Literature DB >> 20434910

Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.

Ralph N Harris1, Russel S Stabler, David B Repke, James M Kress, Keith A Walker, Renee S Martin, Julie M Brothers, Mariola Ilnicka, Simon W Lee, Tara Mirzadegan.   

Abstract

A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism. Copyright 2010. Published by Elsevier Ltd.

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Year:  2010        PMID： 20434910     DOI： 10.1016/j.bmcl.2010.03.110

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  In Silico Screening of Natural Compounds for Candidates 5HT6 Receptor Antagonists against Alzheimer's Disease.

Authors:  Tijana Bojić; Milan Sencanski; Vladimir Perovic; Jelena Milicevic; Sanja Glisic
Journal:  Molecules       Date:  2022-04-19       Impact factor: 4.927

2.  Pyrano[2,3,4-cd]indole as a Scaffold for Selective Nonbasic 5-HT6R Ligands.

Authors:  Jakub Staroń; Stefan Mordalski; Dawid Warszycki; Grzegorz Satała; Adam Hogendorf; Andrzej J Bojarski
Journal:  ACS Med Chem Lett       Date:  2017-03-27       Impact factor: 4.345

3.  Low-basicity 5-HT7 Receptor Agonists Synthesized Using the van Leusen Multicomponent Protocol.

Authors:  Adam S Hogendorf; Agata Hogendorf; Rafał Kurczab; Grzegorz Satała; Tomasz Lenda; Maria Walczak; Gniewomir Latacz; Jadwiga Handzlik; Katarzyna Kieć-Kononowicz; Joanna M Wierońska; Monika Woźniak; Paulina Cieślik; Ryszard Bugno; Jakub Staroń; Andrzej J Bojarski
Journal:  Sci Rep       Date:  2017-05-04       Impact factor: 4.379

4.  Constitutive Activity of Serotonin Receptor 6 Regulates Human Cerebral Organoids Formation and Depression-like Behaviors.

Authors:  Qinying Wang; Xiaoxu Dong; Tingting Hu; Chao Qu; Jing Lu; Yue Zhou; Jinsong Li; Gang Pei
Journal:  Stem Cell Reports       Date:  2020-12-23       Impact factor: 7.765

Review 5.  Multitargeting the Action of 5-HT6 Serotonin Receptor Ligands by Additional Modulation of Kinases in the Search for a New Therapy for Alzheimer's Disease: Can It Work from a Molecular Point of View?

Authors:  Kinga Czarnota-Łydka; Katarzyna Kucwaj-Brysz; Patryk Pyka; Wawrzyniec Haberek; Sabina Podlewska; Jadwiga Handzlik
Journal:  Int J Mol Sci       Date:  2022-08-07       Impact factor: 6.208

6.  Novel N-Arylsulfonylindoles Targeted as Ligands of the 5-HT6 Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity.

Authors:  Loreto Arrieta-Rodríguez; Daniela Espinoza-Rosales; Gonzalo Vera; Young Hwa Cho; David Cabezas; David Vásquez-Velásquez; Jaime Mella-Raipán; Carlos F Lagos; Gonzalo Recabarren-Gajardo
Journal:  Pharmaceuticals (Basel)       Date:  2021-06-01

7.  The serotonin 6 receptor controls neuronal migration during corticogenesis via a ligand-independent Cdk5-dependent mechanism.

Authors:  Moritz Jacobshagen; Mathieu Niquille; Séverine Chaumont-Dubel; Philippe Marin; Alexandre Dayer
Journal:  Development       Date:  2014-07-30       Impact factor: 6.868
  7 in total

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