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1.

001-es BibID:BIBFORM003725
Első szerző:Chung, Jae-Uk
Cím:Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists / Chung, J. U., Kim, S. Y., Lim, J. O., Choi, H. K., Kang, S. U., Yoon, H. S., Ryu, H., Kang, D. W., Lee, J., Kang, B., Choi, S., Toth, A., Pearce, L. V., Pavlyukovets, V. A., Lundberg, D. J., Blumberg, P. M.
Dátum:2007
Megjegyzések:A series of alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. alpha-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds 14 and 18, which possess the R-configuration, exhibited excellent potencies (respectively, K(i)=41 and 39.2 nM and K(i(ant))=4.5 and 37 nM)
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Animals
antagonists &amp
Calcium
Capsaicin
Cells,Cultured
chemical synthesis
chemistry
Cho Cells
Cricetinae
Cricetulus
inhibitors
metabolism
Models,Molecular
Molecular Structure
pharmacology
Rats
Stereoisomerism
Structure-Activity Relationship
Thiourea
TRPV Cation Channels
Megjelenés:Bioorganic and Medical Chemistry. - 15 : 18 (2007), p. 6043-6053. -
További szerzők:Kim, Su Yeon Lim, Ju-Ok Choi, Hyun-Kyung Kang, Sang-Uk Yoon, Hae-Seok Ryu, HyungChul Kang, Dong Wook Lee, Jeewoo Kang, Bomi Choi, Sun Tóth Attila (1971-) (biológus) Pearce, Larry V. Pavlyukovets, Vladimir A. Lundberg, Daniel J. Blumberg, Peter M.
Internet cím:elektronikus változat
DOI
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2.

001-es BibID:BIBFORM058130
Első szerző:Kedei Noémi
Cím:Characterization of the interaction of ingenol 3-angelate with protein kinase C / Noemi Kedei, Daniel J. Lundberg, Attila Toth, Peter Welburn, Susan H. Garfield, Peter M. Blumberg
Dátum:2004
ISSN:0008-5472
Megjegyzések:Ingenol 3-angelate (I3A) is one of the active ingredients in Euphorbia peplus, which has been used in traditional medicine. Here, we report the initial characterization of I3A as a protein kinase C (PKC) ligand. I3A bound to PKC-alpha in the presence of phosphatidylserine with high affinity; however, under these assay conditions, little PKC isoform selectivity was observed. PKC isoforms did show different sensitivity and selectivity for down-regulation by I3A and phorbol 12-myristate 13-acetate (PMA) in WEHI-231, HOP-92, and Colo-205 cells. In all of the three cell types, I3A inhibited cell proliferation with somewhat lower potency than did PMA. In intact CHO-K1 cells, I3A was able to translocate different green fluorescent protein-tagged PKC isoforms, visualized by confocal microscopy, with equal or higher potency than PMA. PKC-delta in particular showed a different pattern of translocation in response to I3A and PMA. I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction. I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance. The in vitro kinase activity of PKC-alpha induced by I3A was lower than that induced by PMA. The novel pattern of behavior of I3A makes it of great interest for further evaluation.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Cancer Research. - 64 : 9 (2004), p. 3243-3255. -
További szerzők:Lundberg, Daniel J. Tóth Attila (1971-) (biológus) Welburn, Peter Garfield, Susan H. Blumberg, Peter M.
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DOI
Intézményi repozitóriumban (DEA) tárolt változat
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3.

001-es BibID:BIBFORM058125
Első szerző:Lee, Jeewoo
Cím:Analysis of structure-activity relationships with the N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea template for vanilloid receptor 1 antagonism / Jeewoo Lee, Su Yeon Kim, Jiyoun Lee, Myungsim Kang, Min-Jung Kil, Hyun-Kyung Choi, Mi-Kyung Jin, Yun Wang, Attila Toth, Larry V. Pearce, Daniel J. Lundberg, Richard Tran, Peter M. Blumberg
Dátum:2004
ISSN:0968-0896
Megjegyzések:In a continuing effort to elucidate the structure-activity relationships of the lead antagonist N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N'-[4-(methylsulfonylamino)benzyl]thiourea (1), the distances between the proposed four pharmacophores in 1 have been varied by insertion or deletion of one carbon to optimize their fit to the receptor. In addition, the acyloxy group of the C region was replaced with amide and N-hydroxy amide to identify the pharmacophoric importance of the ester group in the C2 region. The results indicated that the pharmacophoric arrangement of 1 was optimal for receptor binding affinity and antagonism, and the ester of the C2 region was significant for receptor binding. Among the derivatives, compound 19 showed distinct behavior with a 2-fold improvement in antagonism but a 13-fold reduction in binding affinity compared to 1. The partial separation of pharmacophoric requirements of these two assays has been noted before and compound 19 is thus selective for the calcium entry-linked receptor population. The conformational analysis of 1 generated three distinct conformers having different types of hydrophobic interactions, which will be utilized for exploring the active conformation of the VR1 ligand.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Bioorganic & Medicinal Chemistry. - 12 : 13 (2004), p. 3411-3420. -
További szerzők:Kim, Su Yeon Lee, Jiyoun Kang, Myungshim Kil, Min-Jung Choi, Hyun-Kyung Jin, Mi-Kyung Wang, Yun Tóth Attila (1971-) (biológus) Pearce, Larry V. Lundberg, Daniel J. Tran, Richard Blumberg, Peter M.
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4.

001-es BibID:BIBFORM058129
Első szerző:Lee, Jeewoo
Cím:Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists : discovery of an N-hydroxythiourea analogue with potent analgesic activity / Jeewoo Lee, Sang-Uk Kang, Hyun-Kyung Choi, Jiyoun Lee, Ju-Ok Lim, Min-Jung Kil, Mi-Kyung Jin, Kang-Pil Kim, Jong-Hyuk Sung, Suk-Jae Chung, Hee-Jin Ha, Young-Ho Kim, Larry V. Pearce, Richard Tran, Daniel J. Lundberg, Yun Wang, Attila Toth, Peter M. Blumberg
Dátum:2004
ISSN:0960-894X
Megjegyzések:The structural modifications on the B-region of the potent and high affinity vanilloid receptor (VR1) lead ligand N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea were investigated by the replacement of the thiourea with diverse isosteric functional groups. Structure-activity analysis indicated that the A-region in this series was the primary factor in determining the agonistic/antagonistic activities regardless of the B-region. The N(C)-hydroxy thiourea analogues (12, 13) showed excellent analgesic activities in the acetic acid writhing assay compared to the parent thiourea analogues.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Bioorganic & Medicinal Chemistry Letters. - 14 : 9 (2004), p. 2291-2297. -
További szerzők:Kang, Sang-Uk Choi, Hyun-Kyung Lee, Jiyoun Lim, Ju-Ok Kil, Min-Jung Jin, Mi-Kyung Kim, Kang-Pil Sung, Jong-Hyuk Chung, Suk-Jae Ha, Hee-Jin Kim, Young-Ho Pearce, Larry V. Tran, Richard Lundberg, Daniel J. Wang, Yun Tóth Attila (1971-) (biológus) Blumberg, Peter M.
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Intézményi repozitóriumban (DEA) tárolt változat
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5.

001-es BibID:BIBFORM058133
Első szerző:Lee, Jeewoo
Cím:N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues : novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor / Jeewoo Lee, Jiyoun Lee, Myungshim Kang, Myoungyoup Shin, Ji-Min Kim, Sang-Uk Kang, Ju-Ok Lim, Hyun-Kyung Choi, Young-Ger Suh, Hyeung-Geun Park, Uhtaek Oh, Hee-Doo Kim, Young-Ho Park, Hee-Jin Ha, Young-Ho Kim, Attila Toth, Yun Wang, Richard Tran, Larry V. Pearce, Daniel J. Lundberg, Peter M. Blumberg
Dátum:2003
ISSN:0022-2623 1520-4804
Megjegyzések:Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with the alkylsulfonamido group provides a series of compounds which are effective antagonists to the action of the capsaicin on rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N'-[3-fluoro-4-(methylsulfonylamino)benzyl]thiourea was a full antagonist against capsaicin, displayed a K(i) value of 7.8 nM (compared to 520 nM for capsazepine and 4 nM for 5-iodoRTX), and showed excellent analgesic activity in mice. Structure-activity analysis of the influence of modifications in the A- and C-regions of 4-methylsulfonamide ligands on VR1 agonism/antagonism indicated that 3-fluoro substitution in the A-region and a 4-tert-butylbenzyl moiety in the C-region favored antagonism, whereas a 3-methoxy group in the A-region and 3-acyloxy-2-benzylpropyl moieties in the C-region favored agonism.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Journal of Medicinal Chemistry. - 46 : 14 (2003), p. 3116-3126. -
További szerzők:Lee, Jiyoun Kang, Myungshim Shin, Myoungyoup Kim, Ji-Min Kang, Sang-Uk Lim, Ju-Ok Choi, Hyun-Kyung Suh, Young-Ger Park, Hyeung-Geun Oh, Uhtaek Kim, Hee-Doo Park, Young Ho Ha, Hee-Jin Kim, Young-Ho Tóth Attila (1971-) (biológus) Wang, Yun Tran, Richard Pearce, Larry V. Lundberg, Daniel J. Blumberg, Peter M.
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DOI
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6.

001-es BibID:BIBFORM058122
Első szerző:Lee, Jeewoo
Cím:Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists / Jeewoo Lee, Mi-Kyoung Jin, Sang-Uk Kang, Su Yeon Kim, Jiyoun Lee, Myoungyoup Shin, Jaemin Hwang, Sookhyun Cho, Yeon-Sil Choi, Hyun-Kyung Choi, Sung-Eun Kim, Young-Ger Suh, Yong-Sil Lee, Young-Ho Kim, Hee-Jin Ha, Attila Toth, Larry V. Pearce, Richard Tran, Tamas Szabo, Jacqueline D. Welter, Daniel J. Lundberg, Yun Wang, Jozsef Lazar, Vladimir A. Pavlyukovets, Matthew A. Morgan, Peter M. Blumberg
Dátum:2005
ISSN:0960-894X
Megjegyzések:The structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. A docking model of potent antagonist 2 with the sensor region of TRPV1 is proposed.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Bioorganic & Medicinal Chemistry Letters. - 15 : 18 (2005), p. 4143-4150. -
További szerzők:Jin, Mi-Kyoung Kang, Sang-Uk Kim, Su Yeon Lee, Jiyoun Shin, Myoungyoup Hwang, Jaemin Cho, Sookhyun Choi, Yeon-Sil Choi, Hyun-Kyung Kim, Sung-Eun Suh, Young-Ger Lee, Yong-Sil Kim, Young-Ho Ha, Hee-Jin Tóth Attila (1971-) (biológus) Pearce, Larry V. Tran, Richard Szabó Tamás Welter, Jacqueline D. Lundberg, Daniel J. Wang, Yun Lázár József Pavlyukovets, Vladimir A. Morgan, Matthew A. Blumberg, Peter M.
Internet cím:Szerző által megadott URL
DOI
Intézményi repozitóriumban (DEA) tárolt változat
Borító:

7.

001-es BibID:BIBFORM016029
Első szerző:Lee, Jeewoo
Cím:Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists / Jeewoo Lee, Sang-Uk Kang, Min-Jung Kil, Myoungyoup Shin, Ju-Ok Lim, Hyun-Kyung Choi, Mi-Kyoung Jin, Su Yeon Kim, Sung-Eun Kim, Yong-Sil Lee, Kyung-Hoon Min, Young-Ho Kim, Hee-Jin Ha, Richard Tran, Jacqueline D. Welter, Yun Wang, Tamas Szabo, Larry V. Pearce, Daniel J. Lundberg, Attila Toth, Vladimir A. Pavlyukovets, Matthew A. Morgan, Peter M. Blumberg
Dátum:2005
ISSN:0960-894X
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Bioorganic & Medicinal Chemistry Letters. - 15 : 18 (2005), p. 4136-4142. -
További szerzők:Kang, Sang-Uk Kil, Min-Jung Shin, Myoungyoup Lim, Ju-Ok Choi, Hyun-Kyung Jin, Mi-Kyoung Kim, Su Yeon Kim, Sung-Eun Lee, Yong-Sil Min, Kyung-Hoon Kim, Young-Ho Ha, Hee-Jin Tran, Richard Welter, Jacqueline D. Wang, Yun Szabó Tamás (1968-) (gyermekgyógyász) Pearce, Larry V. Lundberg, Daniel J. Tóth Attila (1971-) (biológus) Pavlyukovets, Vladimir A. Morgan, Matthew A. Blumberg, Peter M.
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
DOI
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8.

001-es BibID:BIBFORM005639
Első szerző:Ryu, HyungChul
Cím:Stereospecific high-affinity TRPV1 antagonists : chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues / Ryu, H., Jin, M. K., Kim, S. Y., Choi, H. K., Kang, S. U., Kang, D. W., Lee, J., Pearce, L. V., Pavlyukovets, V. A., Morgan, M. A., Tran, R., Toth, A., Lundberg, D. J., Blumberg, P. M.
Dátum:2008
ISSN:0022-2623 (Print)
Megjegyzések:Previously, we reported the thiourea antagonists 2a and 2b as potent and high affinity TRPV1 antagonists. For further optimization of the lead compounds, a series of their amide and alpha-substituted amide surrogates were investigated and novel chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues were characterized as potent and stereospecific rTRPV1 antagonists. In particular, compounds 72 and 73 displayed high binding affinities, with K i values of 4.12 and 1.83 nM and potent antagonism with K i values of 0.58 and 5.2 nM, respectively, in rTRPV1/CHO cells. These values are comparable or more potent than those of 5-iodoRTX under the same assay conditions. A distinctive binding model that includes two hydrophobic pockets is proposed for this series of compounds based on docking studies of 57 and 72 with a homology model of the TM3/4 region of TRPV1.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Animals
Benzeneacetamides
Binding Sites
Binding, Competitive
CHO Cells
Calcium/metabolism
Cricetinae
Cricetulus
Hydrophobicity
Mesylates
Models, Molecular
Radioligand Assay
Rats
Stereoisomerism
Structure-Activity Relationship
TRPV Cation Channels
Megjelenés:Journal of Medicinal Chemistry. - 51 : 1 (2008), p. 57-67. -
További szerzők:Jin, Mi-Kyoung Kim, Su Yeon Choi, Hyun-Kyung Kang, Sang-Uk Kang, Dong Wook Lee, Jeewoo Pearce, Larry V. Pavlyukovets, Vladimir A. Morgan, Matthew A. Tran, Richard Tóth Attila (1971-) (biológus) Lundberg, Daniel J. Blumberg, Peter M.
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