Affinity-based selection

Exploring the leucine-proline binding pocket of the Src SH3 domain using structure-based, split-pool synthesis and affinity-based selection. /. Am. Chem. Soc. 1998, 120, 30-36. 

Exploring the Leucine-Proline Binding Pocket of the Sre SH3 Domain Using Structure-Based, Split-Pool Synthesis and Affinity-Based Selection. 

To date, many examples successfully employing DEL technology to discover small molecules against biological targets of therapeutic interests have been reported (Table 10.1). As affinity-based selection technologies do not require screening assays and as multiple selection conditions can be applied (i.e.,... 

The cucurbit [n]uril family (CB[n]) of molecular containers possess remarkable binding affinities and selectivities (Ka values up to 1012M-1, Krei values up to 106) which renders them useful as a component of molecular machines, sensors, and biomimetic systems (123-125). Recently, Wagner and coworkers have reported (126) that CB[10] - with its spacious 870A3 cavity - is capable of acting as a host for free base and metalated tetra (Af-methylpyridinium)porphyrins 19a-d (Fig. 17). Despite the large ellipsoidal deformation of CB[10] upon complexation, the complexed porphyrins retain their fundamental UV/VIS, fluorescence, and electrochemical properties. The CB[ 10] porphyrin... 

Class 3 fluorophores linked, via a spacer or not, to a receptor. The design of such sensors, which are based on molecule or ion recognition by a receptor, requires special care in order to fulfil the criteria of affinity and selectivity. These aspects are relevant to the field of supramolecular chemistry. The changes in photophysical properties of the fluorophore upon interaction with the bound analyte are due to the perturbation by the latter of photoinduced processes such as electron transfer, charge transfer, energy transfer, excimer or exciplex formation or disappearance, etc. These aspects are relevant to the field of photophysics. In the case of ion recognition, the receptor is called an ionophore, and the whole molecular sensor is... 

Siddiqui, A., Alaoui-Ismaili, M.H. Identification of novel and selective Akt-1 inhibitors using affinity-based screening of both basal and activated forms of Akt-1. Am. Assoc. Cancer Res. 

Due to the strong and selective binding that characterizes many affinity ligands, solutes that are analyzed or purified with these ligands can often be separated with little or no interferences from other sample components. In many cases, the solute of interest can be isolated in only one or two steps, with purification yields of hundred- to several thousandfold being common [2,4-6]. In work with hormone receptors, purification yields approaching one millionfold have even been reported with affinity-based separations [5]. 

The actions of cAMP are terminated by phosphodiesterases (PDEs) that catalyze the breakdown of cAMP to 5 -AMP (Diunan and Nestler 1999). There are at least 11 different forms of PDEs that are characterized based on their affinity and selectivity for cAMP, as well as cGMP. In addition, the PDEs are differentially regulated by the cyclic nucleotides themselves, by phosphorylation, and by increased expression of certain splice variants (e.g., some isoforms are... 

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