Literature DB >> 34141064

Risdiplam, the First Approved Small Molecule Splicing Modifier Drug as a Blueprint for Future Transformative Medicines.

Hasane Ratni1, Renata S Scalco1, Alexander H Stephan1.   

Abstract

Not too long ago, the concept of selectively targeting mRNA with small molecules was perceived as a formidable scientific challenge. The discovery of small molecule splicing modifiers and the development of risdiplam for the treatment of spinal muscular atrophy (SMA) have firmly established proof of concept for this exciting new platform and transformed a scientific curiosity into a viable technology to target disease. Today, several approaches to target mRNA with small molecules, supported by biophysical and screening methods, are in place to deliver new drugs with high therapeutic relevance.
© 2021 American Chemical Society.

Entities:  

Year:  2021        PMID: 34141064      PMCID: PMC8201486          DOI: 10.1021/acsmedchemlett.0c00659

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN: 1948-5875            Impact factor:   4.632


  15 in total

Review 1.  The druggable genome.

Authors:  Andrew L Hopkins; Colin R Groom
Journal:  Nat Rev Drug Discov       Date:  2002-09       Impact factor: 84.694

2.  Rewriting the (tran)script: Application to spinal muscular atrophy.

Authors:  Hasane Ratni; Lutz Mueller; Martin Ebeling
Journal:  Prog Med Chem       Date:  2019-02-01

3.  SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice.

Authors:  James Palacino; Susanne E Swalley; Cheng Song; Atwood K Cheung; Lei Shu; Xiaolu Zhang; Mailin Van Hoosear; Youngah Shin; Donovan N Chin; Caroline Gubser Keller; Martin Beibel; Nicole A Renaud; Thomas M Smith; Michael Salcius; Xiaoying Shi; Marc Hild; Rebecca Servais; Monish Jain; Lin Deng; Caroline Bullock; Michael McLellan; Sven Schuierer; Leo Murphy; Marcel J J Blommers; Cecile Blaustein; Frada Berenshteyn; Arnaud Lacoste; Jason R Thomas; Guglielmo Roma; Gregory A Michaud; Brian S Tseng; Jeffery A Porter; Vic E Myer; John A Tallarico; Lawrence G Hamann; Daniel Curtis; Mark C Fishman; William F Dietrich; Natalie A Dales; Rajeev Sivasankaran
Journal:  Nat Chem Biol       Date:  2015-06-01       Impact factor: 15.040

Review 4.  Molecular choreography of pre-mRNA splicing by the spliceosome.

Authors:  Ruixue Wan; Rui Bai; Yigong Shi
Journal:  Curr Opin Struct Biol       Date:  2019-08-30       Impact factor: 6.809

5.  Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 ( SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA).

Authors:  Hasane Ratni; Martin Ebeling; John Baird; Stefanie Bendels; Johan Bylund; Karen S Chen; Nora Denk; Zhihua Feng; Luke Green; Melanie Guerard; Philippe Jablonski; Bjoern Jacobsen; Omar Khwaja; Heidemarie Kletzl; Chien-Ping Ko; Stefan Kustermann; Anne Marquet; Friedrich Metzger; Barbara Mueller; Nikolai A Naryshkin; Sergey V Paushkin; Emmanuel Pinard; Agnès Poirier; Michael Reutlinger; Marla Weetall; Andreas Zeller; Xin Zhao; Lutz Mueller
Journal:  J Med Chem       Date:  2018-07-25       Impact factor: 7.446

Review 6.  Drugging the RNA World.

Authors:  Matthew D Disney; Brendan G Dwyer; Jessica L Childs-Disney
Journal:  Cold Spring Harb Perspect Biol       Date:  2018-11-01       Impact factor: 10.005

7.  Risdiplam distributes and increases SMN protein in both the central nervous system and peripheral organs.

Authors:  Agnès Poirier; Marla Weetall; Katja Heinig; Franz Bucheli; Kerstin Schoenlein; Jochem Alsenz; Simon Bassett; Mohammed Ullah; Claudia Senn; Hasane Ratni; Nikolai Naryshkin; Sergey Paushkin; Lutz Mueller
Journal:  Pharmacol Res Perspect       Date:  2018-11-29

Review 8.  Principles for targeting RNA with drug-like small molecules.

Authors:  Katherine Deigan Warner; Christine E Hajdin; Kevin M Weeks
Journal:  Nat Rev Drug Discov       Date:  2018-07-06       Impact factor: 84.694

Review 9.  A comprehensive map of molecular drug targets.

Authors:  Rita Santos; Oleg Ursu; Anna Gaulton; A Patrícia Bento; Ramesh S Donadi; Cristian G Bologa; Anneli Karlsson; Bissan Al-Lazikani; Anne Hersey; Tudor I Oprea; John P Overington
Journal:  Nat Rev Drug Discov       Date:  2016-12-02       Impact factor: 84.694

10.  Binding to SMN2 pre-mRNA-protein complex elicits specificity for small molecule splicing modifiers.

Authors:  Manaswini Sivaramakrishnan; Kathleen D McCarthy; Sébastien Campagne; Sylwia Huber; Sonja Meier; Angélique Augustin; Tobias Heckel; Hélène Meistermann; Melanie N Hug; Pascale Birrer; Ahmed Moursy; Sarah Khawaja; Roland Schmucki; Nikos Berntenis; Nicolas Giroud; Sabrina Golling; Manuel Tzouros; Balazs Banfai; Gonzalo Duran-Pacheco; Jens Lamerz; Ying Hsiu Liu; Thomas Luebbers; Hasane Ratni; Martin Ebeling; Antoine Cléry; Sergey Paushkin; Adrian R Krainer; Frédéric H-T Allain; Friedrich Metzger
Journal:  Nat Commun       Date:  2017-11-14       Impact factor: 14.919

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  1 in total

1.  Development of 2-deoxystreptamine-nucleobase conjugates for the inhibition of oncogenic miRNA production.

Authors:  Thi Phuong Anh Tran; Sylvain Poulet; Mélanie Pernak; Anita Rayar; Stéphane Azoulay; Audrey Di Giorgio; Maria Duca
Journal:  RSC Med Chem       Date:  2021-12-16
  1 in total

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