Literature DB >> 25875152

Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.

Derek T Rensing1, Sakshi Uppal1, Kendall J Blumer2, Kevin D Moeller1.   

Abstract

A simplified analog (WU-07047) of the selective Gαq/11 inhibitor YM-254890 has been synthesized, and an initial probe of its activity conducted. In the analog, the two peptide-based linkers in the cyclic YM-254890 have been replaced with hydrocarbon chains. This enables a convergent approach to the synthesis of the analog. Biochemical assays showed that while the simplified analog is not as potent as YM-254890, it does still inhibit Gq.

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Year:  2015        PMID： 25875152     DOI： 10.1021/acs.orglett.5b00944

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  12 in total

Review 1.  Gaq proteins: molecular pharmacology and therapeutic potential.

Authors:  Danielle Kamato; Partha Mitra; Felicity Davis; Narin Osman; Rebecca Chaplin; Peter J Cabot; Rizwana Afroz; Walter Thomas; Wenhua Zheng; Harveen Kaur; Margaret Brimble; Peter J Little
Journal:  Cell Mol Life Sci       Date:  2016-11-04       Impact factor: 9.261

Review 2.  Targeting G protein-coupled receptor signalling by blocking G proteins.

Authors:  Adrian P Campbell; Alan V Smrcka
Journal:  Nat Rev Drug Discov       Date:  2018-09-28       Impact factor: 84.694

Review 3.  Heterotrimeric Gq proteins as therapeutic targets?

Authors:  Evi Kostenis; Eva Marie Pfeil; Suvi Annala
Journal:  J Biol Chem       Date:  2020-03-02       Impact factor: 5.157

4.  Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.

Authors:  Xiao-Feng Xiong; Hang Zhang; Christina R Underwood; Kasper Harpsøe; Thomas J Gardella; Mie F Wöldike; Michael Mannstadt; David E Gloriam; Hans Bräuner-Osborne; Kristian Strømgaard
Journal:  Nat Chem       Date:  2016-07-25       Impact factor: 24.427

5.  Capitalizing on Mediated Electrolyses for the Construction of Complex, Addressable Molecular Surfaces.

Authors:  Ruby Krueger; Kevin D Moeller
Journal:  J Org Chem       Date:  2021-10-07       Impact factor: 4.354

6.  Macrocyclic Gq Protein Inhibitors FR900359 and/or YM-254890-Fit for Translation?

Authors:  Jonathan G Schlegel; Mariam Tahoun; Alexander Seidinger; Jan H Voss; Markus Kuschak; Stefan Kehraus; Marion Schneider; Michaela Matthey; Bernd K Fleischmann; Gabriele M König; Daniela Wenzel; Christa E Müller
Journal:  ACS Pharmacol Transl Sci       Date:  2021-02-19

7.  The experimental power of FR900359 to study Gq-regulated biological processes.

Authors:  Ramona Schrage; Anna-Lena Schmitz; Evelyn Gaffal; Suvi Annala; Stefan Kehraus; Daniela Wenzel; Katrin M Büllesbach; Tobias Bald; Asuka Inoue; Yuji Shinjo; Ségolène Galandrin; Naveen Shridhar; Michael Hesse; Manuel Grundmann; Nicole Merten; Thomas H Charpentier; Matthew Martz; Adrian J Butcher; Tanja Slodczyk; Sylvain Armando; Maike Effern; Yoon Namkung; Laura Jenkins; Velten Horn; Anne Stößel; Harald Dargatz; Daniel Tietze; Diana Imhof; Céline Galés; Christel Drewke; Christa E Müller; Michael Hölzel; Graeme Milligan; Andrew B Tobin; Jesús Gomeza; Henrik G Dohlman; John Sondek; T Kendall Harden; Michel Bouvier; Stéphane A Laporte; Junken Aoki; Bernd K Fleischmann; Klaus Mohr; Gabriele M König; Thomas Tüting; Evi Kostenis
Journal:  Nat Commun       Date:  2015-12-14       Impact factor: 14.919

8.  Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity.

Authors:  Davide Malfacini; Julian Patt; Suvi Annala; Kasper Harpsøe; Funda Eryilmaz; Raphael Reher; Max Crüsemann; Wiebke Hanke; Hang Zhang; Daniel Tietze; David E Gloriam; Hans Bräuner-Osborne; Kristian Strømgaard; Gabriele M König; Asuka Inoue; Jesus Gomeza; Evi Kostenis
Journal:  J Biol Chem       Date:  2019-02-11       Impact factor: 5.157

9.  RGS2 squelches vascular Gi/o and Gq signaling to modulate myogenic tone and promote uterine blood flow.

Authors:  Li Jie; Elizabeth A Owens; Lauren A Plante; Zhuyuan Fang; Derek T Rensing; Kevin D Moeller; Patrick Osei-Owusu
Journal:  Physiol Rep       Date:  2016-02

10.  Cell-permeable high-affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors.

Authors:  Markus Kuschak; Vigneshwaran Namasivayam; Muhammad Rafehi; Jan H Voss; Jaspal Garg; Jonathan G Schlegel; Aliaa Abdelrahman; Stefan Kehraus; Raphael Reher; Jim Küppers; Katharina Sylvester; Sonja Hinz; Michaela Matthey; Daniela Wenzel; Bernd K Fleischmann; Alexander Pfeifer; Asuka Inoue; Michael Gütschow; Gabriele M König; Christa E Müller
Journal:  Br J Pharmacol       Date:  2020-02-11       Impact factor: 8.739
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