA.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4775-4780. doi: 10.1016/j.bmcl.2016.08.030. Epub 2016 Aug 12.


Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.

Dowling JE, Alimzhanov M, Bao L, Chuaqui C, Denz CR, Jenkins E, Larsen NA, Lyne PD, Pontz T, Ye Q, Holdgate GA, Snow L, O'Connell N, Ferguson AD.

ACS Med Chem Lett. 2016 Jan 20;7(3):300-5. doi: 10.1021/acsmedchemlett.5b00452. eCollection 2016 Mar 10.


Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.

Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T, Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B, Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q, Yu Y, Zheng X, Scott DA.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct 27.


Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.

Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA, Peng B, Pontz TW, Rivard-Costa C, Saeh JC, Thakur K, Ye Q, Zhang T, Lyne PD.

ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. doi: 10.1021/ml400197u. eCollection 2013 Aug 8.


AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.

Keeton EK, McEachern K, Dillman KS, Palakurthi S, Cao Y, Grondine MR, Kaur S, Wang S, Chen Y, Wu A, Shen M, Gibbons FD, Lamb ML, Zheng X, Stone RM, Deangelo DJ, Platanias LC, Dakin LA, Chen H, Lyne PD, Huszar D.

Blood. 2014 Feb 6;123(6):905-13. doi: 10.1182/blood-2013-04-495366. Epub 2013 Dec 20.


Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD, MacIntyre T, Mohr PJ, Omer CA, Sjögren T, Thress K, Wang B, Wang H, Yu D, Zhang HJ.

ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. doi: 10.1021/ml300074j. eCollection 2012 Sep 13.


Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.

Dakin LA, Block MH, Chen H, Code E, Dowling JE, Feng X, Ferguson AD, Green I, Hird AW, Howard T, Keeton EK, Lamb ML, Lyne PD, Pollard H, Read J, Wu AJ, Zhang T, Zheng X.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. doi: 10.1016/j.bmcl.2012.05.098. Epub 2012 Jun 6.


Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E.

ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection 2012 Apr 12.


Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.

Lyne PD, Aquila B, Cook DJ, Dakin LA, Ezhuthachan J, Ioannidis S, Pontz T, Su M, Ye Q, Zheng X, Block MH, Cowen S, Deegan TL, Lee JW, Scott DA, Custeau D, Drew L, Poondru S, Shen M, Wu A.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1026-9. doi: 10.1016/j.bmcl.2008.10.053. Epub 2008 Oct 15.


Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.

Scott DA, Aquila BM, Bebernitz GA, Cook DJ, Dakin LA, Deegan TL, Hattersley MM, Ioannidis S, Lyne PD, Omer CA, Ye M, Zheng X.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4794-7. doi: 10.1016/j.bmcl.2008.07.093. Epub 2008 Jul 27.


Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.

Wang T, Lamb ML, Scott DA, Wang H, Block MH, Lyne PD, Lee JW, Davies AM, Zhang HJ, Zhu Y, Gu F, Han Y, Wang B, Mohr PJ, Kaus RJ, Josey JA, Hoffmann E, Thress K, Macintyre T, Wang H, Omer CA, Yu D.

J Med Chem. 2008 Aug 14;51(15):4672-84. doi: 10.1021/jm800343j. Epub 2008 Jul 23.


On evaluating molecular-docking methods for pose prediction and enrichment factors.

Chen H, Lyne PD, Giordanetto F, Lovell T, Li J.

J Chem Inf Model. 2006 Jan-Feb;46(1):401-15. Erratum in: J Chem Inf Model. 2008 Jan;48(1):246.


Lead hopping using SVM and 3D pharmacophore fingerprints.

Saeh JC, Lyne PD, Takasaki BK, Cosgrove DA.

J Chem Inf Model. 2005 Jul-Aug;45(4):1122-33.


Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening.

Lyne PD, Kenny PW, Cosgrove DA, Deng C, Zabludoff S, Wendoloski JJ, Ashwell S.

J Med Chem. 2004 Apr 8;47(8):1962-8.


Structure-based virtual screening: an overview.

Lyne PD.

Drug Discov Today. 2002 Oct 15;7(20):1047-55. Review.


Partial molecular alignment via local structure analysis

Robinson DD, Lyne PD, Richards WG.

J Chem Inf Comput Sci. 2000 Mar;40(2):503-12.


Modelling the catalytic reaction in human aldose reductase.

Várnai P, Richards WG, Lyne PD.

Proteins. 1999 Nov 1;37(2):218-27.


Self-organizing molecular field analysis: a tool for structure-activity studies.

Robinson DD, Winn PJ, Lyne PD, Richards WG.

J Med Chem. 1999 Feb 25;42(4):573-83.


A partial model of the erythropoietin receptor complex.

Caravella JA, Lyne PD, Richards WG.

Proteins. 1996 Mar;24(3):394-401.


Molecular modeling of the GM-CSF and IL-3 receptor complexes.

Lyne PD, Bamborough P, Duncan D, Richards WG.

Protein Sci. 1995 Oct;4(10):2223-33.

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