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Items: 42

1.

Protein phosphatase 2A as a therapeutic target in inflammation and neurodegeneration.

Clark AR, Ohlmeyer M.

Pharmacol Ther. 2019 Jun 1. pii: S0163-7258(19)30099-3. doi: 10.1016/j.pharmthera.2019.05.016. [Epub ahead of print] Review.

2.

Direct activation of PP2A for the treatment of tyrosine kinase inhibitor-resistant lung adenocarcinoma.

Tohmé R, Izadmehr S, Gandhe S, Tabaro G, Vallabhaneni S, Thomas A, Vasireddi N, Dhawan NS, Ma'ayan A, Sharma N, Galsky MD, Ohlmeyer M, Sangodkar J, Narla G.

JCI Insight. 2019 Feb 21;4(4). pii: 125693. doi: 10.1172/jci.insight.125693. eCollection 2019 Feb 21.

3.

Protein Phosphatase 2A Reduces Cigarette Smoke-induced Cathepsin S and Loss of Lung Function.

Doherty DF, Nath S, Poon J, Foronjy RF, Ohlmeyer M, Dabo AJ, Salathe M, Birrell M, Belvisi M, Baumlin N, Kim MD, Weldon S, Taggart C, Geraghty P.

Am J Respir Crit Care Med. 2019 Jul 1;200(1):51-62. doi: 10.1164/rccm.201808-1518OC.

PMID:
30641028
4.

Activation of PP2A and Inhibition of mTOR Synergistically Reduce MYC Signaling and Decrease Tumor Growth in Pancreatic Ductal Adenocarcinoma.

Allen-Petersen BL, Risom T, Feng Z, Wang Z, Jenny ZP, Thoma MC, Pelz KR, Morton JP, Sansom OJ, Lopez CD, Sheppard B, Christensen DJ, Ohlmeyer M, Narla G, Sears RC.

Cancer Res. 2019 Jan 1;79(1):209-219. doi: 10.1158/0008-5472.CAN-18-0717. Epub 2018 Nov 2.

PMID:
30389701
5.

Inhibitor of CBP Histone Acetyltransferase Downregulates p53 Activation and Facilitates Methylation at Lysine 27 on Histone H3.

Vincek AS, Patel J, Jaganathan A, Green A, Pierre-Louis V, Arora V, Rehmann J, Mezei M, Zhou MM, Ohlmeyer M, Mujtaba S.

Molecules. 2018 Aug 2;23(8). pii: E1930. doi: 10.3390/molecules23081930.

6.

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells.

Kauko O, O'Connor CM, Kulesskiy E, Sangodkar J, Aakula A, Izadmehr S, Yetukuri L, Yadav B, Padzik A, Laajala TD, Haapaniemi P, Momeny M, Varila T, Ohlmeyer M, Aittokallio T, Wennerberg K, Narla G, Westermarck J.

Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. doi: 10.1126/scitranslmed.aaq1093.

PMID:
30021885
7.

Chronic Cigarette Smoke Exposure Subdues PP2A Activity by Enhancing Expression of the Oncogene CIP2A.

Nath S, Ohlmeyer M, Salathe MA, Poon J, Baumlin N, Foronjy RF, Geraghty P.

Am J Respir Cell Mol Biol. 2018 Dec;59(6):695-705. doi: 10.1165/rcmb.2018-0173OC.

PMID:
30011381
8.

Small-Molecule Activators of Protein Phosphatase 2A for the Treatment of Castration-Resistant Prostate Cancer.

McClinch K, Avelar RA, Callejas D, Izadmehr S, Wiredja D, Perl A, Sangodkar J, Kastrinsky DB, Schlatzer D, Cooper M, Kiselar J, Stachnik A, Yao S, Hoon D, McQuaid D, Zaware N, Gong Y, Brautigan DL, Plymate SR, Sprenger CCT, Oh WK, Levine AC, Kirschenbaum A, Sfakianos JP, Sears R, DiFeo A, Ioannou Y, Ohlmeyer M, Narla G, Galsky MD.

Cancer Res. 2018 Apr 15;78(8):2065-2080. doi: 10.1158/0008-5472.CAN-17-0123. Epub 2018 Jan 22.

9.

Activation of tumor suppressor protein PP2A inhibits KRAS-driven tumor growth.

Sangodkar J, Perl A, Tohme R, Kiselar J, Kastrinsky DB, Zaware N, Izadmehr S, Mazhar S, Wiredja DD, O'Connor CM, Hoon D, Dhawan NS, Schlatzer D, Yao S, Leonard D, Borczuk AC, Gokulrangan G, Wang L, Svenson E, Farrington CC, Yuan E, Avelar RA, Stachnik A, Smith B, Gidwani V, Giannini HM, McQuaid D, McClinch K, Wang Z, Levine AC, Sears RC, Chen EY, Duan Q, Datt M, Haider S, Ma'ayan A, DiFeo A, Sharma N, Galsky MD, Brautigan DL, Ioannou YA, Xu W, Chance MR, Ohlmeyer M, Narla G.

J Clin Invest. 2017 Jun 1;127(6):2081-2090. doi: 10.1172/JCI89548. Epub 2017 May 15.

10.

BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice.

Cheung K, Lu G, Sharma R, Vincek A, Zhang R, Plotnikov AN, Zhang F, Zhang Q, Ju Y, Hu Y, Zhao L, Han X, Meslamani J, Xu F, Jaganathan A, Shen T, Zhu H, Rusinova E, Zeng L, Zhou J, Yang J, Peng L, Ohlmeyer M, Walsh MJ, Zhang DY, Xiong H, Zhou MM.

Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957. doi: 10.1073/pnas.1615601114. Epub 2017 Mar 6.

11.

Identifying a Small Molecule Blocking Antigen Presentation in Autoimmune Thyroiditis.

Li CW, Menconi F, Osman R, Mezei M, Jacobson EM, Concepcion E, David CS, Kastrinsky DB, Ohlmeyer M, Tomer Y.

J Biol Chem. 2016 Feb 19;291(8):4079-90. doi: 10.1074/jbc.M115.694687. Epub 2015 Dec 24.

12.

Corrigendum to "Reengineered tricyclic anti-cancer agents" [Bioorg. Med. Chem. 23 (2015) 6528-6534].

Kastrinsky DB, Sangodkar J, Zaware N, McClinch K, Farrington CC, Giannini HM, Izadmehr S, Dhawan NS, Narla G, Ohlmeyer M.

Bioorg Med Chem. 2015 Dec 1;23(23):7487. doi: 10.1016/j.bmc.2015.11.002. Epub 2015 Nov 9. No abstract available.

PMID:
28290285
13.

Reengineered tricyclic anti-cancer agents.

Kastrinsky DB, Sangodkar J, Zaware N, Izadmehr S, Dhawan NS, Narla G, Ohlmeyer M.

Bioorg Med Chem. 2015 Oct 1;23(19):6528-34. doi: 10.1016/j.bmc.2015.07.007. Epub 2015 Sep 11.

PMID:
26372073
14.

New small molecule agonists to the thyrotropin receptor.

Latif R, Ali MR, Ma R, David M, Morshed SA, Ohlmeyer M, Felsenfeld DP, Lau Z, Mezei M, Davies TF.

Thyroid. 2015 Jan;25(1):51-62. doi: 10.1089/thy.2014.0119.

15.

Control of embryonic stem cell identity by BRD4-dependent transcriptional elongation of super-enhancer-associated pluripotency genes.

Di Micco R, Fontanals-Cirera B, Low V, Ntziachristos P, Yuen SK, Lovell CD, Dolgalev I, Yonekubo Y, Zhang G, Rusinova E, Gerona-Navarro G, Cañamero M, Ohlmeyer M, Aifantis I, Zhou MM, Tsirigos A, Hernando E.

Cell Rep. 2014 Oct 9;9(1):234-247. doi: 10.1016/j.celrep.2014.08.055. Epub 2014 Sep 26.

16.

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.

Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM.

J Med Chem. 2013 Nov 27;56(22):9251-64. doi: 10.1021/jm401334s. Epub 2013 Nov 11.

17.

BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy.

Segura MF, Fontanals-Cirera B, Gaziel-Sovran A, Guijarro MV, Hanniford D, Zhang G, González-Gomez P, Morante M, Jubierre L, Zhang W, Darvishian F, Ohlmeyer M, Osman I, Zhou MM, Hernando E.

Cancer Res. 2013 Oct 15;73(20):6264-76. doi: 10.1158/0008-5472.CAN-13-0122-T. Epub 2013 Aug 15.

18.

Identification of a novel binding site between HIV type 1 Nef C-terminal flexible loop and AP2 required for Nef-mediated CD4 downregulation.

Jin YJ, Cai CY, Mezei M, Ohlmeyer M, Sanchez R, Burakoff SJ.

AIDS Res Hum Retroviruses. 2013 Apr;29(4):725-31. doi: 10.1089/AID.2012.0286. Epub 2012 Dec 31.

19.

γ-H2AX kinetics as a novel approach to high content screening for small molecule radiosensitizers.

Fu S, Yang Y, Das TK, Yen Y, Zhou BS, Zhou MM, Ohlmeyer M, Ko EC, Cagan R, Rosenstein BS, Chen SH, Kao J.

PLoS One. 2012;7(6):e38465. doi: 10.1371/journal.pone.0038465. Epub 2012 Jun 29. Erratum in: PLoS One. 2012;7(9). doi:10.1371/annotation/0d7595f1-c719-4ed9-bef0-8308f4cac7e3. Tirtha, Das [corrected to Das, Tirtha K].

20.

Targeting the FOXO1/KLF6 axis regulates EGFR signaling and treatment response.

Sangodkar J, Dhawan NS, Melville H, Singh VJ, Yuan E, Rana H, Izadmehr S, Farrington C, Mazhar S, Katz S, Albano T, Arnovitz P, Okrent R, Ohlmeyer M, Galsky M, Burstein D, Zhang D, Politi K, Difeo A, Narla G.

J Clin Invest. 2012 Jul;122(7):2637-51. doi: 10.1172/JCI62058. Epub 2012 Jun 1.

21.

Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition.

Zhang G, Liu R, Zhong Y, Plotnikov AN, Zhang W, Zeng L, Rusinova E, Gerona-Nevarro G, Moshkina N, Joshua J, Chuang PY, Ohlmeyer M, He JC, Zhou MM.

J Biol Chem. 2012 Aug 17;287(34):28840-51. doi: 10.1074/jbc.M112.359505. Epub 2012 May 29. Erratum in: J Biol Chem. 2012 Nov 9;287(46):38956.

22.

Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.

Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26.

PMID:
21723725
23.

Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan R, Craighead M, Desai H, Ho KK, MacSweeney C, Milne R, Richard Morphy J, Neagu I, Ohlmeyer MH, Pick J, Presland J, Riviello C, Zanetakos HA, Zhao J, Webb ML.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3813-7. doi: 10.1016/j.bmcl.2011.04.022. Epub 2011 Apr 13.

PMID:
21596563
24.

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan JH, Craighead M, Desai H, Goan KA, Ho KK, Hulskotte EG, MacSweeney CP, Milne R, Morphy JR, Neagu I, Ohlmeyer MH, Peeters AW, Presland J, Riviello C, Ruigt GS, Thomson FJ, Zanetakos HA, Zhao J, Webb ML.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1871-5. doi: 10.1016/j.bmcl.2010.12.081. Epub 2010 Dec 21.

PMID:
21353540
25.

Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.

Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Maclean J, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, McArthur D, McGregor D, McLuskey H, Neagu I, Neale S, Nisbet LA, Ohlmeyer M, Pham Q, Ratcliffe P, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):892-8. doi: 10.1016/j.bmcl.2010.12.092. Epub 2010 Dec 23.

PMID:
21236666
26.

Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.

Brown AR, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, Elmore MA, Firth A, Goodwin R, Goutcher S, Grant E, Grassie M, Grove SJ, Hamilton NM, Hampson H, Hillier A, Ho KK, Kiczun M, Kingsbury C, Kultgen SG, Littlewood PT, Lusher SJ, Macdonald S, McIntosh L, McIntyre T, Mistry A, Morphy JR, Nimz O, Ohlmeyer M, Pick J, Rankovic Z, Sherborne B, Smith A, Speake M, Spinks G, Thomson F, Watson L, Weston M.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):137-40. doi: 10.1016/j.bmcl.2010.11.054. Epub 2010 Nov 16.

PMID:
21129964
27.

Identification and hit-to-lead optimization of a novel class of CB1 antagonists.

Letourneau JJ, Jokiel P, Olson J, Riviello CM, Ho KK, McAleer L, Yang J, Swanson RN, Baker J, Cowley P, Edwards D, Ward N, Ohlmeyer MH, Webb ML.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5449-53. doi: 10.1016/j.bmcl.2010.07.091. Epub 2010 Jul 25.

PMID:
20719511
28.

Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.

Letourneau JJ, Riviello CM, Li H, Cole AG, Ho KK, Zanetakos HA, Desai H, Zhao J, Auld DS, Napier SE, Thomson FJ, Goan KA, Morphy JR, Ohlmeyer MH, Webb ML.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5394-7. doi: 10.1016/j.bmcl.2010.07.118. Epub 2010 Aug 1.

PMID:
20719508
29.

Novel pyrrolidine heterocycles as CCR1 antagonists.

Merritt JR, James R, Paradkar VM, Zhang C, Liu R, Liu J, Jacob B, Chiriac C, Ohlmeyer MJ, Quadros E, Wines P, Postelnek J, Hicks CM, Chen W, Kimble EF, O'Brien L, White N, Desai H, Appell KC, Webb ML.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5477-9. doi: 10.1016/j.bmcl.2010.07.082. Epub 2010 Jul 24.

PMID:
20708929
30.

Integration of small-molecule discovery in academic biomedical research.

Ohlmeyer M, Zhou MM.

Mt Sinai J Med. 2010 Jul-Aug;77(4):350-7. doi: 10.1002/msj.20197. Review.

31.

Selective functional inhibition of JAK-3 is sufficient for efficacy in collagen-induced arthritis in mice.

Lin TH, Hegen M, Quadros E, Nickerson-Nutter CL, Appell KC, Cole AG, Shao Y, Tam S, Ohlmeyer M, Wang B, Goodwin DG, Kimble EF, Quintero J, Gao M, Symanowicz P, Wrocklage C, Lussier J, Schelling SH, Hewet AG, Xuan D, Krykbaev R, Togias J, Xu X, Harrison R, Mansour T, Collins M, Clark JD, Webb ML, Seidl KJ.

Arthritis Rheum. 2010 Aug;62(8):2283-93. doi: 10.1002/art.27536.

32.

2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.

Cole AG, Bohnstedt AC, Paradkar V, Kingsbury C, Quintero JG, Park H, Lu Y, You M, Neagu I, Diller DJ, Letourneau JJ, Shao Y, James RA, Riviello CM, Ho KK, Lin TH, Wang B, Appell KC, Sills M, Quadros E, Kimble EF, Ohlmeyer MH, Webb ML.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6788-92. doi: 10.1016/j.bmcl.2009.09.080. Epub 2009 Sep 25.

PMID:
19836234
33.

Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.

Ho KK, Beasley JR, Belanger L, Black D, Chan JH, Dunn D, Hu B, Klon A, Kultgen SG, Ohlmeyer M, Parlato SM, Ray PC, Pham Q, Rong Y, Roughton AL, Walker TL, Wright J, Xu K, Xu Y, Zhang L, Webb M.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6027-31. doi: 10.1016/j.bmcl.2009.09.046. Epub 2009 Sep 17.

PMID:
19800787
34.

Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.

de Kruijf P, van Heteren J, Lim HD, Conti PG, van der Lee MM, Bosch L, Ho KK, Auld D, Ohlmeyer M, Smit MJ, Wijkmans JC, Zaman GJ, Smit MJ, Leurs R.

J Pharmacol Exp Ther. 2009 May;329(2):783-90. doi: 10.1124/jpet.108.148387. Epub 2009 Feb 3. Erratum in: J Pharmacol Exp Ther. 2009 Jul;330(1):367.

PMID:
19190236
35.

Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.

Merritt JR, Liu J, Quadros E, Morris ML, Liu R, Zhang R, Jacob B, Postelnek J, Hicks CM, Chen W, Kimble EF, Rogers WL, O'Brien L, White N, Desai H, Bansal S, King G, Ohlmeyer MJ, Appell KC, Webb ML.

J Med Chem. 2009 Mar 12;52(5):1295-301. doi: 10.1021/jm801416q.

PMID:
19183043
36.

Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5).

Letourneau JJ, Liu J, Ohlmeyer MH, Riviello C, Rong Y, Li H, Appell KC, Bansal S, Jacob B, Wong A, Webb ML.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):352-5. doi: 10.1016/j.bmcl.2008.11.074. Epub 2008 Nov 24.

PMID:
19081719
37.

Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors.

Davey DD, Adler M, Arnaiz D, Eagen K, Erickson S, Guilford W, Kenrick M, Morrissey MM, Ohlmeyer M, Pan G, Paradkar VM, Parkinson J, Polokoff M, Saionz K, Santos C, Subramanyam B, Vergona R, Wei RG, Whitlow M, Ye B, Zhao ZS, Devlin JJ, Phillips G.

J Med Chem. 2007 Mar 22;50(6):1146-57. Epub 2007 Feb 23.

PMID:
17315988
38.

Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.

Ho KK, Auld DS, Bohnstedt AC, Conti P, Dokter W, Erickson S, Feng D, Inglese J, Kingsbury C, Kultgen SG, Liu RQ, Masterson CM, Ohlmeyer M, Rong Y, Rooseboom M, Roughton A, Samama P, Smit MJ, Son E, van der Louw J, Vogel G, Webb M, Wijkmans J, You M.

Bioorg Med Chem Lett. 2006 May 15;16(10):2724-8. Epub 2006 Mar 15.

PMID:
16540318
39.

Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry.

McMillan K, Adler M, Auld DS, Baldwin JJ, Blasko E, Browne LJ, Chelsky D, Davey D, Dolle RE, Eagen KA, Erickson S, Feldman RI, Glaser CB, Mallari C, Morrissey MM, Ohlmeyer MH, Pan G, Parkinson JF, Phillips GB, Polokoff MA, Sigal NH, Vergona R, Whitlow M, Young TA, Devlin JJ.

Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1506-11.

40.

Small molecule antagonists of the bradykinin B1 receptor.

Horlick RA, Ohlmeyer MH, Stroke IL, Strohl B, Pan G, Schilling AE, Paradkar V, Quintero JG, You M, Riviello C, Thorn MB, Damaj B, Fitzpatrick VD, Dolle RE, Webb ML, Baldwin JJ, Sigal NH.

Immunopharmacology. 1999 Sep;43(2-3):169-77.

PMID:
10596850
41.

A paradigm for drug discovery employing encoded combinatorial libraries.

Burbaum JJ, Ohlmeyer MH, Reader JC, Henderson I, Dillard LW, Li G, Randle TL, Sigal NH, Chelsky D, Baldwin JJ.

Proc Natl Acad Sci U S A. 1995 Jun 20;92(13):6027-31.

42.

Complex synthetic chemical libraries indexed with molecular tags.

Ohlmeyer MH, Swanson RN, Dillard LW, Reader JC, Asouline G, Kobayashi R, Wigler M, Still WC.

Proc Natl Acad Sci U S A. 1993 Dec 1;90(23):10922-6.

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