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Endocrine Abstracts

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ea0054p2 | (1) | NuclearReceptors2018

Next generation glucocorticoid receptor modulators

Edman Karl , Belfield Graham , Dearman Matthew , Edenro Goran , Geschwindner Stefan , Hegelund-Myrback Tove , Hemmerling Martin , Hendrickx Ramon , Keen Christina , Karrman-Mardh Carina , Lepisto Matti , Mitra Suman , Monkley Susan , Prothon Susanne , Ripa Lena , Steele John , Vaarala Outi , Wissler Lisa , Oberg Lisa

Synthetic glucocorticoids bind to the glucocorticoid receptor (GR) and have been used for nearly 70 years to treat inflammatory diseases. However, their use is limited by adverse effects such as diabetes, muscle wasting and osteoporosis. High throughput screening identified a novel non-steroidal scaffold with great potential for chemical optimization. Through rational design we developed the indazole ether series which combines high potency with structural motifs that provide ...
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Published by BioScientifica

Endocrine Abstracts
ISSN 1470-3947 (print) | ISSN 1479-6848 (online)
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