| Chapter title |
Recombinant Kinase Production and Fragment Screening by NMR Spectroscopy.
|
|---|---|
| Chapter number | 3 |
| Book title |
Kinase Screening and Profiling
|
| Published in |
Methods in molecular biology, January 2016
|
| DOI | 10.1007/978-1-4939-3073-9_3 |
| Pubmed ID | |
| Book ISBNs |
978-1-4939-3072-2, 978-1-4939-3073-9
|
| Authors |
Han, Byeonggu, Ahn, Hee-Chul, Byeonggu Han, Hee-Chul Ahn |
| Abstract |
During the past decade fragment-based drug discovery (FBDD) has rapidly evolved and several drugs or drug candidates developed by FBDD approach are clinically in use or in clinical trials. For example, vemurafenib, a V600E mutated BRAF inhibitor, was developed by utilizing FBDD approach and approved by FDA in 2011. In FBDD, screening of fragments is the starting step for identification of hits and lead generation. Fragment screening usually relies on biophysical techniques by which the protein-bound small molecules can be detected. NMR spectroscopy has been extensively used to study the molecular interaction between the protein and the ligand, and has many advantages in fragment screening over other biophysical techniques. This chapter describes the practical aspects of fragment screening by saturation transfer difference NMR. |
Mendeley readers
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 6 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 2 | 33% |
| Student > Ph. D. Student | 1 | 17% |
| Student > Bachelor | 1 | 17% |
| Student > Doctoral Student | 1 | 17% |
| Unknown | 1 | 17% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 3 | 50% |
| Biochemistry, Genetics and Molecular Biology | 2 | 33% |
| Unknown | 1 | 17% |