Ligand-target

Figure 15.3 Annotated ligand-target knowledge space.

Figure 1 A schematic conceptualization of the three-compartment model of CNS penetration demonstrating the importance of intercompartmental unbound compound concentration relationships to target pharmacology interactions [21,22,25-28]. An exaggerated synapse is shown in the brain compartment to emphasize the locale of transmembrane proteins (squares) versus intracellular (oval) targets, and the matrix compound concentrations dictating their respective ligand-target interactions.

Thomas M, Kularatne S A, Qi L, Kleindl P, Leamon CP, Hansen MJ, Low PS (2009) Ligand-targeted delivery of small interfering RNAs to malignant cells and tissues. Ann N Y Acad Sci 1175 32-39... 

Schiffelers RM, Ansari A, Xu J, Zhou Q, Tang Q, Storm G, Molema G, Lu PY, Scaria PV, Woodle MC (2004) Cancer siRNA therapy by tumor selective delivery with ligand-targeted sterically stabilized nanoparticle. Nucleic Acids Res 32 el49... 

Leserman, L., and Machy, P. (1987) Ligand targeting of liposomes. In Liposomes From Biophysics to Therapeutics (M.J. Ostro, ed.), pp. 157-194. Dekker, New York. 

Receptor-Based Subtype Pharmacophore and Ligand-Target/Antitarget Interaction-Based QSAR... 

Among chemical-physics properties, lipophilicity is certainly a key parameter to understand and predict absorption, distribution, metabolism, excretion, and toxicity (ADMET) of NCE furthermore, it contributes to model ligand-target interactions underlying the pharmacodynamic phase [15],... 

Noble CA, Kirpotin DB, Hayes ME, et al. Development of ligand-targeted liposomes for cancer therapy. Expert Opin Ther Targets 2004 8 335-353. 

Forssen E, Willis M. Ligand-targeted liposomes. Adv Drug Deliver Rev 1998 29 249. 

Allen TM. Ligand-targeted therapeutics in anticancer therapy. Nat Rev Cancer 2002 2 750. 

Sapra P, Allen TM. Ligand-targeted liposomal anticancer drugs. Prog Lipid Res 2003 42 439. 

Carlomagno T (2005) Ligand-target interactions what can we learn from NMR Annu Rev Biophys Biomol Struct 34 245... 

A further characteristic of ligand-target interaction is the dissociation rate constant. Dissociation experiments are not only an important criterion for the establishment of binding assays, they also can show the reversibility of the specific marker binding at the target [16], which is usually verified by dissociation experiments (see also Section 7.2.1). In the MS binding assays presented here, GABA was used as a competitor to initiate dissociation. The experiment was then termi-... 

Name of ligand Type of ligand Target and applicability Reference... 

Like many other typical bacterial secondary metabolites, AGAs tend to be produced as complex product mixtures released from their producing cells. We interpret this as a strong sign for ongoing evolution of the respective pathways and ligand-target site interactions. In other words the biochemical interactions... 

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