From fragment to clinical candidate—a historical perspective Export

@article{citeulike:4495961, abstract = {As recently as ten years ago few scientists had heard of fragment screening, let alone considered low molecular weight fragments (MW < 300) with weak binding affinities to be attractive start points for drug discovery programs. Today, however, there is widespread acceptance that these fragments can be progressed into lead series and on to become clinical candidates. Consequently, over the past 3-4 years, fragment-based drug discovery has become firmly established within the biotechnology and pharmaceutical industries as a complimentary strategy to high-throughput screening. In this review, we give a historical perspective of how rapidly fragment-based drug discovery has developed and describe a number of clinical compounds discovered using this approach.}, author = {Chessari, Gianni and Woodhead, Andrew J.}, citeulike-article-id = {4495961}, citeulike-linkout-0 = {http://dx.doi.org/10.1016/j.drudis.2009.04.007}, citeulike-linkout-1 = {http://linkinghub.elsevier.com/retrieve/pii/S1359644609001470}, day = {07}, doi = {10.1016/j.drudis.2009.04.007}, issn = {13596446}, journal = {Drug Discovery Today}, keywords = {astex, cdk2, factor, fbdd, ppar, xa}, month = {July}, number = {13-14}, pages = {668--675}, posted-at = {2009-05-08 22:41:51}, priority = {5}, title = {From fragment to clinical candidate—a historical perspective}, url = {http://dx.doi.org/10.1016/j.drudis.2009.04.007}, volume = {14}, year = {2009} }

TY - JOUR ID - citeulike:4495961 L3 - citeulike-article-id:4495961 N2 - As recently as ten years ago few scientists had heard of fragment screening, let alone considered low molecular weight fragments (MW < 300) with weak binding affinities to be attractive start points for drug discovery programs. Today, however, there is widespread acceptance that these fragments can be progressed into lead series and on to become clinical candidates. Consequently, over the past 3-4 years, fragment-based drug discovery has become firmly established within the biotechnology and pharmaceutical industries as a complimentary strategy to high-throughput screening. In this review, we give a historical perspective of how rapidly fragment-based drug discovery has developed and describe a number of clinical compounds discovered using this approach. IS - 13-14 JF - Drug Discovery Today SN - 13596446 EP - 675 TI - From fragment to clinical candidate—a historical perspective VL - 14 SP - 668 KW - astex KW - cdk2 KW - factor KW - fbdd KW - ppar KW - xa AU - Chessari, Gianni AU - Woodhead, Andrew PY - 2009/07/07/ UR - http://dx.doi.org/10.1016/j.drudis.2009.04.007 ER -