Discovering high-affinity ligands for proteins: SAR by NMR.

by: SB Shuker, PJ Hajduk, RP Meadows, SW Fesik

Science, Vol. 274, No. 5292. (29 November 1996), pp. 1531-1534.

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摘要

A nuclear magnetic resonance (NMR)-based method is described in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands. The approach is called "SAR by NMR" because structure-activity relationships (SAR) are obtained from NMR. With this technique, compounds with nanomolar affinities for the FK506 binding protein were rapidly discovered by tethering two ligands with micromolar affinities. The method reduces the amount of chemical synthesis and time required for the discovery of high-affinity ligands and appears particularly useful in target-directed drug research.

@article{citeulike:838515, abstract = {A nuclear magnetic resonance (NMR)-based method is described in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands. The approach is called "SAR by NMR" because structure-activity relationships (SAR) are obtained from NMR. With this technique, compounds with nanomolar affinities for the FK506 binding protein were rapidly discovered by tethering two ligands with micromolar affinities. The method reduces the amount of chemical synthesis and time required for the discovery of high-affinity ligands and appears particularly useful in target-directed drug research.}, address = {Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA.}, author = {Shuker, S. B. and Hajduk, P. J. and Meadows, R. P. and Fesik, S. W. }, citeulike-article-id = {838515}, doi = {http://dx.doi.org/10.1126/science.274.5292.1531}, issn = {0036-8075}, journal = {Science}, keywords = {nmr, sar}, month = {November}, number = {5292}, pages = {1531--1534}, posted-at = {2007-11-04 07:24:55}, priority = {2}, title = {Discovering high-affinity ligands for proteins: SAR by NMR.}, url = {http://dx.doi.org/10.1126/science.274.5292.1531}, volume = {274}, year = {1996} }

RIS record

TY - JOUR ID - citeulike:838515 L3 - citeulike-article-id:838515 N2 - A nuclear magnetic resonance (NMR)-based method is described in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands. The approach is called "SAR by NMR" because structure-activity relationships (SAR) are obtained from NMR. With this technique, compounds with nanomolar affinities for the FK506 binding protein were rapidly discovered by tethering two ligands with micromolar affinities. The method reduces the amount of chemical synthesis and time required for the discovery of high-affinity ligands and appears particularly useful in target-directed drug research. IS - 5292 JF - Science SN - 0036-8075 AD - Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA. EP - 1534 TI - Discovering high-affinity ligands for proteins: SAR by NMR. VL - 274 SP - 1531 KW - nmr KW - sar AU - Shuker, SB AU - Hajduk, PJ AU - Meadows, RP AU - Fesik, SW PY - 1996/11/29/ UR - http://dx.doi.org/10.1126/science.274.5292.1531 ER -

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