Abstract
Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD = human progesterone receptor ligand binding domain) cocrystal structure will also be presented.
MeSH terms
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Alkaline Phosphatase / metabolism
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Animals
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Area Under Curve
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Benzoxazines / chemical synthesis*
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Benzoxazines / chemistry
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Benzoxazines / pharmacology
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Binding, Competitive
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Cell Line, Tumor
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Contraceptive Agents, Female / chemical synthesis
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Contraceptive Agents, Female / chemistry
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Contraceptive Agents, Female / pharmacology
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Decidua / drug effects
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Decidua / metabolism
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Female
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Half-Life
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Humans
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In Vitro Techniques
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Ligands
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Molecular Structure
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Oxazines / chemical synthesis*
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Oxazines / chemistry
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Oxazines / pharmacology
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Protein Structure, Tertiary
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology
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Rats
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Rats, Sprague-Dawley
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Receptors, Progesterone / agonists*
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Receptors, Progesterone / antagonists & inhibitors
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Receptors, Progesterone / chemistry
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Structure-Activity Relationship
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Thiones / chemical synthesis*
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Thiones / chemistry
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Thiones / pharmacology
Substances
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Benzoxazines
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Contraceptive Agents, Female
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Ligands
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Oxazines
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Pyrroles
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Receptors, Progesterone
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Thiones
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tanoproget
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Alkaline Phosphatase