scholarly journals Important Considerations Related to Permeability of Peptides

2021 ◽  
Vol 75 (6) ◽  
pp. 522-524
Author(s):  
Thomas E. Vorherr

This review on intracellular delivery and oral bioavailability of peptides reflects a number of principal investigations at Novartis. Our studies were aimed at either understanding features enabling peptides to interfere with intracellular protein–protein interactions, or to achieve a more patient-friendly delivery by the oral route. In the light of these objectives, we have also spent some effort on assay development to come up with alternative methods for monitoring cellular peptide uptake. This summary of our insights is intended to help in the assessment and development of peptide therapeutics requiring membrane transition

2021 ◽  
Vol 29 ◽  
pp. 115906
Author(s):  
Sanjeevini Babu Reddiar ◽  
Hareth Al-Wassiti ◽  
Colin W. Pouton ◽  
Cameron J. Nowell ◽  
Macgregor A. Matthews ◽  
...  

2020 ◽  
Vol 142 (47) ◽  
pp. 19950-19955
Author(s):  
Stephen E. Miller ◽  
Kohei Tsuji ◽  
Rachel P.M. Abrams ◽  
Terrence R. Burke ◽  
Joel P. Schneider

2016 ◽  
Vol 128 (36) ◽  
pp. 10770-10773 ◽  
Author(s):  
Daisuke Fujiwara ◽  
Hidekazu Kitada ◽  
Masahiro Oguri ◽  
Toshio Nishihara ◽  
Masataka Michigami ◽  
...  

2013 ◽  
Vol 66 (12) ◽  
pp. 1544 ◽  
Author(s):  
Martin J. Drysdale

Fragment-Based Drug Discovery (FBDD) is here to stay. Validated as a technology with the delivery of Zelboraf (Vemurafenib) for the treatment of mutant B-RafV600E melanoma, it has become embedded within the pharmaceutical and biotechnology industries. FBDD has delivered clinical development candidates for a broad range of targets including some of the most challenging cases such as β-secretase (BACE1) and protein–protein interactions. But the best is surely still to come.


2021 ◽  
Author(s):  
Shuhui Lim ◽  
Nicolas Boyer ◽  
Nicole Boo ◽  
Chunhui Huang ◽  
Gireedhar Venkatachalam ◽  
...  

Macrocyclic peptides have the potential to address intracellular protein-protein interactions (PPIs) of high value therapeutic targets that have proven largely intractable to small molecules. Here, we report broadly applicable lessons...


2020 ◽  
Vol 11 (21) ◽  
pp. 5577-5591 ◽  
Author(s):  
Srinivasaraghavan Kannan ◽  
Pietro G. A. Aronica ◽  
Simon Ng ◽  
Dawn Thean Gek Lian ◽  
Yuri Frosi ◽  
...  

Peptide-based molecules hold great potential as targeted inhibitors of intracellular protein–protein interactions (PPIs).


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