Výsledky vyhledávání - "Chun-Wel Lin"

Substituted Hexahydrobenzo[f]thieno[c]quinolines as Dopamine D1-Selective Agonists: Synthesis and Biological Evaluation in Vitro and in Vivo

Autor: Chun Wel Lin, Michael R. Michaelides, Karen E. Asin, Kazumi Shiosaki, Erol K. Bayburt, Stanley Didomenico, Yufeng Hong, Donald R. Britton

Publikováno v: Journal of Medicinal Chemistry. 40:1585-1599

A series of substituted 9,10-dihydroxyhexahydrobenzo[f]thieno[c]quinolines (TB[f]Q), varying with respect to the position of the thiophene relative to the benzo[f]quinoline core and the nature and position of the substituent on the thiophene, were pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::757ccfc60392bf1f1491270137f13d31
https://doi.org/10.1021/jm970038v

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Human astrocytoma U138MG cells express predominantly type-A endothelin receptor

Autor: Jinshyun R. Wu-Wong, Bruce R Bianchi, Scott R. Magnuson, William J. Chiou, Chun Wel Lin

Publikováno v: Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. 1311:155-163

Endothelin-1 (ET-1) binding to human astrocytoma U138MG cells was time-dependent, and bound [125I]ET-1 was difficult to dissociate. The Bmax and Kd values of [125I]ET-1 binding were 70 fmol/mg and 0.07 nM, respectively. Interestingly, different from

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fa7586c990a1a39f25299edc0d5d9b3
https://doi.org/10.1016/0167-4889(95)00202-2

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Amino acid-derived piperidides as novel CCKB ligands with anxiolytic-like properties

Autor: Chun Wel Lin, Thomas R. Miller, Alex M. Nadzan, Mark W. Holladay, James F. Kerwin, Alyssa B. O'Neill, Michael J. Bennett, Hao Bai, Michael Stashko, Jorge D. Brioni, Jeffrey W. Ralston

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:3057-3062

The development of a novel series of carbamoylamino acid benzoylpiperidides as CCK B ligands is described. Selected members of the series antagonized CCK 8 -induced calcium mobilization and showed efficacy in the mouse elevated-plus maze, a measure o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3a9417dff910f69b0bb3355c5436362d
https://doi.org/10.1016/0960-894x(95)00537-3

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Double bond isosteres of the peptide bond: Synthesis and biological activity of cholecystokinin (CCK) C-terminal hexapeptide analogs

Autor: Sharon L. Kuyper, Alex M. Nadzan, Chun Wel Lin, Michael D. Tufano, Mike Stashko, Thomas R. Miller, Mark W. Holladay, Hana Kopecka, David G. Witte, Y.‐K. Shue, George M. Carrera

Publikováno v: Bioorganic & Medicinal Chemistry. 1:161-171

New and existing methodologies were used to prepare a series of modified CCK analogs in which each amide bond was replaced by a trans-alkene unit. The data indicate that every amide linkage at C-terminal tetrapeptide (CCK-4) region is crucial for bio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aed43732409febe53663b805ae77254d
https://doi.org/10.1016/s0968-0896(00)82117-3

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Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists

Autor: Alex M. Nadzan, Kazumi Shiosaki, Michael A. Stashko, David G. Witte, Chun Wel Lin, Thomas R. Miller, Howard E. Morton, M.Robert Leanna

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:855-860

The backbone amide bonds in two series of tetrapeptide-based CCK-A receptor agonists were systematically replaced with the methylene amino isostere. Potent and selective pseudopeptides were identified that will facilitate our understanding of how the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c11ec55e2cb071dc868d95018cdc817e
https://doi.org/10.1016/s0960-894x(00)80680-0

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Characterization of the novel CCK analogs JMV-180, JMV-320, and JMV-332 in H345 cells

Autor: Alex M. Nadzan, Jean Martinez, Marc Rodriguez, David G. Witte, Chun Wel Lin

Publikováno v: Peptides. 13:1227-1232

The interaction of the novel CCK analogs JMV-180, JMV-320, and JMV-332 with CCK-B/gastrin receptors on small cell lung cancer (SCLC) cells was investigated. JMV-180, JMV-320, and JMV-332 potently inhibited specific binding of 125I-CCK-8 to CCK-B/gast

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85b2efa402924a40433d21e5ef37a1d2
https://doi.org/10.1016/0196-9781(92)90033-y

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Synthesis and biological activity of CCK heptapeptide analogs. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo

Autor: Mark W. Holladay, Bruce R. Bianchi, Chun Wel Lin, Michael D. Tufano, Karen E. Asin, A. L. Nikkel, L. Bednarz, Thomas R. Miller, M. J. Bennett, David G. Witte

Publikováno v: Journal of Medicinal Chemistry. 35:2919-2928

A series of modifications of the CCK7 analogue (des-NH2)Tyr(SO3-)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 was prepared and tested for binding to guinea pig CCK-A and CCK-B receptors and in CCK-A-mediated functional assays. Selected analogues also were tested for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7dfd97b6802cad79e529f6edcaf41025
https://doi.org/10.1021/jm00094a001

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