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Items: 1 to 50 of 435

1.

Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.

Lee H, Ahn S, Ann J, Ha H, Yoo YD, Kim YH, Hwang JY, Hur KH, Jang CG, Pearce LV, Esch TE, Lewin NE, Blumberg PM, Lee J.

Eur J Med Chem. 2019 Aug 21;182:111634. doi: 10.1016/j.ejmech.2019.111634. [Epub ahead of print]

PMID:
31472474
2.

Combination of a Rapidly Penetrating Agonist and a Slowly Penetrating Antagonist Affords Agonist Action of Limited Duration at the Cellular Level.

Pearce LV, Ann J, Blumberg PM, Lee J.

Biomol Ther (Seoul). 2019 Sep 1;27(5):435-441. doi: 10.4062/biomolther.2019.013.

3.

Munc13 Is a Molecular Target of Bryostatin 1.

Blanco FA, Czikora A, Kedei N, You Y, Mitchell GA, Pany S, Ghosh A, Blumberg PM, Das J.

Biochemistry. 2019 Jul 9;58(27):3016-3030. doi: 10.1021/acs.biochem.9b00427. Epub 2019 Jun 20.

4.

Differential Regulation of Gene Expression in Lung Cancer Cells by Diacyglycerol-Lactones and a Phorbol Ester Via Selective Activation of Protein Kinase C Isozymes.

Cooke M, Casado-Medrano V, Ann J, Lee J, Blumberg PM, Abba MC, Kazanietz MG.

Sci Rep. 2019 Apr 15;9(1):6041. doi: 10.1038/s41598-019-42581-4.

5.

4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands.

Kim C, Ann J, Lee S, Kim E, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem. 2018 Aug 15;26(15):4509-4517. doi: 10.1016/j.bmc.2018.07.040. Epub 2018 Jul 25.

PMID:
30078610
6.

Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.

Kim C, Ann J, Lee S, Sun W, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem Lett. 2018 Aug 1;28(14):2539-2542. doi: 10.1016/j.bmcl.2018.05.043. Epub 2018 May 23.

PMID:
29884534
7.

α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.

Ann J, Czikora A, Saini AS, Zhou X, Mitchell GA, Lewin NE, Peach ML, Blumberg PM, Lee J.

J Med Chem. 2018 Jul 26;61(14):6261-6276. doi: 10.1021/acs.jmedchem.8b00661. Epub 2018 Jul 3.

PMID:
29860841
8.

Characterization of AJH-836, a diacylglycerol-lactone with selectivity for novel PKC isozymes.

Cooke M, Zhou X, Casado-Medrano V, Lopez-Haber C, Baker MJ, Garg R, Ann J, Lee J, Blumberg PM, Kazanietz MG.

J Biol Chem. 2018 Jun 1;293(22):8330-8341. doi: 10.1074/jbc.RA117.000235. Epub 2018 Apr 10.

9.

Deletion of the C26 Methyl Substituent from the Bryostatin Analogue Merle 23 Has Negligible Impact on Its Biological Profile and Potency.

Zhao X, Kedei N, Michalowski A, Lewin NE, Keck GE, Blumberg PM.

Chembiochem. 2018 May 18;19(10):1049-1059. doi: 10.1002/cbic.201700677. Epub 2018 Apr 27.

PMID:
29517836
10.

Synthesis and Biological Evaluation of Fluorescent Bryostatin Analogues.

Cummins TJ, Kedei N, Czikora A, Lewin NE, Kirk S, Petersen ME, McGowan KM, Chen JQ, Luo X, Johnson RC, Ravichandran S, Blumberg PM, Keck GE.

Chembiochem. 2018 Apr 16;19(8):877-889. doi: 10.1002/cbic.201700655. Epub 2018 Mar 25.

PMID:
29424951
11.

Structural determinants of phorbol ester binding activity of the C1a and C1b domains of protein kinase C theta.

Czikora A, Pany S, You Y, Saini AS, Lewin NE, Mitchell GA, Abramovitz A, Kedei N, Blumberg PM, Das J.

Biochim Biophys Acta Biomembr. 2018 May;1860(5):1046-1056. doi: 10.1016/j.bbamem.2018.01.007. Epub 2018 Jan 6.

12.

Critical Role of Trp-588 of Presynaptic Munc13-1 for Ligand Binding and Membrane Translocation.

Das J, Kedei N, Kelsey JS, You Y, Pany S, Mitchell GA, Lewin NE, Blumberg PM.

Biochemistry. 2018 Feb 6;57(5):732-741. doi: 10.1021/acs.biochem.7b00764. Epub 2018 Jan 5.

13.

The C1 domain of Vav3, a novel potential therapeutic target.

Kelsey JS, Géczy T, Kaler CJ, Blumberg PM.

Cell Signal. 2017 Dec;40:133-142. doi: 10.1016/j.cellsig.2017.09.008. Epub 2017 Sep 18.

14.

Importance of the REM (Ras exchange) domain for membrane interactions by RasGRP3.

Czikora A, Kedei N, Kalish H, Blumberg PM.

Biochim Biophys Acta Biomembr. 2017 Dec;1859(12):2350-2360. doi: 10.1016/j.bbamem.2017.09.010. Epub 2017 Sep 11.

15.

Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).

Pearce LV, Ann J, Jung A, Thorat SA, Herold BKA, Habtemichael AD, Blumberg PM, Lee J.

J Med Chem. 2017 Oct 12;60(19):8246-8252. doi: 10.1021/acs.jmedchem.7b00859. Epub 2017 Sep 21.

PMID:
28892388
16.

Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Lee S, Kim C, Ann J, Thorat SA, Kim E, Park J, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4383-4388. doi: 10.1016/j.bmcl.2017.08.020. Epub 2017 Aug 12.

PMID:
28838698
17.

Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands.

Ohashi N, Kobayashi R, Nomura W, Kobayakawa T, Czikora A, Herold BK, Lewin NE, Blumberg PM, Tamamura H.

Bioconjug Chem. 2017 Aug 16;28(8):2135-2144. doi: 10.1021/acs.bioconjchem.7b00299. Epub 2017 Jul 21.

PMID:
28671468
18.

Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKCα, PKCε, and RasGRP.

Elhalem E, Donadío LG, Zhou X, Lewin NE, Garcia LC, Lai CC, Kelley JA, Peach ML, Blumberg PM, Comin MJ.

Bioorg Med Chem. 2017 Jun 15;25(12):2971-2980. doi: 10.1016/j.bmc.2017.03.022. Epub 2017 Mar 10.

19.

t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Lee S, Kang DW, Ryu H, Kim C, Ann J, Lee H, Kim E, Hong S, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem. 2017 Apr 15;25(8):2451-2462. doi: 10.1016/j.bmc.2017.03.004. Epub 2017 Mar 6.

PMID:
28314510
20.

Replacement of the Bryostatin A- and B-Pyran Rings With Phenyl Rings Leads to Loss of High Affinity Binding With PKC.

Petersen ME, Kedei N, Lewin NE, Blumberg PM, Keck GE.

Tetrahedron Lett. 2016 Oct 19;57(42):4749-4753.

21.

Evaluation of Chromane-Based Bryostatin Analogues Prepared via Hydrogen-Mediated C-C Bond Formation: Potency Does Not Confer Bryostatin-like Biology.

Ketcham JM, Volchkov I, Chen TY, Blumberg PM, Kedei N, Lewin NE, Krische MJ.

J Am Chem Soc. 2016 Oct 12;138(40):13415-13423. Epub 2016 Sep 27.

22.

Synthesis and Biological Evaluation of Several Bryostatin Analogues Bearing a Diacylglycerol Lactone C-Ring.

Baumann DO, McGowan KM, Kedei N, Peach ML, Blumberg PM, Keck GE.

J Org Chem. 2016 Sep 2;81(17):7862-83. doi: 10.1021/acs.joc.6b01516. Epub 2016 Aug 23.

PMID:
27494208
23.

Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.

Ann J, Sun W, Zhou X, Jung A, Baek J, Lee S, Kim C, Yoon S, Hong S, Choi S, Turcios NA, Herold BK, Esch TE, Lewin NE, Abramovitz A, Pearce LV, Blumberg PM, Lee J.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3603-7. doi: 10.1016/j.bmcl.2016.06.010. Epub 2016 Jun 7.

PMID:
27317643
24.

To not be hot when TRPV1 is not.

Blumberg PM.

Temperature (Austin). 2015 May 7;2(2):166-7. doi: 10.1080/23328940.2015.1048045. eCollection 2015 Apr-Jun.

25.

Engineering vanilloid-sensitivity into the rat TRPV2 channel.

Zhang F, Hanson SM, Jara-Oseguera A, Krepkiy D, Bae C, Pearce LV, Blumberg PM, Newstead S, Swartz KJ.

Elife. 2016 May 13;5. pii: e16409. doi: 10.7554/eLife.16409.

26.

Structural Basis for the Failure of the C1 Domain of Ras Guanine Nucleotide Releasing Protein 2 (RasGRP2) to Bind Phorbol Ester with High Affinity.

Czikora A, Lundberg DJ, Abramovitz A, Lewin NE, Kedei N, Peach ML, Zhou X, Merritt RC Jr, Craft EA, Braun DC, Blumberg PM.

J Biol Chem. 2016 May 20;291(21):11133-47. doi: 10.1074/jbc.M116.725333. Epub 2016 Mar 28.

27.

Multi-Functional Diarylurea Small Molecule Inhibitors of TRPV1 with Therapeutic Potential for Neuroinflammation.

Feng Z, Pearce LV, Zhang Y, Xing C, Herold BK, Ma S, Hu Z, Turcios NA, Yang P, Tong Q, McCall AK, Blumberg PM, Xie XQ.

AAPS J. 2016 Jul;18(4):898-913. doi: 10.1208/s12248-016-9888-z. Epub 2016 Mar 21.

28.

2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

Ann J, Ki Y, Yoon S, Kim MS, Lee JU, Kim C, Lee S, Jung A, Baek J, Hong S, Choi S, Pearce LV, Esch TE, Turcios NA, Lewin NE, Ogunjirin AE, Herold BK, McCall AK, Blumberg PM, Lee J.

Bioorg Med Chem. 2016 Mar 15;24(6):1231-40. doi: 10.1016/j.bmc.2016.01.051. Epub 2016 Jan 28.

PMID:
26860926
29.

Biological activity of the bryostatin analog Merle 23 on mouse epidermal cells and mouse skin.

Kelsey JS, Cataisson C, Chen J, Herrmann MA, Petersen ME, Baumann DO, McGowan KM, Yuspa SH, Keck GE, Blumberg PM.

Mol Carcinog. 2016 Dec;55(12):2183-2195. doi: 10.1002/mc.22460. Epub 2016 Feb 9.

PMID:
26859836
30.

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem. 2015 Nov 1;23(21):6844-54. doi: 10.1016/j.bmc.2015.10.001. Epub 2015 Oct 9.

PMID:
26474664
31.

α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists.

Tran PT, Kim HS, Ann J, Kim SE, Kim C, Hong M, Hoang VH, Ngo VT, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.

Bioorg Med Chem Lett. 2015 Jun 1;25(11):2326-30. doi: 10.1016/j.bmcl.2015.04.024. Epub 2015 Apr 12.

PMID:
25937016
32.

Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.

Kedei N, Kraft MB, Keck GE, Herald CL, Melody N, Pettit GR, Blumberg PM.

J Nat Prod. 2015 Apr 24;78(4):896-900. doi: 10.1021/acs.jnatprod.5b00094. Epub 2015 Mar 26.

33.

RasGRP3 regulates the migration of glioma cells via interaction with Arp3.

Lee HK, Finniss S, Cazacu S, Xiang C, Poisson LM, Blumberg PM, Brodie C.

Oncotarget. 2015 Jan 30;6(3):1850-64.

34.

Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

Ryu H, Seo S, Lee JY, Ha TH, Lee S, Jung A, Ann J, Kim SE, Yoon S, Hong M, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, Frormann S, Lee J.

Eur J Med Chem. 2015 Mar 26;93:101-8. doi: 10.1016/j.ejmech.2015.02.001. Epub 2015 Feb 2.

PMID:
25659771
35.

Structural insight into tetrameric hTRPV1 from homology modeling, molecular docking, molecular dynamics simulation, virtual screening, and bioassay validations.

Feng Z, Pearce LV, Xu X, Yang X, Yang P, Blumberg PM, Xie XQ.

J Chem Inf Model. 2015 Mar 23;55(3):572-88. doi: 10.1021/ci5007189. Epub 2015 Feb 18.

36.

6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.

Sun W, Kim HS, Lee S, Jung A, Kim SE, Ann J, Yoon S, Choi S, Lee JH, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, Frormann S, Lee J.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):803-6. doi: 10.1016/j.bmcl.2014.12.086. Epub 2015 Jan 5.

PMID:
25597011
37.

Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones).

Ann J, Yoon S, Baek J, Kim DH, Lewin NE, Hill CS, Blumberg PM, Lee J.

Eur J Med Chem. 2015 Jan 27;90:332-41. doi: 10.1016/j.ejmech.2014.11.025. Epub 2014 Nov 13.

PMID:
25437619
38.

Protein kinase Cδ promotes proliferation and induces malignant transformation in skeletal muscle.

Czifra G, Szöllősi A, Nagy Z, Boros M, Juhász I, Kiss A, Erdődi F, Szabó T, Kovács I, Török M, Kovács L, Blumberg PM, Bíró T.

J Cell Mol Med. 2015 Feb;19(2):396-407. doi: 10.1111/jcmm.12452. Epub 2014 Oct 6.

39.

Synthesis of seco-B-ring bryostatin analogue WN-1 via C-C bond-forming hydrogenation: critical contribution of the B-ring in determining bryostatin-like and phorbol 12-myristate 13-acetate-like properties.

Andrews IP, Ketcham JM, Blumberg PM, Kedei N, Lewin NE, Peach ML, Krische MJ.

J Am Chem Soc. 2014 Sep 24;136(38):13209-16. doi: 10.1021/ja507825s. Epub 2014 Sep 10.

40.

Synthesis of a des-B-ring bryostatin analogue leads to an unexpected ring expansion of the bryolactone core.

Kraft MB, Poudel YB, Kedei N, Lewin NE, Peach ML, Blumberg PM, Keck GE.

J Am Chem Soc. 2014 Sep 24;136(38):13202-8. doi: 10.1021/ja5078188. Epub 2014 Sep 10.

41.

2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

Ryu H, Seo S, Kim MS, Kim MY, Kim HS, Ann J, Tran PT, Hoang VH, Byun J, Cui M, Son K, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Koegel BY, Christoph T, Frormann S, Lee J.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):4044-7. doi: 10.1016/j.bmcl.2014.05.072. Epub 2014 Jun 2.

PMID:
25011915
42.

2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

Ryu H, Seo S, Cho SH, Kim HS, Jung A, Kang DW, Son K, Cui M, Hong SH, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Schiene K, Christoph T, Frormann S, Lee J.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):4039-43. doi: 10.1016/j.bmcl.2014.05.074. Epub 2014 Jun 2.

PMID:
24948568
43.

Molecular systems pharmacology: isoelectric focusing signature of protein kinase Cδ provides an integrated measure of its modulation in response to ligands.

Kedei N, Chen JQ, Herrmann MA, Telek A, Goldsmith PK, Petersen ME, Keck GE, Blumberg PM.

J Med Chem. 2014 Jun 26;57(12):5356-69. doi: 10.1021/jm500417b. Epub 2014 Jun 6.

44.

Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.

Garcia LC, Donadío LG, Mann E, Kolusheva S, Kedei N, Lewin NE, Hill CS, Kelsey JS, Yang J, Esch TE, Santos M, Peach ML, Kelley JA, Blumberg PM, Jelinek R, Marquez VE, Comin MJ.

Bioorg Med Chem. 2014 Jun 15;22(12):3123-40. doi: 10.1016/j.bmc.2014.04.024. Epub 2014 Apr 20.

45.

α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.

Kim HS, Jin MK, Kang SU, Lim JO, Tran PT, Hoang VH, Ann J, Ha TH, Pearce LV, Pavlyukovets VA, Blumberg PM, Lee J.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2685-8. doi: 10.1016/j.bmcl.2014.04.054. Epub 2014 Apr 23.

PMID:
24794110
46.

Function of RasGRP3 in the formation and progression of human breast cancer.

Nagy Z, Kovács I, Török M, Tóth D, Vereb G, Buzás K, Juhász I, Blumberg PM, Bíró T, Czifra G.

Mol Cancer. 2014 Apr 29;13:96. doi: 10.1186/1476-4598-13-96.

47.

Charge density influences C1 domain ligand affinity and membrane interactions.

Kelsey JS, Geczy T, Lewin NE, Kedei N, Hill CS, Selezneva JS, Valle CJ, Woo W, Gorshkova I, Blumberg PM.

Chembiochem. 2014 May 26;15(8):1131-1144. doi: 10.1002/cbic.201400041. Epub 2014 Apr 28.

48.

Diacylglycerol lactones targeting the structural features that distinguish the atypical C1 domains of protein kinase C ζ and ι from typical C1 domains.

Pu Y, Kang JH, Sigano DM, Peach ML, Lewin NE, Marquez VE, Blumberg PM.

J Med Chem. 2014 May 8;57(9):3835-44. doi: 10.1021/jm500165n. Epub 2014 Apr 17.

49.

Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands.

Kim MS, Ki Y, Ahn SY, Yoon S, Kim SE, Park HG, Sun W, Son K, Cui M, Choi S, Pearce LV, Esch TE, Deandrea-Lazarus IA, Blumberg PM, Lee J.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):382-5. doi: 10.1016/j.bmcl.2013.10.064. Epub 2013 Nov 6.

PMID:
24321344
50.

TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.

Ha TH, Ryu H, Kim SE, Kim HS, Ann J, Tran PT, Hoang VH, Son K, Cui M, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, Frormann S, Lee J.

Bioorg Med Chem. 2013 Nov 1;21(21):6657-64. doi: 10.1016/j.bmc.2013.08.015. Epub 2013 Aug 13.

PMID:
24035514

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