85 relations: Adenylyl cyclase, Aglepristone, Agonist, Agonist-antagonist, Alpha helix, Alternative splicing, Alzheimer's disease, Amine, Amino acid, Arginine, Asoprisnil, Asparagine, Cell nucleus, Coactivator (genetics), Conformational ensembles, Corepressor, Crystallography, Cushing's syndrome, Cyclic adenosine monophosphate, Dimethylamine, DNA, DNA-binding domain, Drug, Drug discovery, Electronegativity, Emergency contraception, Endometriosis, Endometrium, Epithelium, Exon, Female reproductive system, Follicular phase, G protein–coupled receptor, Glucocorticoid receptor, Glutamic acid, Glutamine, Heat shock protein, Heterocyclic compound, Hydrogen bond, Hydrophobe, Immunophilins, In vitro, Ketone, Lead compound, Leiomyoma, Leucine, Ligand (biochemistry), Luteal phase, Mammary gland, Membrane progesterone receptor, ..., Menstrual cycle, Metaplasia, Methionine, Mifepristone, N-terminus, Nuclear receptor, Nuclear receptor co-repressor 1, Nuclear receptor coregulators, Ovulation, Oxime, Phenylalanine, Phytoprogestogen, Progesterone, Progesterone receptor, Progestin, Protein, Protein domain, Protein isoform, Psychosis, Receptor antagonist, Reporter gene, Selective androgen receptor modulator, Selective estrogen receptor modulator, Selective glucocorticoid receptor modulator, Selective receptor modulator, Steroid, Steroid hormone receptor, Stroma of ovary, Structural analog, Tanaproget, Telapristone, Tissue (biology), Tyrosine, Ulipristal acetate, Uterine fibroid. Expand index (35 more) » « Shrink index
Adenylyl cyclase (also commonly known as adenyl cyclase and adenylate cyclase, abbreviated AC) is an enzyme with key regulatory roles in essentially all cells.
Aglepristone (brand name Alizine; former developmental code names RU-46534, RU-534) is a synthetic, steroidal antiprogestogen related to mifepristone which is marketed by Virbac in several European countries for use in veterinary medicine.
An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.
In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists).
The alpha helix (α-helix) is a common motif in the secondary structure of proteins and is a righthand-spiral conformation (i.e. helix) in which every backbone N−H group donates a hydrogen bond to the backbone C.
Alternative splicing, or differential splicing, is a regulated process during gene expression that results in a single gene coding for multiple proteins.
Alzheimer's disease (AD), also referred to simply as Alzheimer's, is a chronic neurodegenerative disease that usually starts slowly and worsens over time.
In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair.
Amino acids are organic compounds containing amine (-NH2) and carboxyl (-COOH) functional groups, along with a side chain (R group) specific to each amino acid.
Arginine (symbol Arg or R) is an α-amino acid that is used in the biosynthesis of proteins.
Asoprisnil (INN; developmental code name J-867) is a synthetic, steroidal selective progesterone receptor modulator that was under development by Schering and TAP Pharmaceutical Products for the treatment of uterine fibroids.
Asparagine (symbol Asn or N), is an α-amino acid that is used in the biosynthesis of proteins.
In cell biology, the nucleus (pl. nuclei; from Latin nucleus or nuculeus, meaning kernel or seed) is a membrane-enclosed organelle found in eukaryotic cells.
A coactivator is a type of transcriptional coregulator that binds to an activator (a transcription factor) to increase the rate of transcription of a gene or set of genes.
Conformational ensembles, also known as structural ensembles are experimentally constrained computational models describing the structure of intrinsically unstructured proteins.
In the field of molecular biology, a corepressor is a substance that inhibits the expression of genes.
Crystallography is the experimental science of determining the arrangement of atoms in crystalline solids (see crystal structure).
Cushing's syndrome is a collection of signs and symptoms due to prolonged exposure to cortisol.
Cyclic adenosine monophosphate (cAMP, cyclic AMP, or 3',5'-cyclic adenosine monophosphate) is a second messenger important in many biological processes.
Dimethylamine is an organic compound with the formula (CH3)2NH.
Deoxyribonucleic acid (DNA) is a thread-like chain of nucleotides carrying the genetic instructions used in the growth, development, functioning and reproduction of all known living organisms and many viruses.
A DNA-binding domain (DBD) is an independently folded protein domain that contains at least one structural motif that recognizes double- or single-stranded DNA.
A drug is any substance (other than food that provides nutritional support) that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes a temporary physiological (and often psychological) change in the body.
In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered.
Electronegativity, symbol ''χ'', is a chemical property that describes the tendency of an atom to attract a shared pair of electrons (or electron density) towards itself.
Emergency contraception (EC), or emergency postcoital contraception, are birth control measures that may be used after sexual intercourse to prevent pregnancy.
Endometriosis is a condition in which the endometrium, the layer of tissue that normally covers the inside of the uterus, grows outside of it.
The endometrium is the inner epithelial layer, along with its mucous membrane, of the mammalian uterus.
Epithelium is one of the four basic types of animal tissue, along with connective tissue, muscle tissue and nervous tissue.
An exon is any part of a gene that will encode a part of the final mature RNA produced by that gene after introns have been removed by RNA splicing.
The female reproductive system is made up of the internal and external sex organs that function in reproduction of new offspring.
The follicular phase is the phase of the estrous cycle, (or, in humans and great apes, the menstrual cycle) during which follicles in the ovary mature.
G protein–coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses.
The glucocorticoid receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind.
Glutamic acid (symbol Glu or E) is an α-amino acid with formula.
Glutamine (symbol Gln or Q) is an α-amino acid that is used in the biosynthesis of proteins.
Heat shock proteins (HSP) are a family of proteins that are produced by cells in response to exposure to stressful conditions.
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s).
A hydrogen bond is a partially electrostatic attraction between a hydrogen (H) which is bound to a more electronegative atom such as nitrogen (N), oxygen (O), or fluorine (F), and another adjacent atom bearing a lone pair of electrons.
In chemistry, hydrophobicity is the physical property of a molecule (known as a hydrophobe) that is seemingly repelled from a mass of water.
In molecular biology, immunophilins are endogenous cytosolic peptidyl-prolyl isomerases (PPI) that catalyze the interconversion between the cis and trans isomers of peptide bonds containing the amino acid proline (Pro).
In vitro (meaning: in the glass) studies are performed with microorganisms, cells, or biological molecules outside their normal biological context.
In chemistry, a ketone (alkanone) is an organic compound with the structure RC(.
A lead compound (i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by back-up compounds.
A leiomyoma, also known as fibroids, is a benign smooth muscle tumor that very rarely becomes cancer (0.1%).
Leucine (symbol Leu or L) is an essential amino acid that is used in the biosynthesis of proteins.
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose.
The luteal phase is the latter phase of the menstrual cycle (in humans and a few other animals) or the earlier phase of the estrous cycle (in other placental mammals).
A mammary gland is an exocrine gland in mammals that produces milk to feed young offspring.
Membrane progesterone receptors (mPRs) are a group of cell surface receptors and membrane steroid receptors belonging to the progestin and adipoQ receptor (PAQR) family which bind the endogenous progestogen and neurosteroid progesterone, as well as the neurosteroid allopregnanolone.
The menstrual cycle is the regular natural change that occurs in the female reproductive system (specifically the uterus and ovaries) that makes pregnancy possible.
Metaplasia ("change in form") is the reversible transformation of one differentiated cell type to another differentiated cell type.
Methionine (symbol Met or M) is an essential amino acid in humans.
Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol, to bring about an abortion.
The N-terminus (also known as the amino-terminus, NH2-terminus, N-terminal end or amine-terminus) is the start of a protein or polypeptide referring to the free amine group (-NH2) located at the end of a polypeptide.
In the field of molecular biology, nuclear receptors are a class of proteins found within cells that are responsible for sensing steroid and thyroid hormones and certain other molecules.
The nuclear receptor co-repressor 1 also known as thyroid-hormone- and retinoic-acid-receptor-associated co-repressor 1 (TRAC-1) is a protein that in humans is encoded by the NCOR1 gene.
Nuclear receptor coregulatorsThis article is based on the transcript of an animated course on the Nuclear Receptor Signaling Atlas (NURSA) website entitled "Nuclear receptor signaling: concepts and models".
Ovulation is the release of eggs from the ovaries.
An oxime is a chemical compound belonging to the imines, with the general formula R1R2C.
Phenylalanine (symbol Phe or F) is an α-amino acid with the formula.
Phytoprogestogens, also known as phytoprogestins, are phytochemicals (that is, naturally occurring, plant-derived chemicals) with progestogenic effects.
Progesterone (P4) is an endogenous steroid and progestogen sex hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species.
The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells.
A progestin is a type of medication which is used most commonly in hormonal birth control and menopausal hormone therapy.
Proteins are large biomolecules, or macromolecules, consisting of one or more long chains of amino acid residues.
A protein domain is a conserved part of a given protein sequence and (tertiary) structure that can evolve, function, and exist independently of the rest of the protein chain.
A protein isoform, or "protein variant" is a member of a set of highly similar proteins that originate from a single gene or gene family and are the result of genetic differences.
Psychosis is an abnormal condition of the mind that results in difficulties telling what is real and what is not.
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.
In molecular biology, a reporter gene (often simply reporter) is a gene that researchers attach to a regulatory sequence of another gene of interest in bacteria, cell culture, animals or plants.
Selective androgen receptor modulators or SARMs are a novel class of androgen receptor ligands.
Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER).
Selective glucocorticoid receptor modulators (SEGRMs) and selective glucocorticoid receptor agonists (SEGRAs) formerly known as dissociated glucocorticoid receptor agonists (DIGRAs) are a class of experimental drugs designed to share many of the desirable anti-inflammatory, immunosuppressive, or anticancer properties of classical glucocorticoid drugs but with fewer side effects such as skin atrophy.
In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues.
A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration.
Steroid hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells.
The stroma of the ovary is a unique type of connective tissue abundantly supplied with blood vessels, consisting for the most part of spindle-shaped stroma cells.
A structural analog, also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component.
Tanaproget (INN; developmental code names NSP-989, WAY-166989) is an investigational nonsteroidal progestin.
Telapristone, as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids.
In biology, tissue is a cellular organizational level between cells and a complete organ.
Tyrosine (symbol Tyr or Y) or 4-hydroxyphenylalanine is one of the 20 standard amino acids that are used by cells to synthesize proteins.
Ulipristal acetate, sold under the brand name Ella among others, is a medication used for emergency birth control and uterine fibroids.
Uterine fibroids, also known as uterine leiomyomas or fibroids, are benign smooth muscle tumors of the uterus.
Discovery and Development of Selective progesterone receptor modulators, Discovery and development of selective progesterone receptor modulators, Selective Progesterone Receptor Modulators, Selective progesterone receptor modulators.