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Items: 43

1.

Targeting adenosine A2A receptor antagonism for treatment of cancer.

Congreve M, Brown GA, Borodovsky A, Lamb ML.

Expert Opin Drug Discov. 2018 Nov;13(11):997-1003. doi: 10.1080/17460441.2018.1534825. Epub 2018 Oct 18.

PMID:
30336706
2.

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.

PMID:
30297535
3.

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.

PMID:
29559278
4.

Structure-Based Design of Selective Noncovalent CDK12 Inhibitors.

Johannes JW, Denz CR, Su N, Wu A, Impastato AC, Mlynarski S, Varnes JG, Prince DB, Cidado J, Gao N, Haddrick M, Jones NH, Li S, Li X, Liu Y, Nguyen TB, O'Connell N, Rivers E, Robbins DW, Tomlinson R, Yao T, Zhu X, Ferguson AD, Lamb ML, Manchester JI, Guichard S.

ChemMedChem. 2018 Feb 6;13(3):231-235. doi: 10.1002/cmdc.201700695. Epub 2018 Jan 26.

PMID:
29266803
5.

Correction to "Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors".

Johannes JW, Bates S, Beigie C, Belmonte MA, Breen J, Cao S, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Ferguson AD, Habeshian S, Hargreaves D, Joubran C, Kazmirski S, Keefe AD, Lamb ML, Lan H, Li Y, Ma H, Mlynarski S, Packer MJ, Rawlins PB, Robbins DW, Shen H, Sigel EA, Soutter HH, Su N, Troast DM, Wang H, Wickson KF, Wu C, Zhang Y, Zhao Q, Zheng X, Hird AW.

ACS Med Chem Lett. 2017 Oct 18;8(11):1204. doi: 10.1021/acsmedchemlett.7b00397. eCollection 2017 Nov 9.

6.

Deconvoluting Kinase Inhibitor Induced Cardiotoxicity.

Lamore SD, Ahlberg E, Boyer S, Lamb ML, Hortigon-Vinagre MP, Rodriguez V, Smith GL, Sagemark J, Carlsson L, Bates SM, Choy AL, Stålring J, Scott CW, Peters MF.

Toxicol Sci. 2017 Jul 1;158(1):213-226. doi: 10.1093/toxsci/kfx082.

7.

Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.

Johannes JW, Bates S, Beigie C, Belmonte MA, Breen J, Cao S, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Ferguson AD, Habeshian S, Hargreaves D, Joubran C, Kazmirski S, Keefe AD, Lamb ML, Lan H, Li Y, Ma H, Mlynarski S, Packer MJ, Rawlins PB, Robbins DW, Shen H, Sigel EA, Soutter HH, Su N, Troast DM, Wang H, Wickson KF, Wu C, Zhang Y, Zhao Q, Zheng X, Hird AW.

ACS Med Chem Lett. 2016 Dec 27;8(2):239-244. doi: 10.1021/acsmedchemlett.6b00464. eCollection 2017 Feb 9. Erratum in: ACS Med Chem Lett. 2017 Oct 18;8(11):1204.

8.

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain.

Akçay G, Belmonte MA, Aquila B, Chuaqui C, Hird AW, Lamb ML, Rawlins PB, Su N, Tentarelli S, Grimster NP, Su Q.

Nat Chem Biol. 2016 Nov;12(11):931-936. doi: 10.1038/nchembio.2174. Epub 2016 Sep 5.

PMID:
27595327
9.

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.

PMID:
27578247
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.

PMID:
26546219
11.

Evaluating Free Energies of Binding and Conservation of Crystallographic Waters Using SZMAP.

Bayden AS, Moustakas DT, Joseph-McCarthy D, Lamb ML.

J Chem Inf Model. 2015 Aug 24;55(8):1552-65. doi: 10.1021/ci500746d. Epub 2015 Aug 3.

PMID:
26176600
12.

Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.

Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J, Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG, Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T.

ACS Med Chem Lett. 2015 Jan 13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12.

13.

Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening.

Yang B, Lamb ML, Zhang T, Hennessy EJ, Grewal G, Sha L, Zambrowski M, Block MH, Dowling JE, Su N, Wu J, Deegan T, Mikule K, Wang W, Kaspera R, Chuaqui C, Chen H.

J Med Chem. 2014 Dec 11;57(23):9958-70. doi: 10.1021/jm501179r. Epub 2014 Dec 2.

PMID:
25458601
14.

Ensemble-based docking using biased molecular dynamics.

Campbell AJ, Lamb ML, Joseph-McCarthy D.

J Chem Inf Model. 2014 Jul 28;54(7):2127-38. doi: 10.1021/ci400729j. Epub 2014 Jun 18.

PMID:
24881672
15.

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.

16.

Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1.

Wu J, Mikule K, Wang W, Su N, Petteruti P, Gharahdaghi F, Code E, Zhu X, Jacques K, Lai Z, Yang B, Lamb ML, Chuaqui C, Keen N, Chen H.

ACS Chem Biol. 2013 Oct 18;8(10):2201-8. doi: 10.1021/cb400186w. Epub 2013 Aug 16.

PMID:
23895133
17.

Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.

Guan H, Lamb ML, Peng B, Huang S, Degrace N, Read J, Hussain S, Wu J, Rivard C, Alimzhanov M, Bebernitz G, Bell K, Ye M, Zinda M, Ioannidis S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3105-10. doi: 10.1016/j.bmcl.2013.02.111. Epub 2013 Mar 7.

PMID:
23562594
18.

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.

19.

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.

PMID:
22727640
20.

Utilization of HIV voluntary counseling and testing in Vietnam: an evaluation of 5 years of routine program data for national response.

Hong NT, Wolfe MI, Dat TT, McFarland DA, Kamb ML, Thang NT, Thai HN, Del Rio C.

AIDS Educ Prev. 2011 Jun;23(3 Suppl):30-48. doi: 10.1521/aeap.2011.23.3_supp.30. Erratum in: AIDS Educ Prev. 2012 Feb;24(1):89. Lamb, Mary L [corrected to Kamb, Mary L].

PMID:
21689035
21.

In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.

Wang T, Ioannidis S, Almeida L, Block MH, Davies AM, Lamb ML, Scott DA, Su M, Zhang HJ, Alimzhanov M, Bebernitz G, Bell K, Zinda M.

Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61. doi: 10.1016/j.bmcl.2011.03.053. Epub 2011 Mar 21.

PMID:
21493067
22.

Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.

Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E, Rivard C, Green I, Howard T, Pollard H, Read J, Alimzhanov M, Bebernitz G, Bell K, Ye M, Huszar D, Zinda M.

J Med Chem. 2011 Jan 13;54(1):262-76. doi: 10.1021/jm1011319. Epub 2010 Dec 7.

PMID:
21138246
23.

Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.

Ioannidis S, Lamb ML, Almeida L, Guan H, Peng B, Bebernitz G, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1669-73. doi: 10.1016/j.bmcl.2010.01.091. Epub 2010 Jan 25.

PMID:
20144546
24.

Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.

Ioannidis S, Lamb ML, Davies AM, Almeida L, Su M, Bebernitz G, Ye M, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6524-8. doi: 10.1016/j.bmcl.2009.10.054. Epub 2009 Oct 24.

PMID:
19857966
25.

Trk kinase inhibitors as new treatments for cancer and pain.

Wang T, Yu D, Lamb ML.

Expert Opin Ther Pat. 2009 Mar;19(3):305-19. doi: 10.1517/13543770902721261. Review.

PMID:
19441906
26.

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.

PMID:
18646745
27.
28.

SitePrint: three-dimensional pharmacophore descriptors derived from protein binding sites for family based active site analysis, classification, and drug design.

Arnold JR, Burdick KW, Pegg SC, Toba S, Lamb ML, Kuntz ID.

J Chem Inf Comput Sci. 2004 Nov-Dec;44(6):2190-8.

PMID:
15554689
29.

Design of a gene family screening library targeting G-protein coupled receptors.

Lamb ML, Bradley EK, Beaton G, Bondy SS, Castellino AJ, Gibbons PA, Suto MJ, Grootenhuis PD.

J Mol Graph Model. 2004 Sep;23(1):15-21.

PMID:
15331050
30.

Performance of 3D-database molecular docking studies into homology models.

Oshiro C, Bradley EK, Eksterowicz J, Evensen E, Lamb ML, Lanctot JK, Putta S, Stanton R, Grootenhuis PD.

J Med Chem. 2004 Jan 29;47(3):764-7.

PMID:
14736258
31.

A computational ensemble pharmacophore model for identifying substrates of P-glycoprotein.

Penzotti JE, Lamb ML, Evensen E, Grootenhuis PD.

J Med Chem. 2002 Apr 25;45(9):1737-40.

PMID:
11960484
32.

Design, docking, and evaluation of multiple libraries against multiple targets.

Lamb ML, Burdick KW, Toba S, Young MM, Skillman AG, Zou X, Arnold JR, Kuntz ID.

Proteins. 2001 Feb 15;42(3):296-318.

PMID:
11151003
33.
34.

Estimation of the binding affinities of FKBP12 inhibitors using a linear response method.

Lamb ML, Tirado-Rives J, Jorgensen WL.

Bioorg Med Chem. 1999 May;7(5):851-60.

PMID:
10400338
35.

Prognostic significance of K-ras codon 12 mutations in patients with resected stage I and II non-small-cell lung cancer.

Graziano SL, Gamble GP, Newman NB, Abbott LZ, Rooney M, Mookherjee S, Lamb ML, Kohman LJ, Poiesz BJ.

J Clin Oncol. 1999 Feb;17(2):668-75.

PMID:
10080613
36.

Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.

Smith RH Jr, Jorgensen WL, Tirado-Rives J, Lamb ML, Janssen PA, Michejda CJ, Kroeger Smith MB.

J Med Chem. 1998 Dec 17;41(26):5272-86.

PMID:
9857095
37.

Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.

Lamb ML, Jorgensen WL.

J Med Chem. 1998 Oct 8;41(21):3928-39.

PMID:
9767630
38.

Computational approaches to molecular recognition.

Lamb ML, Jorgensen WL.

Curr Opin Chem Biol. 1997 Dec;1(4):449-57. Review.

PMID:
9667895
39.

Pseudocleavage is dispensable for polarity and development in C. elegans embryos.

Rose LS, Lamb ML, Hird SN, Kemphues KJ.

Dev Biol. 1995 Apr;168(2):479-89.

40.

Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.

Ward JS, Merritt L, Klimkowski VJ, Lamb ML, Mitch CH, Bymaster FP, Sawyer B, Shannon HE, Olesen PH, Honoré T, et al.

J Med Chem. 1992 Oct 30;35(22):4011-9.

PMID:
1433209
41.

Detection and follow-up of moderate and severe hypertensive subjects in the Australia community.

Hunyor SN, Bauer GE, Abernethy JD, Baker JL, Bullen MU, Lamb ML, Stewart MR.

Med J Aust. 1977 Apr 9;1(15):517-20.

PMID:
875785
42.

Report on progress in the Australian National Blood Pressure Study (NBPS).

Abernethy JD, Baker JL, Bullen MU, Lamb ML, Stewart MR.

Clin Sci Mol Med Suppl. 1976 Dec;3:645s-647s.

PMID:
1071698
43.

Borderline hypertension discovered during screening: effect of twelve months' treatment.

McCall MG, Lamb ML, Stenhouse NS.

Drugs. 1976;11 SUPPL 1:6-11.

PMID:
776582

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