• modulators
  • The progesterone active metabolites 5α-dihydroprogesterone, also a progestogen, and allopregnanolone, which are positive allosteric modulators of the GABAA receptor, have been found to rapidly influence sexual receptivity and behavior in mice, actions that are GABAA receptor-dependent. (wikipedia.org)
  • In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. (wikipedia.org)
  • androgen
  • The finding of androgen receptors (AR) as a potential target in breast. (bio-medicine.org)
  • Evidence presented at the AACR Annual Meeting 2013 adds a fourth: androgen receptors. (bio-medicine.org)
  • This is a continuing line of work with all evidence pointing toward the addition of the androgen receptor as potential target and useful marker in all of the major subtypes of breast cancer," says Jennifer Richer, PhD, investigator at the University of Colorado Cancer Center and co-director of the CU Cancer Center Tissue Processing and Procurement Core. (bio-medicine.org)
  • acetate
  • We have recently shown, by using a medroxyprogesterone acetate (MPA)-induced murine breast cancer model ( 2 ), that fibroblast growth factor 2 (FGF2) is highly expressed in the stroma of hormone-independent carcinomas and that the FGF receptor (FGFR) inhibitor PD173074 decreased tumor growth ( 3 ). (aacrjournals.org)
  • vitro
  • Basal phosphorylation on Ser-81, Ser-162, Ser-190 and Ser-400 is increased in response to progesterone and can be phosphorylated in vitro by the CDK2-A1 complex. (abcam.com)
  • PR is expressed as two proteins (PRA and PRB) with different functions, and in vitro evidence reveals PRA to inhibit PRB function, so the cellular ratio of PRA:PRB is likely to be an important determinant of progesterone action. (aacrjournals.org)
  • For example, progesterone (or sometimes dydrogesterone or hydroxyprogesterone caproate) is used for luteal support in in-vitro fertilization protocols. (wikipedia.org)
  • progestogens
  • They are one of three types of sex hormone agonists, the others being androgens/anabolic steroids like testosterone and progestogens like progesterone. (wikipedia.org)
  • It might also interact with hormonal contraceptives and progestogens such as levonorgestrel and other substrates of the progesterone receptor, as well as with glucocorticoids. (wikipedia.org)
  • Progestogens, also sometimes spelled progestagens or gestagens, are a class of steroid hormones that bind to and activate the progesterone receptor (PR). (wikipedia.org)
  • In the first step in the steroidogenic pathway, cholesterol is converted into pregnenolone, which serves as the precursor to the progestogens progesterone and 17α-hydroxyprogesterone. (wikipedia.org)
  • Progestogens, including both progestins and progesterone, are used medically in hormonal contraception, hormone therapy, in the treatment of gynecological disorders, and for other indications. (wikipedia.org)
  • Targets
  • This study represents the first demonstration of a nuclear interaction between FGFR-2 and STAT5, as PR coactivators at the DNA progesterone responsive elements, suggesting that FGFRs are valid therapeutic targets for human breast cancer treatment. (aacrjournals.org)
  • antagonistic
  • and especially after the discovery of its receptor in 1970 there has been a significant interest in developing an antagonistic agent for therapeutic use. (wikipedia.org)
  • GABAA
  • Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chlorine ions into the neuron, making the cell hyperpolarized and less likely to fire. (wikipedia.org)
  • In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. (wikipedia.org)
  • The GABAA receptors have historically been a target of drug treatment research. (wikipedia.org)
  • Benzodiazepines function by binding to the benzodiazepine site on most, but not all, GABAA receptors. (wikipedia.org)
  • The GABAA receptors are made up of subunits which form a receptor complex. (wikipedia.org)
  • The most common complex that includes around 40% of the GABAA receptors is the α1β2γ2 combination. (wikipedia.org)
  • For example, the binding site of neurosteroids in the GABAA receptor is not known and barbiturates bind at a beta subunit that is distinct from the benzodiazepine binding site. (wikipedia.org)