Ligand selectivity

The development of ligands selective for individual receptor subtypes relevant to a targeted disease could decrease these toxic effects thereby improving the therapeutic index. Two new arotinoids are already available for topical use in skin diseases. These are tazarotenic acid (tazarotene) and 6-[3-(l-adamanty 1)-... 

Mergny JL et al. (2001) Telomerase inhibitors based on quadruplex ligands selected by a fluorescence assay. Proc Natl Acad Sci USA 98(6) 3062-3067... 

Complexes of tetravalent zirconium and ligands selected from organic acids such as citric, tartaric, malic, and lactic acid and a complex of aluminum and citric acid are suitable as dispersants [288-291]. This type of dispersant is especially useful in dispersing bentonite suspensions. The muds can be used at pH values ranging from slightly acidic to strongly basic. 

Tian Y, New DC, Yung LY, et al. Differential chemokine activation of CC chemokine receptor 1-regulated pathways ligand selective activation of Galpha 14-coupled pathways. Eur J Immunol 2004 34(3) 785-795. 

Kenakin T., Inverse, protean, and ligand-selective agonism matters of receptor conformation, FASEB J., 15(3), 598-611, 2001. 

The preparative potential of silyl- or stannyl-substituted polynuclear complexes is currently far from being exploited. Due to the reactivity of silyl ligands, selective cleavage of metal-silicon bonds is possible. In some cases this was observed during the reaction of an anionic silyl complex with metal... 

The use of single-site initiators for the polymerization of acrylates is attractive, since steric protection of the metal center should eliminate the unwanted side reactions described above, allowing living polymerization systems to be developed. Further, stereocontrol may be achievable by appropriate ligand selection. 

Whereas ligand selection for the biphasic water-organic and the induced phase separation system are somewhat limited, there is very wide array of organophosphorus... 

We have delineated viable coordinated ligand reactions and their attendant intermediates for the stoichiometric conversion of CO ligands selectively to the C2 organics ethane, ethylene, methyl (or ethyl) acetate, and acetaldehyde. We now outline results from three lines of research (1) T -Alkoxymethyl iron complexes CpFe(C0)2CH20R (2) are available by reducing coordinated CO on CpFe(C0)3+ (1) [Cp = r -CsHs]. Compounds 2 then form t -alkoxyacetyl complexes via migratory-insertion (i,e. CO... 

Hogner, A., Kastrup, J. S Jin, R., Liljefors, T Mayer, M. L., Egebjerg, J., et al. (2002) Structural basis for AMPA receptor activation and ligand selectivity crystal structures of five agonist complexes with the GluR2 binding core../. Mol. Biol. 322,93-109. 

These workers have also investigated the use of pyridyl bis(pyrazoles) as ligands. Selectivities are modest with Cu(I) although a Rh(III) precatalyst affords better results (68). The hydrido tris(pyrazolyl)borate (97) provides slightly better results (69). Although diastereoselectivity is still poor, enantioselectivities are improved. Importantly, these ligands favor the formation of the cis isomer. 

Scheme 10.1S. Dummy ligands selective transfer of the methyl (or alkyl, alkenyl, aryl) group in preference to transfer of the alkynyl group.

Y. M. Dunayevskiy, J.-J. Lai, C. Quinn, F. Talley, P. Vouros Mass spectrometric identification of ligands selected from combinatorial libraries using gel filtration. Rapid Commun. Mass Spectrom. 1997, 11, 1178-1184. 

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