We also find that drug nanoaggregates are stabilized in an amorphous core-shell structure. These findings demonstrate that rational design can address intracellular aggregation and pharmacologic/delivery challenges in conventional and fragment-based drug development processes....
Twenty years on: the impact of fragments on drug discovery. Nat Rev Drug Discov 15, 605–19 (2016). 37. Congreve, M., Oswald, C. & Marshall, F. H. Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs. Trends Pharmacol Sci 38, 837–847 (2017). 38. ...
the R&D project title is “Global innovation technology alliance”, and the research title is “Development of global antibody drug based on novel epitope
This versatile antibody switch platform may be used as a core molecular control component to develop an advanced, next generation immunotherapeutic platform for cell-based or antibody-based immunotherapies and biologics with a range of applications including but not limited to cancer, autoimmune diseases ...
Fragment-based drug design: Computational & experimental state of the art. Comb. Chem. High. Throughput Screen. 2011, 14, 500–520. [CrossRef] [PubMed] 16. Fielding, L. NMR methods for the determination of protein–ligand dissociation constants. Prog. Nucl. Magn. Reson. Spectrosc. 2007, ...
Keywords: fragment-based drug design; 19F-NMR; labelling; chemical shift; linewidth; ligand; protein; peptide 1. Introduction With a decline in the number of new FDA-approved drugs reaching the clinic each year [1], in particular in the area of new antibiotics [2], new approaches to the ...
Keywords: adenosine receptors; positive allosteric modulators; fragment-based approaches; supervised molecular dynamics 1. Introduction Structure-driven fragment-based (SDFB) approaches have provided efficient methods for the design of novel pharmacological probes as well as drug candidates [1]. One of ...
NMR-based screening: A powerful tool in fragment-based drug discovery. Analyst 2007, 132, 693–705. [CrossRef] [PubMed] 25. Zhang, X.; Tang, H.; Ye, C.; Liu, M. Structure-based drug design: NMR-based approach for ligand-protein interactions. Drug Discov. Today Technol. 2006, 3,...
viruses Article Screening and Identification of Lassa Virus Entry Inhibitors from a Fragment-Based Drug Discovery Library Yuxia Hou 1,2, Yang Liu 1, Xiaoying Jia 1,2, Minmin Zhou 1,2, Wenting Mao 1,2, Siqi Dong 1,2, Yueli Zhang 1,3, Gengfu Xiao 1,2 and Wei Wang 1,2,* 1 State...
International Journal of Molecular Sciences Article Design and In Vitro Evaluation of a Cytotoxic Conjugate Based on the Anti-HER2 Affibody Fused to the Fc Fragment of IgG1 Alicja M. Sochaj-Gregorczyk 1, Patryk Ludzia 1, Emilia Kozdrowska 1, Piotr Jakimowicz 2, Aleksandra Sokolowska-Wedzina...