Literature DB >> 12372520

Synthesis and biological activity of retinoic acid receptor-alpha specific amides.

Richard L Beard1, Tien T Duong, Min Teng, Elliott S Klein, Andrew M Standevan, Roshantha A S Chandraratna.   

Abstract

Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.

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Year:  2002        PMID: 12372520     DOI: 10.1016/s0960-894x(02)00647-9

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


  10 in total

1.  An in vitro model for the pro-fibrotic effects of retinoids: mechanisms of action.

Authors:  A C Rankin; B M Hendry; J P Corcoran; Q Xu
Journal:  Br J Pharmacol       Date:  2013-11       Impact factor: 8.739

Review 2.  Strategies to generate functionally normal neutrophils to reduce infection and infection-related mortality in cancer chemotherapy.

Authors:  Hisham Abdel-Azim; Weili Sun; Lingtao Wu
Journal:  Pharmacol Ther       Date:  2019-08-27       Impact factor: 12.310

Review 3.  Retinoid roles and action in skeletal development and growth provide the rationale for an ongoing heterotopic ossification prevention trial.

Authors:  Maurizio Pacifici
Journal:  Bone       Date:  2017-08-19       Impact factor: 4.398

4.  Superenhancer Analysis Defines Novel Epigenomic Subtypes of Non-APL AML, Including an RARα Dependency Targetable by SY-1425, a Potent and Selective RARα Agonist.

Authors:  Michael R McKeown; M Ryan Corces; Matthew L Eaton; Chris Fiore; Emily Lee; Jeremy T Lopez; Mei Wei Chen; Darren Smith; Steven M Chan; Julie L Koenig; Kathryn Austgen; Matthew G Guenther; David A Orlando; Jakob Lovén; Christian C Fritz; Ravindra Majeti
Journal:  Cancer Discov       Date:  2017-07-20       Impact factor: 39.397

Review 5.  Potential role for all-trans retinoic acid in nonpromyelocytic acute myeloid leukemia.

Authors:  Hayley S Ma; Tara M Robinson; Donald Small
Journal:  Int J Hematol Oncol       Date:  2017-03-14

6.  Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.

Authors:  Earl Clarke; Christopher I Jarvis; Maria B Goncalves; S Barret Kalindjian; David R Adams; Jane T Brown; Jason J Shiers; David M A Taddei; Elodie Ravier; Stephanie Barlow; Iain Miller; Vanessa Smith; Alan D Borthwick; Jonathan P T Corcoran
Journal:  Bioorg Med Chem       Date:  2017-12-09       Impact factor: 3.641

Review 7.  RARG Gene Dysregulation in Acute Myeloid Leukemia.

Authors:  Maria Rosa Conserva; Immacolata Redavid; Luisa Anelli; Antonella Zagaria; Giorgina Specchia; Francesco Albano
Journal:  Front Mol Biosci       Date:  2019-10-24

Review 8.  Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review.

Authors:  Alan D Borthwick; Maria B Goncalves; Jonathan P T Corcoran
Journal:  Bioorg Med Chem       Date:  2020-07-29       Impact factor: 3.641

9.  Uncoupling RARA transcriptional activation and degradation clarifies the bases for APL response to therapies.

Authors:  Julien Ablain; Magdalena Leiva; Laurent Peres; Julien Fonsart; Elodie Anthony; Hugues de Thé
Journal:  J Exp Med       Date:  2013-03-18       Impact factor: 14.307

10.  Discovery of retinoic acid receptor agonists as proliferators of cardiac progenitor cells through a phenotypic screening approach.

Authors:  Lauren Drowley; Jane McPheat; Anneli Nordqvist; Samantha Peel; Ulla Karlsson; Sofia Martinsson; Erik Müllers; Anita Dellsén; Sinead Knight; Ian Barrett; José Sánchez; Björn Magnusson; Boris Greber; Qing-Dong Wang; Alleyn T Plowright
Journal:  Stem Cells Transl Med       Date:  2019-09-11       Impact factor: 6.940

  10 in total

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