TY - JOUR
T1 - Fragment-to-Lead Medicinal Chemistry Publications in 2019
AU - Jahnke, Wolfgang
AU - Erlanson, Daniel A.
AU - De Esch, Iwan J.P.
AU - Johnson, Christopher N.
AU - Mortenson, Paul N.
AU - Ochi, Yuji
AU - Urushima, Tatsuya
PY - 2020/12/24
Y1 - 2020/12/24
N2 - Fragment-based drug discovery (FBDD) has grown and matured to a point where it is valuable to keep track of its extent and details of application. This Perspective summarizes successful fragment-to-lead stories published in 2019. It is the fifth in a series that started with literature published in 2015. The analysis of screening methods, optimization strategies, and molecular properties of hits and leads are presented in the hope of informing best practices for FBDD. Moreover, FBDD is constantly evolving, and the latest technologies and emerging trends are summarized. These include covalent FBDD, FBDD for the stabilization of proteins or protein-protein interactions, FBDD for enzyme activators, new screening technologies, and advances in library design and chemical synthesis.
AB - Fragment-based drug discovery (FBDD) has grown and matured to a point where it is valuable to keep track of its extent and details of application. This Perspective summarizes successful fragment-to-lead stories published in 2019. It is the fifth in a series that started with literature published in 2015. The analysis of screening methods, optimization strategies, and molecular properties of hits and leads are presented in the hope of informing best practices for FBDD. Moreover, FBDD is constantly evolving, and the latest technologies and emerging trends are summarized. These include covalent FBDD, FBDD for the stabilization of proteins or protein-protein interactions, FBDD for enzyme activators, new screening technologies, and advances in library design and chemical synthesis.
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U2 - 10.1021/acs.jmedchem.0c01608
DO - 10.1021/acs.jmedchem.0c01608
M3 - Article
C2 - 33226222
AN - SCOPUS:85097887656
SN - 0022-2623
VL - 63
SP - 15494
EP - 15507
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
IS - 24
ER -