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Our Science – Blumberg Website

Peter M. Blumberg, Ph.D.

Selected Publications

1)  Kedei N, Chen J, Herrmann MA, Telek A, Goldsmith PK, Petersen ME, Keck GE, Blumberg PM.
Molecular Systems Pharmacology: Isoelectric Focusing Signature of Protein Kinase Cd Provides an Integrated Measure of Its Modulation in Response to Ligands.
J. Med. Chem. [Epub ahead of print], 2014.
[Journal]
2)  Kedei N, Telek A, Michalowski AM, Kraft MB, Li W, Poudel YB, Rudra A, Petersen ME, Keck GE, Blumberg PM.
Comparison of transcriptional response to phorbol ester, bryostatin 1, and bryostatin analogs in LNCaP and U937 cancer cell lines provides insight into their differential mechanism of action.
Biochem. Pharmacol. 85: 313-24, 2013.
[Journal]
3)  Geczy T, Peach ML, El Kazzouli S, Sigano DM, Kang J, Valle CJ, Selezneva J, Woo W, Kedei N, Lewin NE, Garfield SH, Lim L, Mannan P, Marquez VE, Blumberg PM.
Molecular basis for failure of the "atypical" C1 domain of Vav1 to bind diacylglycerol / phorbol ester.
J. Biol. Chem. 287: 13137-58, 2012.
[Journal]
4)  Yang D, Tao J, Li L, Kedei N, Tóth ZE, Czap A, Velasquez JF, Mihova D, Michalowski AM, Yuspa SH, Blumberg PM.
RasGRP3, a Ras activator, contributes to signaling and the tumorigenic phenotype in human melanoma.
Oncogene. 30(45): 4590-4600, 2011.
[Journal]
5)  Keck GE, Kraft MB, Truong AP, Li W, Sanchez CC, Kedei N, Lewin NE, Blumberg PM.
Convergent assembly of highly potent analogues of bryostatin 1 via pyran annulation: bryostatin look-alikes that mimic phorbol ester function.
J. Am. Chem. Soc. 130: 6660-1, 2008.
[Journal]
6)  Kim HS, Jin MK, Kang SU, Lim JO, Tran PT, Hoang VH, Ann J, Ha TH, Pearce LV, Pavlyukovets VA, Blumberg PM, Lee J.
a-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.
Bioorg. Med. Chem. Lett. 24: 2685-8, 2014.
[Journal]
7)  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.
Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands.
Bioorg. Med. Chem. Lett. 24: 382-5, 2014.
[Journal]
8)  Kelsey JS, Geczy T, Lewin NE, Kedei N, Hill CS, Selezneva JS, Valle CJ, Woo W, Gorshkova I, Blumberg PM.
Charge density influences c1 domain ligand affinity and membrane interactions.
Chembiochem. 15: 1131-44, 2014.
[Journal]
9)  Pu Y, Kang J, Sigano DM, Peach ML, Lewin NE, Marquez VE, Blumberg PM.
Diacylglycerol Lactones Targeting the Structural Features That Distinguish the Atypical C1 Domains of Protein Kinase C ? and ? from Typical C1 Domains.
J. Med. Chem. [Epub ahead of print], 2014.
[Journal]
10)  Nagy Z, Kovács I, Török M, Tóth D, Vereb G, Buzás K, Juhász I, Blumberg PM, Bíró T, Czifra G.
Function of RasGRP3 in the formation and progression of human breast cancer.
Mol. Cancer. 13: 96, 2014.
[Journal]
11)  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.
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
Bioorg. Med. Chem. 22: 3123-40, 2014.
[Journal]
12)  Thorat SA, Kang DW, Ryu H, Kim MS, Kim HS, Ann J, Ha T, Kim SE, Son K, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, Lee J.
2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: structure activity relationships of the 2-oxy pyridine C-region.
Eur J Med Chem. 64: 589-602, 2013.
[Journal]
13)  Kortum RL, Rouquette-Jazdanian AK, Miyaji M, Merrill RK, Markegard E, Pinski JM, Wesselink A, Nath NN, Alexander CP, Li W, Kedei N, Roose JP, Blumberg PM, Samelson LE, Sommers CL.
A phospholipase C-?1-independent, RasGRP1-ERK-dependent pathway drives lymphoproliferative disease in linker for activation of T cells-Y136F mutant mice.
J. Immunol. 190: 147-58, 2013.
[Journal]
14)  Chen J, R Heldman M, Herrmann MA, Kedei N, Woo W, Blumberg PM, Goldsmith PK.
Absolute quantitation of endogenous proteins with precision and accuracy using a capillary western system.
Anal. Biochem. 442: 97-103, 2013.
[Journal]
15)  Kedei N, Lewin NE, Géczy T, Selezneva J, Braun DC, Chen J, Herrmann MA, Heldman MR, Lim L, Mannan P, Garfield SH, Poudel YB, Cummins TJ, Rudra A, Blumberg PM, Keck GE.
Biological Profile of the Less Lipophilic and Synthetically More Accessible Bryostatin 7 Closely Resembles That of Bryostatin 1.
ACS Chem. Biol. 8(4): 767-777, 2013.
[Journal]
16)  Rahman GM, Shanker S, Lewin NE, Kedei N, Hill CS, Prasad BV, Blumberg PM, Das J.
Identification of the activator-binding residues in the second cysteine-rich regulatory domain of protein kinase C? (PKC?).
Biochem. J. 451: 33-44, 2013.
[Journal]
17)  van Veghel D, Cleynhens J, Pearce LV, Deandrea-Lazarus IA, Blumberg PM, Van Laere K, Verbruggen A, Bormans G.
New Transient Receptor Potential Vanilloid Subfamily Member 1 Positron Emission Tomography Radioligands: Synthesis, Radiolabeling, and Preclinical Evaluation.
ACS Chem Neurosci. 4(4): 624-634, 2013.
[Journal]
18)  Song X, Lopez-Campistrous A, Sun L, Dower NA, Kedei N, Yang J, Kelsey JS, Lewin NE, Esch TE, Blumberg PM, Stone JC.
RasGRPs are targets of the anti-cancer agent ingenol-3-angelate.
PLoS ONE. 8: e72331, 2013.
[Journal]
19)  van Veghel D, Cleynhens J, Pearce LV, Blumberg PM, Van Laere K, Verbruggen A, Bormans G.
Synthesis and biological evaluation of [11C]SB366791: a new PET-radioligand for in vivo imaging of the TRPV1 receptor.
Nucl. Med. Biol. 40: 141-7, 2013.
[Journal]
20)  Lim KS, Lee H, Kim SE, Ha TH, Ann J, Son K, Choi S, Sun W, Pearce LV, DeAndrea-Lazarus IA, Blumberg PM, Lee J.
The carbonate analogues of 5"-halogenated resiniferatoxin as TRPV1 ligands.
Eur J Med Chem. 68: 233-43, 2013.
[Journal]
21)  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.
TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.
Bioorg. Med. Chem. 21: 6657-64, 2013.
[Journal]
22)  Kim MS, Ryu H, Kang DW, Cho SH, Seo S, Park YS, Kim MY, Kwak EJ, Kim YS, Bhondwe RS, Kim HS, Park SG, Son K, Choi S, DeAndrea-Lazarus IA, Pearce LV, Blumberg PM, Frank R, Bahrenberg G, Stockhausen H, Kögel BY, Schiene K, Christoph T, Lee J.
2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.
J. Med. Chem. 55: 8392-408, 2012.
[Journal]
23)  Sun W, Liu K, Ryu H, Kang DW, Kim YS, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Kim HS, Pearce LV, Pavlyukovets VA, Tran R, Morgan MA, Lazar J, Ryder CB, Toth A, Blumberg PM, Lee J.
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions.
Bioorg. Med. Chem. 20: 1310-8, 2012.
[Journal]
24)  Kim YS, Kil MJ, Kang SU, Ryu H, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Sun W, Liu K, Lee JH, Choi S, Pearce LV, Pavlyukovets VA, Morgan MA, Tran R, Lazar J, Blumberg PM, Lee J.
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Bioorg. Med. Chem. 20: 215-24, 2012.
[Journal]
25)  Keck GE, Poudel YB, Rudra A, Stephens JC, Kedei N, Lewin NE, Blumberg PM.
Role of the C(8)gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
Bioorg Med Chem Lett. 22(12): 4084-4088, 2012.
[Journal]
26)  Bhondwe RS, Kang DW, Kim MS, Kim HS, Park S, Son K, Choi S, Lang Kuhs KA, Pavlyukovets VA, Pearce LV, Blumberg PM, Lee J.
Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism.
Bioorg. Med. Chem. Lett. 22: 3656-60, 2012.
[Journal]
27)  Cho Y, Kim MS, Kim HS, Ann J, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Blumberg PM, Lee J.
The SAR analysis of TRPV1 agonists with the alpha-methylated B-region.
Bioorg. Med. Chem. Lett. 22(16): 5237-5231, 2012.
[Journal]
28)  Ohashi N, Nomura W, Narumi T, Lewin NE, Itotani K, Blumberg PM, Tamamura H.
Fluorescent-responsive synthetic C1b domains of protein kinase C delta as reporters of specific high-affinity ligand binding.
Bioconjug. Chem. 22: 82-7, 2011.
[Journal]
29)  Gal N, Kolusheva S, Kedei N, Telek A, Naeem TA, Lewin NE, Lim L, Mannan P, Garfield SH, El Kazzouli S, Sigano DM, Marquez VE, Blumberg PM, Jelinek R.
N-methyl-substituted fluorescent DAG-indololactone isomers exhibit dramatic differences in membrane interactions and biological activity.
Chembiochem. 12: 2331-40, 2011.
[Journal]
30)  Lim KS, Kang DW, Kim YS, Kim MS, Park SG, Choi S, Pearce LV, Blumberg PM, Lee J.
Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands.
Bioorg. Med. Chem. Lett. 21: 299-302, 2011.
[Journal]
31)  Kedei N, Lubart E, Lewin NE, Telek A, Lim L, Mannan P, Garfield SH, Kraft MB, Keck GE, Kolusheva S, Jelinek R, Blumberg PM.
Some Phorbol Esters Might Partially Resemble Bryostatin 1 in their Actions on LNCaP Prostate Cancer Cells and U937 Leukemia Cells.
Chembiochem. 12: 1242-51, 2011.
[Journal]
32)  Lee JH, Lee Y, Ryu H, Kang DW, Lee J, Lazar J, Pearce LV, Pavlyukovets VA, Blumberg PM, Choi S.
Structural insights into transient receptor potential vanilloid type 1 (TRPV1) from homology modeling, flexible docking, and mutational studies.
J. Comput. Aided Mol. Des. 25: 317-27, 2011.
[Journal]
33)  Nomura W, Narumi T, Ohashi N, Serizawa Y, Lewin NE, Blumberg PM, Furuta T, Tamamura H.
Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C.
Chembiochem. 12: 535-9, 2011.
[Journal]
34)  Kedei N, Telek A, Czap A, Lubart ES, Czifra G, Yang D, Chen J, Morrison T, Goldsmith PK, Lim L, Mannan P, Garfield SH, Kraft MB, Li W, Keck GE, Blumberg PM.
The synthetic bryostatin analog Merle 23 dissects distinct mechanisms of bryostatin activity in the LNCaP human prostate cancer cell line.
Biochem. Pharmacol. 81: 1296-308, 2011.
[Journal]
35)  Blumberg PM, Pearce LV, Lee J.
TRPV1 Activation is Not an All-or-None Event: TRPV1 Partial Agonism/Antagonism and its Regulatory Modulation.
Curr Top Med Chem. 11: 2151-2158, 2011.
[Journal]
36)  Blumberg PM, Kedei N, Lewin NE, Yang D, Tao J, Telek A, Geczy T.
Kazanietz MG, eds.
PKC enaymes - receptors for diacylglycerol and phorbol esters. In: Protein Kinase C in Cancer Signaling and Therapy.
New York: Springer Publishing Co; 2010. p. 25-53 [Book Chapter]
37)  Kang DW, Kim YS, Lim KS, Kim MS, Pearce LV, Pavlyukovets VA, Tao AK, Lang-Kuhs KA, Blumberg PM, Lee J.
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorg. Med. Chem. 18: 8092-105, 2010.
[Journal]
38)  Raifman O, Kolusheva S, Comin MJ, Kedei N, Lewin NE, Blumberg PM, Marquez VE, Jelinek R.
Membrane anchoring of diacylglycerol lactones substituted with rigid hydrophobic acyl domains correlates with biological activities.
FEBS J. 277: 233-43, 2010.
[Journal]
39)  Raifman O, Kolusheva S, El Kazzouli S, Sigano DM, Kedei N, Lewin NE, Lopez-Nicolas R, Ortiz-Espin A, Gomez-Fernandez JC, Blumberg PM, Marquez VE, Corbalan-Garcia S, Jelinek R.
Membrane-Surface Anchoring of Charged Diacylglycerol-Lactones Correlates with Biological Activities.
Chembiochem. 11: 2003-2009, 2010.
[Journal]
40)  Keck GE, Poudel YB, Rudra A, Stephens JC, Kedei N, Lewin NE, Peach ML, Blumberg PM.
Molecular Modeling, Total Synthesis, and Biological Evaluations of C9-Deoxy Bryostatin 1.
Angew Chem Int Ed Engl. 49(27): 4580-4584, 2010.
[Journal]
41)  Kang JH, Kim Y, Won SH, Park SK, Lee CW, Kim HM, Lewin NE, Perry NA, Pearce LV, Lundberg DJ, Surawski RJ, Blumberg PM, Lee J.
Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents.
Bioorg. Med. Chem. Lett. 20: 1008-12, 2010.
[Journal]
42)  Yang D, Kedei N, Li L, Tao J, Velasquez JF, Michalowski AM, Tóth BI, Marincsák R, Varga A, Bíró T, Yuspa SH, Blumberg PM.
RasGRP3 contributes to formation and maintenance of the prostate cancer phenotype.
Cancer Res. 70: 7905-17, 2010.
[Journal]
43)  Stang SL, Lopez-Campistrous A, Song X, Dower NA, Blumberg PM, Wender PA, Stone JC.
A proapoptotic signaling pathway involving RasGRP, Erk, and Bim in B cells.
Exp. Hematol. 37: 122-134, 2009.
[Journal]
44)  Tóth A, Blumberg PM, Boczán J.
Anandamide and the vanilloid receptor (TRPV1).
Vitam. Horm. 81: 389-419, 2009.
[Journal]
45)  Sosa MS, Lewin NE, Choi SH, Blumberg PM, Kazanietz MG.
Biochemical characterization of hyperactive beta2-chimaerin mutants revealed an enhanced exposure of C1 and Rac-GAP domains.
Biochemistry. 48: 8171-8, 2009.
[Journal]
46)  Pu Y, Garfield SH, Kedei N, Blumberg PM.
Characterization of the differential roles of the twin C1a and C1b domains of protein kinase C-delta.
J. Biol. Chem. 284: 1302-12, 2009.
[Journal]
47)  Comin MJ, Czifra G, Kedei N, Telek A, Lewin NE, Kolusheva S, Velasquez JF, Kobylarz R, Jelinek R, Blumberg PM, Marquez VE.
Conformationally Constrained Analogues of Diacylglycerol (DAG). 31. Modulation of the Biological Properties of Diacylgycerol Lactones (DAG-lactones) Containing Rigid-Rod Acyl Groups Separated from the Core Lactone by Spacer Units of Different Lengths.
J. Med. Chem. 52: 3274-3283, 2009.
[Journal]
48)  Choi HK, Choi S, Lee Y, Kang DW, Ryu H, Maeng HJ, Chung SJ, Pavlyukovets VA, Pearce LV, Toth A, Tran R, Wang Y, Morgan MA, Blumberg PM, Lee J.
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Bioorg. Med. Chem. 17: 690-8, 2009.
[Journal]
49)  Szegedi A, Páyer E, Czifra G, Tóth BI, Schmidt E, Kovács L, Blumberg PM, Bíró T.
Protein kinase C isoenzymes differentially regulate the differentiation-dependent expression of adhesion molecules in human epidermal keratinocytes.
Exp. Dermatol. 18(2): 122-129, 2009.
[Journal]
50)  Lazar J, Gharat L, Khairathkar-Joshi N, Blumberg P, Szallasi A.
Screening TRPV1 antagonists for the treatment of pain - lessons learned over a dodecade.
Exp Opin Drug Discovery. 4: 159-180, 2009.
[Journal]
51)  Kozikowski AP, Chen Y, Subhasish T, Lewin NE, Blumberg PM, Zhong Z, D'Annibale MA, Wang W, Shen Y, Langley B.
Searching for Disease Modifiers-PKC Activation and HDAC Inhibition-A Dual Drug Approach to Alzheimer's Disease that Decreases Abeta Production while Blocking Oxidative Stress.
ChemMedChem. 4: 1095-1105, 2009.
[Journal]
52)  Keck GE, Poudel YB, Welch DS, Kraft MB, Truong AP, Stephens JC, Kedei N, Lewin NE, Blumberg PM.
Substitution on the A-ring confers to bryopyran analogues the unique biological activity characteristic of bryostatins and distinct from that of the phorbol esters.
Org. Lett. 11: 593-6, 2009.
[Journal]
53)  Ohashi N, Nomura W, Kato M, Narumi T, Lewin NE, Blumberg PM, Tamamura H.
Synthesis of protein kinase Cdelta C1b domain by native chemical ligation methodology and characterization of its folding and ligand binding.
J. Pept. Sci. 15: 642-646, 2009.
[Journal]
54)  Keck GE, Li W, Kraft MB, Kedei N, Lewin NE, Blumberg PM.
The Bryostatin 1 A-Ring Acetate is Not the Critical Determinant for Antagonism of Phorbol Ester-Induced Biological Responses.
Org. Lett. 11: 2277-2280, 2009.
[Journal]
55)  Gonczi M, Telek A, Czifra G, Balogh A, Blumberg PM, Biro T, Csernoch L.
Altered calcium handling following the recombinant overexpression of protein kinase C isoforms in HaCaT cells.
Exp. Dermatol. 17: 584-91, 2008.
[Journal]
56)  Choi SH, Czifra G, Kedei N, Lewin NE, Lazar J, Pu Y, Marquez VE, Blumberg PM.
Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.
J. Biol. Chem. 283: 10543-9, 2008.
[Journal]
57)  Duan D, Sigano DM, Kelley JA, Lai CC, Lewin NE, Kedei N, Peach ML, Lee J, Abeyweera TP, Rotenberg SA, Kim H, Kim YH, El Kazzouli S, Chung JU, Young HA, Young MR, Baker A, Colburn NH, Haimovitz-Friedman A, Truman JP, Parrish DA, Deschamps JR, Perry NA, Surawski RJ, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities.
J. Med. Chem. 51: 5198-220, 2008.
[Journal]
58)  El Kazzouli S, Lewin NE, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.
J. Med. Chem. 51: 5371-86, 2008.
[Journal]
59)  Lim J, Jin M, Ryu H, Kang DW, Lee J, Pearce LV, Tran R, Toth A, Blumberg PM.
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.
Eur J Med Chem. 44: 322-31, 2008.
[Journal]
60)  Pearce LV, Toth A, Ryu H, Kang DW, Choi HK, Jin MK, Lee J, Blumberg PM.
Differential modulation of agonist and antagonist structure activity relations for rat TRPV1 by cyclosporin A and other protein phosphatase inhibitors.
Naunyn Schmiedebergs Arch. Pharmacol. 377: 149-57, 2008.
[Journal]
61)  Zhu H, Yang Y, Zhang H, Han Y, Li Y, Zhang Y, Yin D, He Q, Zhao Z, Blumberg PM, Han J, Wang Y.
Interaction between protein kinase D1 and transient receptor potential V1 in primary sensory neurons is involved in heat hypersensitivity.
Pain. 137: 574-88, 2008.
[Journal]
62)  Lomonaco SL, Kahana S, Blass M, Brody Y, Okhrimenko H, Xiang C, Finniss S, Blumberg PM, Lee HK, Brodie C.
Phosphorylation of protein kinase Cdelta on distinct tyrosine residues induces sustained activation of Erk1/2 via down-regulation of MKP-1: role in the apoptotic effect of etoposide.
J. Biol. Chem. 283: 17731-9, 2008.
[Journal]
63)  Philosof-Mazor L, Volinsky R, Comin MJ, Lewin NE, Kedei N, Blumberg PM, Marquez VE, Jelinek R.
Self-Assembly and Lipid Interactions of Diacylglycerol Lactone Derivatives Studied at the Air/Water Interface.
Langmuir. 24: 11043-52, 2008.
[Journal]
64)  Ryu H, Jin MK, Kim SY, Choi HK, Kang SU, Kang DW, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Tran R, Toth A, Lundberg DJ, Blumberg PM.
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
J. Med. Chem. 51: 57-67, 2008.
[Journal]
65)  Blumberg PM, Kedei N, Lewin NE, Yang D, Czifra G, Pu Y, Peach ML, Marquez VE.
Wealth of opportunity - the C1 domain as a target for drug development.
Curr Drug Targets. 9: 641-52, 2008.
[Journal]
66)  Chung JU, Kim SY, Lim JO, Choi HK, Kang SU, Yoon HS, Ryu H, Kang DW, Lee J, Kang B, Choi S, Toth A, Pearce LV, Pavlyukovets VA, Lundberg DJ, Blumberg PM.
alpha-Substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Bioorg. Med. Chem. 15: 6043-53, 2007.
[Journal]
67)  Tang L, Chen Y, Chen Z, Blumberg PM, Kozikowski AP, Wang ZJ.
Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor.
J. Pharmacol. Exp. Ther. 321: 791-8, 2007.
[Journal]
68)  Malolanarasimhan K, Kedei N, Sigano DM, Kelley JA, Lai CC, Lewin NE, Surawski RJ, Pavlyukovets VA, Garfield SH, Wincovitch S, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
J. Med. Chem. 50: 962-78, 2007.
[Journal]
69)  Choi Y, Pu Y, Peach ML, Kang JH, Lewin NE, Sigano DM, Garfield SH, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.
J. Med. Chem. 50: 3465-81, 2007.
[Journal]
70)  Kang DW, Ryu H, Lee J, Lang KA, Pavlyukovets VA, Pearce LV, Ikeda T, Lazar J, Blumberg PM.
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorg. Med. Chem. Lett. 17: 214-9, 2007.
[Journal]
71)  Blumberg PM.
Lighting a backfire to quench the blaze: a combined drug approach targeting the vanilloid receptor TRPV1.
Mol. Interv. 7: 310-2, 2007.
[Journal]
72)  Szallasi A, Blumberg P.
Liedtke W, Heller S, eds.
Complex regulation of TRPV1 by vanilloids. In: TRP ion channel function in sensory transduction and cellular signaling cascades.
Boca Raton, FL: CRC Press, Inc.; 2006. p. 85-104 [Book Chapter]
73)  Lee J, Lee JH, Kim SY, Perry NA, Lewin NE, Ayres JA, Blumberg PM.
2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands.
Bioorg. Med. Chem. 14: 2022-31, 2006.
[Journal]
74)  Lee J, Kang JH, Han KC, Kim Y, Kim SY, Youn HS, Mook-Jung I, Kim H, Lo Han JH, Ha HJ, Kim YH, Marquez VE, Lewin NE, Pearce LV, Lundberg DJ, Blumberg PM.
Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.
J. Med. Chem. 49: 2028-36, 2006.
[Journal]
75)  Kang JH, Benzaria S, Sigano DM, Lewin NE, Pu Y, Peach ML, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.
J. Med. Chem. 49: 3185-203, 2006.
[Journal]
76)  Choi SH, Hyman T, Blumberg PM.
Differential effect of bryostatin 1 and phorbol 12-myristate 13-acetate on HOP-92 cell proliferation is mediated by down-regulation of protein kinase Cdelta.
Cancer Res. 66: 7261-9, 2006.
[Journal]
77)  Pu Y, Peach ML, Garfield SH, Wincovitch S, Marquez VE, Blumberg PM.
Effects on ligand interaction and membrane translocation of the positively charged arginine residues situated along the C1 domain binding cleft in the atypical protein kinase C isoforms.
J. Biol. Chem. 281: 33773-88, 2006.
[Journal]
78)  Czifra G, Toth IB, Marincsak R, Juhasz I, Kovacs I, Acs P, Kovacs L, Blumberg PM, Biro T.
Insulin-like growth factor-I-coupled mitogenic signaling in primary cultured human skeletal muscle cells and in C2C12 myoblasts. A central role of protein kinase Cdelta.
Cell Signaling. 18: 1461-1472, 2006.
[Journal]
79)  Lazar J, Braun DC, Tóth A, Wang Y, Pearce LV, Pavlyukovets VA, Blumberg PM, Garfield SH, Wincovitch S, Choi HK, Lee J.
Kinetics of penetration influence the apparent potency of vanilloids on TRPV1.
Mol. Pharmacol. 69: 1166-73, 2006.
[Journal]
80)  Lizanecz E, Bagi Z, Paztor ET, Papp Z, Edes I, Kedei N, Blumberg PM, Toth A.
Phosphorylation-dependent desensitization by anandamide of vanilloid receptor-1 (TRPV1) function in rat skeletal muscle arterioles and in Chinese hamster ovary cells expressing TRPV1.
Mol. Pharmacol. 69: 1015-23, 2006.
[Journal]
81)  Mach UR, Lewin NE, Blumberg PM, Kozikowski AP.
Synthesis and Pharmacological Evaluation of 8- and 9-Substituted Benzolactam-V8 Derivatives as Potent Ligands for Protein Kinase C, a Therapeutic Target for Alzheimer's Disease.
ChemMedChem. 1: 307-314, 2006.
[Journal]
82)  Blumberg P, Braun D, Kedei N, Lazar J, Pavlyukovets V, Pearce L.
Malmberg A, Bley K, eds.
Insights into TRPV1 pharmacology provided by non-capsaicin ligands. In: Turning up the Heat on Pain: TRPV1 Receptors in Pain and Inflammation.
New York: Birkhauser Verlag; 2005. p. 55-69 [Book Chapter]
83)  Pu Y, Perry NA, Yang D, Lewin NE, Kedei N, Braun DC, Choi SH, Blumberg PM, Garfield SH, Stone JC, Duan D, Marquez VE.
A novel diacylglycerol-lactone shows marked selectivity in vitro among C1 domains of protein kinase C (PKC) isoforms alpha and delta as well as selectivity for RasGRP compared with PKCalpha.
J Biol Chem. 280: 27329-38, 2005.
[Journal]
84)  Braun DC, Garfield SH, Blumberg PM.
Analysis by fluorescence resonance energy transfer of the interaction between ligands and protein kinase Cdelta in the intact cell.
J Biol Chem. 280: 8164-71, 2005.
[Journal]
85)  Lee J, Kang SU, Kil MJ, Shin M, Lim JO, Choi HK, Jin MK, Kim SY, Kim SE, Lee YS, Min KH, Kim YH, Ha HJ, Tran R, Welter JD, Wang Y, Szabo T, Pearce LV, Lundberg DJ, Toth A, Pavlyukovets VA, Morgan MA, Blumberg PM.
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Bioorg Med Chem Lett. 15: 4136-42, 2005.
[Journal]
86)  Lee J, Jin MK, Kang SU, Kim SY, Lee J, Shin M, Hwang J, Cho S, Choi YS, Choi HK, Kim SE, Suh YG, Lee YS, Kim YH, Ha HJ, Toth A, Pearce LV, Tran R, Szabo T, Welter JD, Lundberg DJ, Wang Y, Lazar J, Pavlyukovets VA, Morgan MA, Blumberg PM.
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Bioorg Med Chem Lett. 15: 4143-50, 2005.
[Journal]
87)  Kang JH, Peach ML, Pu Y, Lewin NE, Nicklaus MC, Blumberg PM, Marquez VE.
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
J. Med. Chem. 48: 5738-48, 2005.
[Journal]
88)  Toth A, Wang Y, Kedei N, Tran R, Pearce LV, Kang S, Jin M, Choi H, Lee J, Blumberg PM.
Different vanilloid agonists cause different patterns of calcium response in CHO cells heterologously expressing rat TRPV1.
Life Sci. 76: 2921-32, 2005.
[Journal]
89)  Toth A, Boczan J, Kedei N, Lizanecz E, Bagi Z, Papp Z, Edes I, Csiba L, Blumberg PM.
Expression and distribution of vanilloid receptor 1 (TRPV1) in the adult rat brain.
Brain Res Mol Brain Res. 135: 162-8, 2005.
[Journal]
90)  Braun DC, Cao Y, Wang S, Garfield SH, Hur GM, Blumberg PM.
Role of phorbol ester localization in determining protein kinase C or RasGRP3 translocation: real-time analysis using fluorescent ligands and proteins.
Mol Cancer Ther. 4: 141-50, 2005.
[Journal]
91)  Okhrimenko H, Lu W, Xiang C, Ju D, Blumberg PM, Gomel R, Kazimirsky G, Brodie C.
Roles of tyrosine phosphorylation and cleavage of protein kinase Cdelta in its protective effect against tumor necrosis factor-related apoptosis inducing ligand-induced apoptosis.
J Biol Chem. 280: 23643-52, 2005.
[Journal]
92)  Qiang YW, Walsh K, Yao L, Kedei N, Blumberg PM, Rubin JS, Shaughnessy J, Rudikoff S.
Wnts induce migration and invasion of myeloma plasma cells.
Blood. 106: 1786-93, 2005.
[Journal]
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This page was last updated on 6/16/2014.