Compounds that bind

A number of promising approaches have emerged in the eady to mid-1980s that may ultimately provide an agent. In general these approaches have focused on compounds that bind to the platelet glycoprotein (GP) Ilb/Ilia receptor. This receptor on the platelet surface is responsible for its binding to... 

Although estrone and estradiol (26) have both been isolated from human urine, it has recently been shown that it is the latter that is the active compound that binds to the so-called estrogen receptor protein. Reduction of estrone with any of a large number of reducing agents (for example, any of the complex metal hydrides) leads cleanly to estradiol. This high degree of stereoselectivity to afford the product of attack at the alpha side of the molecule is characteristic of many reactions of steroids. 

Bryostatins are another class of compounds that bind to the Cl domain and result in acute activation of PKC. However, unlike phorbol esters, these marine natural products have antitumor effects. Bryostatins are currently in phase II clinical trials and show promise as anticancer drugs, particularly when combined with other adjuvant therapy. 

Screening of a compound library to detect compounds that bind to the active site of the protein by correlation spectroscopy. 

Screening for a second compound that binds in the vicinity of the fust one using the same procedure. 

Clomiphene (Clomid) is a synthetic nonsteroidal compound that binds to estrogen receptors, decreasing the amount of available estrogen receptors and causing the anterior pituitary to increase secretion of FSH and LH. It is used to induce ovulation in anovulatory (nonovulating) women. 

Figure 19.7 The activity spectrum for different generic groups of compounds that bind to the benzodiazepine domain on the GABAa receptor...

A compound that binds at a different site to the natural receptor and produces a conformational distortion that prevents receptor activation. 

Meneghini R. 1974. Repair replication of opossum lymphocyte DNA Effect of compounds that bind to DNA. Chem Biol Interact 8 113-126. 

Phytoestrogens are a diverse group of polyphenolic non-steroidal plant compounds that bind to human estrogen receptors (Cos et al., 2003). The best studied of these compounds are the isoflavones, the phytoestrogens present in soy and red clover. 

Espeseth, A.S., Xu, M., Huand, Q., et al. (2005) Compounds that bind APP and inhibit AP processing in vitro suggest a novel approach to Alzheimer disease therapeutics. J. Biol. Chem., 280, 17792-17797. 

The treatment of metal poisoning is to administer a compound that binds the metal ion more strongly than does the group in the active centre of the enzyme. These compounds are known as chelating agents. For lead, the compound ethyl-enediaminetetraacetic acid (EDTA) is used. For mercury, dimercaptopropanol (dimercaprol) is used. 

A secondary screen for compounds that bind non-covalently to estrogen receptor (ER, MW 67 kDa) was evaluated and illustrated for 17yS-estradiol (Ka 1 nM,... 

About 32 000 compounds were screened to identify compounds that bind non-covalently to RGS4 using the GPC spin column/ESI-MS methodology and 1720 compounds were identified to bind (including very weak binders) to RGS4 [15],... 

As a follow-up to the RGS4 primary screen, the GPC spin column/ESI-MS methodology was applied to a selected series of seven RGS4 drug candidates to identify those compounds that bind non-covalently to RGS4 and not to G alpha [24]. Three ESI-MS experiments were performed with each of the compounds. 

ALIS reports only compounds that bind directly to the target of interest, preventing false positives that arise from off-target activity or interactions with substrates or other reagents. Since ALIS directly identifies bound components by MS, the incidence of false positives based on bulk effects and non-specific binding is lower than that of biochemical assays that yield a secondary readout of activity. 

Fig. 4.4 Scheme of pulsed ultrafiltration-mass spectrometry (PUF-MS) to screen chemical mixtures for compounds that bind to a macromolecular receptor. The ultrafiltration membrane traps a receptor in solution, but allows low molecular weight... 

Woods V.L. Jr Methods for identifying hot-spot residues of binding proteins and small compounds that bind to the same. U.S. Patent 6 599 707, 2003. 

A compound that binds to an ion in a manner which greatly facihtates the bound ion s permeabihty across a membrane. Naturally occurring ionophores include both mobile carriers (e.g., valinomycin and nigericin) and channel formers (e.g., gramicidin A). 

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