Literature DB >> 16250835

Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach.

R A Glennon1.   

Abstract

At least two different types of sigma (sigma1 and sigma2) receptors have been identified. A structural feature common to high-affinity (Ki <10 nM) sigma1 ligands is: C-N(R)-X-Ph; both C and Ph are associated with regions of bulk tolerance. Numerous other ligands bind, but typically do so with lower affinity.

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Year:  2005        PMID： 16250835     DOI： 10.2174/138955705774329519

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN： 1389-5575            Impact factor:   3.862


  30 in total

1.  The sigma-1 receptor chaperone as an inter-organelle signaling modulator.

Authors:  Tsung-Ping Su; Teruo Hayashi; Tangui Maurice; Shilpa Buch; Arnold E Ruoho
Journal:  Trends Pharmacol Sci       Date:  2010-10-01       Impact factor: 14.819

Review 2.  The ligand binding region of the sigma-1 receptor: studies utilizing photoaffinity probes, sphingosine and N-alkylamines.

Authors:  Arnold E Ruoho; Uyen B Chu; Subramaniam Ramachandran; Dominique Fontanilla; Timur Mavlyutov; Abdol R Hajipour
Journal:  Curr Pharm Des       Date:  2012       Impact factor: 3.116

3.  Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.

Authors:  Rong Xu; John R Lever; Susan Z Lever
Journal:  Bioorg Med Chem Lett       Date:  2007-02-04       Impact factor: 2.823

Review 4.  Evolutions in fragment-based drug design: the deconstruction-reconstruction approach.

Authors:  Haijun Chen; Xiaobin Zhou; Ailan Wang; Yunquan Zheng; Yu Gao; Jia Zhou
Journal:  Drug Discov Today       Date:  2014-09-27       Impact factor: 7.851

5.  Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (σ2) receptor and P-gp protein in the cytotoxic action: In vitro and in vivo activity in pancreatic tumors.

Authors:  Maria Laura Pati; Mauro Niso; Dirk Spitzer; Francesco Berardi; Marialessandra Contino; Chiara Riganti; William G Hawkins; Carmen Abate
Journal:  Eur J Med Chem       Date:  2017-12-08       Impact factor: 6.514

6.  The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.

Authors:  Richard A Glennon
Journal:  J Med Chem       Date:  2017-03-15       Impact factor: 7.446

7.  Photoaffinity labeling of the sigma-1 receptor with N-[3-(4-nitrophenyl)propyl]-N-dodecylamine: evidence of receptor dimers.

Authors:  Uyen B Chu; Subramaniam Ramachandran; Abdol R Hajipour; Arnold E Ruoho
Journal:  Biochemistry       Date:  2013-01-28       Impact factor: 3.162

8.  In vitro evaluation of guanidine analogs as sigma receptor ligands for potential anti-stroke therapeutics.

Authors:  Adam A Behensky; Michelle Cortes-Salva; Michael J Seminerio; Rae R Matsumoto; Jon C Antilla; Javier Cuevas
Journal:  J Pharmacol Exp Ther       Date:  2012-10-12       Impact factor: 4.030

9.  The sigma1 receptor interacts with N-alkyl amines and endogenous sphingolipids.

Authors:  Subramaniam Ramachandran; Uyen B Chu; Timur A Mavlyutov; Arindam Pal; Susan Pyne; Arnold E Ruoho
Journal:  Eur J Pharmacol       Date:  2009-03-11       Impact factor: 4.432

10.  An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure-affinity relationship for butyrophenones.

Authors:  Ivan T Lee; Shiuhwei Chen; John A Schetz
Journal:  Eur J Pharmacol       Date:  2007-10-02       Impact factor: 4.432
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