Bismethylenedioxy Steroids. IV.<sup>1</sup> 11α-Methylhydrocortisone Acetate and 9α-Chloro-11α-Methylhydrocortisone Acetate

Beyler, Roger E.; Hoffman, Frances; Sarett, L. H.

doi:10.1021/ja01486a040

Anti‐Inflammatory Steroids

Avery

¹

,

Woolfrey

²

2003

Burger's Medicinal Chemistry and Drug Discovery

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We know today that structural changes in steroids can bring about potency alterations in animal pharmacology through a number of mechanisms. The processes that are affected include pharmacokinetic parameters such as drug absorption and drug distribution, as well as drug metabolism to more or less active metabolites. There is now a large body of literature dealing with these phenomena that makes predictive thinking possible in these areas. Other mechanisms that are involved in the effect of structural changes on pharmacological activity in steroids include the effect of steroid structure on receptor affinity and the manner in which changes in the steroid agonist affect intrinsic activity through alterations in gene expression. These and other concepts relating to anti‐inflammatory steroids are discussed in this chapter.

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Anti‐Inflammatory Glucocorticoids

Avery

¹

,

Chittiboyina

²

2010

Burger's Medicinal Chemistry and Drug Discovery

0

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Glucocorticoids are the first line medication used in the treatment of afflictions ranging from the moderate skin rash to severe acute inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand‐dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. The glucocorticoid receptor ( GR ) is a cytoplasmic protein of complex structure that is associated with various heat shock proteins (e.g., hsp 90). The desired immunosuppressive effect is apparently due largely to the downregulation of a variety of proinflammatory factors, whereas adverse reactions such as corticoid‐induced diabetes and osteoporosis could be connected to the inappropriate activation of genes involved in the control of metabolic processes. The discovery of selective receptor modulators, which maintain beneficial therapeutic activity together with a diminished risk of side effects, focuses on ligands that lead to repression rather than activation of genes targeted by the glucocorticoid receptor. Current drug‐screening programs have yielded a number of molecules including steroidal as well as nonsteroidal compounds, which preferentially induce receptor‐mediated repression.

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Anti‐Inflammatory Glucocorticoids

Avery¹,

Chittiboyina²

2021

Burger's Medicinal Chemistry and Drug Discovery

0

View full text Add to dashboard Cite

Glucocorticoids are the first line medication used in the treatment of afflictions ranging from the moderate skin rash to severe acute inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand‐dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. The glucocorticoid receptor ( GR ) is a cytoplasmic protein of complex structure that is associated with various heat shock proteins (e.g., hsp 90). The desired immunosuppressive effect is apparently due largely to the downregulation of a variety of proinflammatory factors, whereas adverse reactions such as corticoid‐induced diabetes and osteoporosis could be connected to the inappropriate activation of genes involved in the control of metabolic processes. The discovery of selective receptor modulators, which maintain beneficial therapeutic activity together with a diminished risk of side effects, focuses on ligands that lead to repression rather than activation of genes targeted by the glucocorticoid receptor. Current drug‐screening programs have yielded a number of molecules including steroidal as well as nonsteroidal compounds, which preferentially induce receptor‐mediated repression.

show abstract

Bismethylenedioxy Steroids. IV.¹ 11α-Methylhydrocortisone Acetate and 9α-Chloro-11α-Methylhydrocortisone Acetate

Cited by 13 publications

References 1 publication

Anti‐Inflammatory Steroids

Anti‐Inflammatory Steroids

Anti‐Inflammatory Glucocorticoids

Anti‐Inflammatory Glucocorticoids

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Bismethylenedioxy Steroids. IV.1 11α-Methylhydrocortisone Acetate and 9α-Chloro-11α-Methylhydrocortisone Acetate

Cited by 13 publications

References 1 publication

Anti‐Inflammatory Steroids

Anti‐Inflammatory Steroids

Anti‐Inflammatory Glucocorticoids

Anti‐Inflammatory Glucocorticoids

Contact Info

Product

Resources

About

Bismethylenedioxy Steroids. IV.¹ 11α-Methylhydrocortisone Acetate and 9α-Chloro-11α-Methylhydrocortisone Acetate