Loading...
*  BacMam
Coupled Receptor Drug Discovery". Receptors and Channels. 10 (3-4): 99-107. doi:10.1080/10606820490514969. PMID 15512844. Ames ... Coupled Receptors in U-2 OS Osteosarcoma Cells". Receptors and Channels. 10 (3-4): 117-124. doi:10.1080/10606820490515012. PMID ... including several of the genes involved in Toll-like receptor signaling pathway and cytokine-cytokine receptor interaction. ... Drug Discov. 2 (12): 1669-1681. doi:10.1517/17460441.2.12.1669. PMID 23488908. Distelmaier, Felix; Koopman, Werner J. H.; Testa ...
*  Edith Bülbring
1-13 In: "Drug Receptors", ed. H.P. Rang. Macmillan London. Possible mechanism of the action of catecbolamines on smooth muscle ... She used this preparation later on in her studies of drug action (published in 1930). After the death of her mentor, Paul ... 1972 Recent developments in the study of drug action on cellular mechanisms ill smooth muscle. International Congress of ...
*  Pepducin
New Insights into G-protein Coupled Receptor Drug Development". J Biol Chem. 287: 12787-96. doi:10.1074/jbc.r112.355461. PMC ... Pepducins employ lipidated fragments of intracellular G protein-coupled receptor loops to modulate GPCR action in targeted cell ... Kuliopulos A, Covic L (December 2003). "Blocking receptors on the inside: pepducin-based intervention of PAR signaling and ... Pepducins are cell-penetrating peptides that act as intracellular modulators of signal transference from receptors to G ...
*  Jennifer L. Martin
"Functional group contributions to drug-receptor interactions". J Med Chem. 27: 1648-57. doi:10.1021/jm00378a021. PMID 6094812. ... In 2016, Martin was appointed Director of the Eskitis Drug Discovery Institute at Griffith University, which hosts unique drug ... Eskitis Drug Discovery Institute "Leading scientist to head Griffith's Eskitis Institute". Retrieved 2016-10-23. "Prof Jenny ... "Glucose analogue inhibitors of glycogen phosphorylase: the design of potential drugs for diabetes". Biochemistry. 30: 10101-16 ...
*  GABRD
"GABAA receptor drugs and neuronal plasticity in reward and aversion: focus on the ventral tegmental area". Frontiers in ... For this reason, receptors containing δ-subunits are sometimes referred to as "benzodiazepine insensitive" GABAA receptors. The ... The most common GABAA receptors have the gamma subunit, which allows the receptor to bind benzodiazepines. ... Gamma-aminobutyric acid receptor subunit delta is a protein that in humans is encoded by the GABRD gene. γ-Aminobutyric acid ( ...
*  Multi-wavelength anomalous dispersion
... drug receptors) via solution of the phase problem. MAD was developed by Wayne Hendrickson while working as a postdoctoral ...
*  ZM-182345
Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 209-. ISBN 978-3- ...
*  Pipendoxifene
ISBN 978-1-60805-496-1. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons ... Selective Estrogen Receptor Modulators: A New Brand of Multitarget Drugs. Springer Science & Business Media. pp. 58-. ISBN 978- ... The drug reached phase II clinical trials before its development was discontinued. It was synthesized at the same time as ... Pipendoxifene (INN) (developmental code name ERA-923) is a nonsteroidal selective estrogen receptor modulator (SERM) that was ...
*  Droloxifene
Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 153-. ISBN 978-3-527-62330-3. Vincent T. Devita; Samuel Hellman; ... The drug was found to be significantly less effective than tamoxifen in the treatment of breast cancer in two phase III ... 298-. ISBN 978-1-59259-699-7. J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and ... adisinsight.springer.com/drugs/800000847+&cd=1&hl=en&ct=clnk&gl=us Eckhard Ottow; Hilmar Weinmann (8 September 2008). ...
*  ERB-196
52-. ISBN 978-1-4816-8771-3. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... The drug was under development by Wyeth for the treatment of inflammation and sepsis starting in 2004 but development was ... 8β-VE2 Diarylpropionitrile FERb 033 Prinaberel WAY-166818 WAY-200070 WAY-214156 R. E. Hubbard (2006). Structure-based Drug ... a selective estrogen receptor-beta agonist, protects against death in experimental septic shock". Crit. Care Med. 34 (8): 2188- ...
*  Fispemifene
52-. ISBN 978-3-540-34742-2. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... Selective Estrogen Receptor Modulators: A New Brand of Multitarget Drugs. Springer Science & Business Media. pp. ... The drug failed to achieve statistical significance on key effectiveness endpoints in clinical trials and was discontinued by ... Fispemifene (INN, USAN) (developmental code name HM-101) is a nonsteroidal selective estrogen receptor modulator (SERM) of the ...
*  Propylpyrazoletriol
Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50-. ISBN 978-3-527-62330-3. Tony M. Plant; Anthony J. Zeleznik (15 ... 220-. ISBN 978-1-4649-9741-9. Synthesis of Non-steroidal Estrogen Receptor Proteolysis Targeting Chimeric Molecules (PROTACS). ... 2311-. ISBN 978-0-12-397769-4. Cytoplasmic and Nuclear Receptors-Advances in Research and Application: 2012 Edition. ...
*  Sergio A. Lira
Gerd Folkers; Martine J. Smit; Sergio A. Lira; Leurs, Rob; Raimund Mannhold; Hugo Kubinyi (2010). Chemokine Receptors as Drug ... CS1 maint: Multiple names: authors list (link) "Wiley::Chemokine Receptors as Drug Targets". Retrieved April 26, 2011. "Mount ... 2005). "The chemokine receptor D6 limits the inflammatory response in vivo". Nat Immunol. 6 (4): 403-411. doi:10.1038/ni1182. ... 2007). "Lymphotoxin beta receptor signaling is required for inflammatory lymphangiogenesis in the thyroid". Proc Natl Acad Sci ...
*  Penicillium oblatum
Eckhard Ottow; Hilmar Weinmann (2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. ISBN 3-527-62330-2. Zbigniew J. ...
*  Mespirenone
Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 410-. ISBN 978-3- ... The drug was under development by Schering (now Bayer Schering Pharma) and reached phase II clinical trials but was ... Canrenone Drospirenone Spironolactone J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, ...
*  Antiestrogen
977-. ISBN 978-0-7817-4868-1. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production. Antiestrogens are one of ... ISBN 978-1-84816-959-3. Walter Sneader (23 June 2005). Drug Discovery: A History. John Wiley & Sons. pp. 198-199. ISBN 978-0- ... Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like ...
*  Sodelglitazar
Eckhard Ottow, Hilmar Weinmann (2008). Nuclear Receptors as Drug Targets. Wiley. pp. 380-. ISBN 978-3-527-31872-8. Retrieved 2 ... While it is primarily active at the PPARδ receptor, it is considered a pan agonist with activity at PPARα and PPARγ receptors. ... Elafibranor GW0742 GW501516 MBX-8025 Peroxisome proliferator-activated receptor US Patent No. 7105551 "96 dpi image of original ... Sodelglitazar, formerly known as GW 677954, is a thiazole PPARδ receptor agonist developed by GlaxoSmithKline. ...
*  Methylpiperidinopyrazole
11-. ISBN 978-0-549-90990-3. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... 220-. ISBN 978-1-4649-9741-9. Synthesis of Non-steroidal Estrogen Receptor Proteolysis Targeting Chimeric Molecules (PROTACS). ... 2311-. ISBN 978-0-12-397769-4. Cytoplasmic and Nuclear Receptors-Advances in Research and Application: 2012 Edition. ... and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor. It has 200- ...
*  Miproxifene phosphate
251-. ISBN 978-1-59259-768-0. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... The drug is a phosphate ester and prodrug of miproxifene (DP-TAT-59) with improved water solubility that was better suited for ... 90-. ISBN 978-3-527-62330-3. Kristian Stromgaard; Povl Krogsgaard-Larsen; Ulf Madsen (19 August 2016). Textbook of Drug Design ... Miproxifene phosphate (former developmental code name TAT-59) is a nonsteroidal selective estrogen receptor modulator (SERM) of ...
*  Miproxifene
251-. ISBN 978-1-59259-768-0. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... The drug has been found to be 3- to 10-fold more potent than tamoxifen in inhibiting breast cancer cell growth in in vitro ... Miproxifene (INN) (former developmental code name DP-TAT-59) is a nonsteroidal selective estrogen receptor modulator (SERM) of ... 90-. ISBN 978-3-527-62330-3. Kristian Stromgaard; Povl Krogsgaard-Larsen; Ulf Madsen (19 August 2016). Textbook of Drug Design ...
*  Trimegestone
Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 208-. ISBN 978-3-527-62330-3. Annual Reports in Medicinal Chemistry. ... Trimegestone has very high affinity for the progesterone receptor, only weak affinity for the mineralocorticoid receptor, and ... Trimegestone is the generic name of the drug and its INN, USAN, and BAN, while trimégestone is its DCF. Trimegestone is ... Unlike progesterone, trimegestone does not metabolize into neurosteroids and hence does not influence GABAA receptor signaling ...
*  Antiandrogen
Mateo J, Smith A, Ong M, de Bono JS (2014). "Novel drugs targeting the androgen receptor pathway in prostate cancer". Cancer ... Shen, Howard C.; Taplin, Mary-Ellen; Balk, Steven P. (2010). "Androgen Receptor Antagonists". Drug Management of Prostate ... 233-. ISBN 978-1-4471-2086-5. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley ... There are several different varieties of antiandrogens, including the following: Androgen receptor antagonists: drugs that bind ...
*  Tachyphylaxis
Ličko V (1985). "Drugs, Receptors and Tolerance". Pharmacokinetics and Pharmacodynamics of Psychoactive Drugs. pp. 311-322. ... sudden decrease in response to a drug after its administration, i.e. a rapid and short-term onset of drug tolerance. It can ... Increasing the dose of the drug may be able to restore the original response. Tachyphylaxis is characterized by the rate ... July 2000). "The effect of polymorphisms of the beta(2)-adrenergic receptor on the response to regular use of albuterol in ...
*  Chemical specificity
For example, the basis that drugs must successfully be proven to accomplish is both the ability to bind the target receptor in ... "drug_receptor_theory [TUSOM , Pharmwiki]". tmedweb.tulane.edu. Retrieved 2016-06-11. Maity, Biswanath; Sheff, David; Fisher, ... Drugs depend on the specificity of the designed molecules and formulations to inhibit particular molecular targets. Novel drug ... Specificity is important for novel drug discovery and the field of clinical research, with new drugs being tested for its ...
*  Enthalpy-entropy compensation
In drug receptor binding, it has been suggested that enthalpy-entropy compensation arises due to an intrinsic property of ... Gilli, P.; Ferretti, V.; Gilli, G.; Borea, P. A. Enthalpy-Entropy Compensation in Drug-Receptor Binding. J. Phys. Chem. 1994, ...