Dr. Lapinsky - Estrogens And Progestins Section

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Across
  1. 3. Anastrozole and Letrozole are non-covalent, reversible aromatase inhibitors that contain a triazole ring that functions to chelate the ________ atom within aromatase such that it can no longer hold a molecule of ______ as a chemical reagent
  2. 7. the brand name of an injectable form of Medroxyprogesterone Acetate that is used as a method of birth control and as a part of menopausal hormone therapy
  3. 8. oftentimes you find the term "nor" within the chemical names of specific drugs or drug classes (e.g., 19-nor-androstanes, Norethindrone), wherein "nor" means _________
  4. 11. a prototype progesterone antagonist that was developed by adding bulk to a 19-nor-androstane, thus creating a controversial abortifacient
  5. 13. a selective estrogen receptor degrader (SERD) that works by binding to the ER and destabilizing it, thus causing the cell's normal protein degradation processes via the proteasome to destroy the drug•ER complex
  6. 14. the rod part of the estrogen receptor that folds over towards creating a pharmacologically active ER agonist•ER complex
  7. 17. ___________ symptoms, commonly called hot flashes or flushes and night sweats, are the menopausal symptoms for which women seek treatment with ER agonists during menopause, most often
  8. 18. this steroid is not only an essential component of cell membranes but also serves as the starting material to synthesize estrogens, progestins, androgens, and adrenocorticoids
  9. 19. the principal enzyme required for prodrug activation of Premarin that is also currently being investigated as a drug target for future treatment of estrogen-dependent breast cancer
  10. 20. oftentimes counting the number of carbons in a steroid can give you a quick sense of that steroid compound's ______________ class
  11. 21. oftentimes a basic bulky amine is added to the structure of an ER agonist to create a Selective Estrogen Receptor _______________
  12. 22. a vaginal tablet form of Estradiol that should NOT be taken orally to manage vaginal symptoms associated with menopause
  13. 23. a prototype non-steroidal estrogen receptor agonist that represents one of the most famous examples of rational medicinal chemistry drug design
Down
  1. 1. despite being C18 estranes, 19-nor-androstanes lack an ________________, which is the critical structural feature that is required for binding of an agonist to the ER
  2. 2. Premarin is one example of a drug class called CEEs, which stands for ______ ________ Estrogens
  3. 4. in the language of steroids, the terms "alpha" and "beta" refer to the _______ of a particular carbon atom within a steroid compound
  4. 5. the active metabolite of this SERM predominantly functions as an ER in the hypothalamus to treat infertility
  5. 6. 17-beta HSD is the enzyme responsible for catalyzing the metabolic ___________ of Estradiol to Estrone
  6. 9. a natural endogenous C19 compound that functions to "maintain a pregnancy", inhibits ovulation during pregnancy, and is also responsible for signaling normal menstrual bleeding in females
  7. 10. an irreversible, steroidal aromatase inactivator that acts as a false substrate for aromatase, and is processed to an intermediate that binds irreversibly to the active site of aromatase causing its inactivation, an effect also known as "suicide inhibition"
  8. 12. Fluoxetine and Paroxetine should NOT be used to manage hot flashes/night sweats associated with Tamoxifen, namely because the former drugs prevent ___________________ of Tamoxifen
  9. 15. the most common ER agonist found in oral contraceptives that was created by replacing the 17-hydrogen atom in Estradiol with a two-carbon triple-bonded functional group
  10. 16. the enzyme for creating the critical structural feature found in all ER agonists, namely by removing the C19 methyl group from endogenous androgen receptor agonists