The current state of peptide drug discovery: Back to the future? J. Med. Chem. 2017. [CrossRef] [PubMed]Henninot, A.; Collins, J.C.; Nuss, J.M. The current state of peptide drug discovery: back to the future? J. Med. Chem., 2018, 61(4), 1382-1414. [http...
Tulla-Puche Judit,Spengler Jan,Albericio Fernando.The synthesis of naturally occurring peptides and their analogs.Current opinion in drug discovery & ... T Cupido,J Tullapuche,J Spengler,... - 《Curr Opin Drug Discov Devel》 被引量: 238发表: 2007年 Advances in the Prediction of Protein-...
The peptides were designed by performing molecular docking in the active site ofhDHFR. Analysis of the crystal coordinates of human DHFR (PDB ID 4M6K) reveals that its substrate (folic acid) exhibits two H-bonds with Glu 30 through the NH2(1.88 Å) and NH (1.86 Å) moiety o...
drug discovery cyclic peptide cell proliferation cell signaling cell migration biologics cancer therapeutics Introduction Aberrant signaling from the small G-protein Ras has been shown to drive approximately one-third of all human cancers making it a compelling therapeutic target (1). Targeting Ras isofor...
Therapeutic peptides: historical perspectives, current development trends, and future directions. Bioorg. Med. Chem. 26, 2700–2707 (2018). Article CAS PubMed Google Scholar Bruno, B. J., Miller, G. D. & Lim, C. S. Basics and recent advances in peptide and protein drug delivery. Ther...
1A), some of them had extremely low Ki values (Table 1). For DOR the ligands showed comparable binding affinities than the selective DOR agonist Ile5,6-deltorphin II peptide ligand (Fig. 1B) except 8 (Ki > 3000 nM). In the KOR binding assays, performed in guinea pig brain ...
Drug transport via the intestinal peptide transporter PepT1. Curr. Opin. Pharmacol. 13, 881–887 (2013). Article CAS PubMed Google Scholar Soul-Lawton, J. et al. Absolute bioavailability and metabolic disposition of valaciclovir, the L-valyl ester of acyclovir, following oral administration to...
Bacterial resistance to conventional antibiotics is a growing issue, and the development of novel antimicrobial compounds has not been able to keep pace with the emergence of multi drug resistant pathogens. Antimicrobial peptides are source of inspiration for the development of next generation antimicrobi...
The existence of SONOS-linked peptides (C22-K61-C44) could not be directly proven by mass spectrometry of the proteolytically digested protein similar to the initially discovered NOS crosslink in a transaldolase28, but we noticed that residues C22 and C44 were only accessible for alkylation afte...
Alternative formats to mAbs, such as protein scaffolds (designed ankyrin-repeat proteins (DARPins), nanobodies, single-chain variable fragments (scFvs) and peptide–drug conjugates), dual-labelled ADCs and biparatopic drug conjugates, present new research avenues. There are several possible indications...