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COMMUNICATIONS
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1251-1252
Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the -Opioid Receptor Does Not Affect Dynorphin A(1-13) Affinity and Function
David M. Ferguson,
Stacy Kramer,
Thomas G. Metzger,
Ping Y. Law, and
Philip S. Portoghese
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1253-1256
A Novel Macromolecular Prodrug Concept Exploiting Endogenous Serum Albumin as a Drug Carrier for Cancer Chemotherapy
Felix Kratz,
Ralph Müller-Driver,
Inga Hofmann,
Joachim Drevs, and
Clemens Unger
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EXPEDITED ARTICLES
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1257-1263
N-3-Substituted Imidazoquinazolinones: Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile Dysfunction
David P. Rotella,
Zhong Sun,
Yeheng Zhu,
John Krupinski,
Ronald Pongrac,
Laurie Seliger,
Diane Normandin, and
John E. Macor
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ARTICLES
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1264-1270
Synthesis, Conformational Analysis, and Biological Activity of C-Thioribonucleosides Related to Tiazofurin
Palmarisa Franchetti,
Stefano Marchetti,
Loredana Cappellacci,
Hiremagalur N. Jayaram,
Joel Aaron Yalowitz,
Barry M. Goldstein,
Jean-Louis Barascut,
David Dukhan,
Jean-Louis Imbach, and
Mario Grifantini
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1271-1281
Conformational Selection of Inhibitors and Substrates by Proteolytic Enzymes: Implications for Drug Design and Polypeptide Processing
David P. Fairlie,
Joel D. A. Tyndall,
Robert C. Reid,
Allan K. Wong,
Giovanni Abbenante,
Martin J. Scanlon,
Darren R. March,
Douglas A. Bergman,
Christina L. L. Chai, and
Brendan A. Burkett
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1282-1292
Cyclin-Dependent Kinase Inhibition by New C-2 Alkynylated Purine Derivatives and Molecular Structure of a CDK2-Inhibitor Complex
Michel Legraverend,
Paul Tunnah,
Martin Noble,
Pierre Ducrot,
Odile Ludwig,
David S. Grierson,
Maryse Leost,
Laurent Meijer, and
Jane Endicott
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1293-1310
Novel Benzofuran and Benzothiophene Biphenyls as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic Properties
Michael S. Malamas,
Janet Sredy,
Christopher Moxham,
Alan Katz,
Weixin Xu,
Robert McDevitt,
Folake O. Adebayo,
Diane R. Sawicki,
Laura Seestaller,
Donald Sullivan, and
Joseph R. Taylor
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1311-1319
Synthesis and Anticonvulsant and Neurotoxic Properties of Substituted N-Phenyl Derivatives of the Phthalimide Pharmacophore
Joseph Vamecq,
Pierre Bac,
Christine Herrenknecht,
Pierre Maurois,
Philippe Delcourt, and
James P. Stables
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1320-1328
Statistical Molecular Design of Building Blocks for Combinatorial Chemistry
Anna Linusson,
Johan Gottfries,
Fredrik Lindgren, and
Svante Wold
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1329-1338
High-Affinity, Non-Peptide Agonists for the ORL1 (Orphanin FQ/Nociceptin) Receptor
Stephan Röver,
Geo Adam,
Andrea M. Cesura,
Guido Galley,
François Jenck,
Frederick J. Monsma, Jr.,
Jürgen Wichmann, and
Frank M. Dautzenberg
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1339-1349
Derivatives of (R)-1,11-Methyleneaporphine: Synthesis, Structure, and Interactions with G-Protein Coupled Receptors
Tero Linnanen,
Magnus Brisander,
Lena Unelius,
Göran Sundholm,
Uli Hacksell, and
Anette M. Johansson
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1350-1358
Bis(phenazine-1-carboxamides): Structure-Activity Relationships for a New Class of Dual Topoisomerase I/II-Directed Anticancer Drugs
Julie A. Spicer,
Swarna A. Gamage,
Gordon W. Rewcastle,
Graeme J. Finlay,
David J. A. Bridewell,
Bruce C. Baguley, and
William A. Denny
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1359-1366
Deltorphin II Analogues with 6-Hydroxy-2-aminotetralin-2-carboxylic Acid in Position 1
Zsuzsanna Darula,
Katalin E. Kövér,
Krisztina Monory,
Anna Borsodi,
Éva Makó,
András Rónai,
Dirk Tourwé,
Antal Péter, and
Géza Tóth
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1367-1379
Lipopolycationic Telomers for Gene Transfer: Synthesis and Evaluation of Their in Vitro Transfection Efficiency
Géraldine Verderone,
Nathalie Van Craynest,
Otmane Boussif,
Catherine Santaella,
Rainer Bischoff,
Hanno V. J. Kolbe, and
Pierre Vierling
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1380-1397
Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions
Jeff B. Smaill,
Gordon W. Rewcastle,
Joseph A. Loo,
Kenneth D. Greis,
O. Helen Chan,
Eric L. Reyner,
Elke Lipka,
H. D. Hollis Showalter,
Patrick W. Vincent,
William L. Elliott, and
William A. Denny
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1398-1408
Phosphinic Derivatives as New Dual Enkephalin-Degrading Enzyme Inhibitors: Synthesis, Biological Properties, and Antinociceptive Activities
Huixiong Chen,
Florence Noble,
Aurélie Mothé,
Hervé Meudal,
Pascale Coric,
Sophie Danascimento,
Bernard P. Roques,
Pascal George, and
Marie-Claude Fournié-Zaluski
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BRIEF ARTICLES
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1409-1412
Synthesis and Oral Antitumor Activity of Tetrakis(carboxylato)platinum(IV) Complexes
Young-A Lee,
Sung Sil Lee,
Kwan Mook Kim,
Chong Ock Lee, and
Youn Soo Sohn
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1413-1417
Inhibition of Protein Kinase C by Dequalinium Analogues: Dependence on Linker Length and Geometry
Donghui Qin,
Regina Sullivan,
William F. Berkowitz,
Robert Bittman, and
Susan A. Rotenberg
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1418-1421
Protection against Oxidative Damage by Iron Chelators: Effect of Lipophilic Analogues and Prodrugs of N,N'-Bis(3,4,5-trimethoxybenzyl)ethylenediamine- N,N'-diacetic Acid (OR10141)
Jean-Baptiste Galey,
Odile Destrée,
Jacqueline Dumats,
Sylvie Génard, and
Pierre Tachon
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BOOK REVIEWS
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1422-1422
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1422-1422
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ADDITIONS AND CORRECTIONS
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1423-1426
2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the 2D Adrenergic Receptor
Tina M. Ross,
Michele C. Jetter,
Mark E. McDonnell,
Robert E. Boyd,
Charlene D. Connelly,
Rebecca P. Martinez,
Martin A. Lewis,
Ellen E. Codd,
Robert B. Raffa, and
Allen B. Reitz
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