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J Med Chem. 2018 May 24;61(10):4283-4289. doi: 10.1021/acs.jmedchem.7b01120. Epub 2017 Nov 28.

Importance of Rigidity in Designing Small Molecule Drugs To Tackle Protein-Protein Interactions (PPIs) through Stabilization of Desired Conformers.

Author information

1
UCB , 216 Bath Road , Slough SL1 3WE , United Kingdom.
2
Bohicket Pharma Consulting LLC , 2556 Seabrook Island Road , Seabrook Island , South Carolina 29455 , United States.

Abstract

Tackling PPIs, particularly by stabilizing clinically favored conformations of target proteins, with orally available, bona fide small molecules remains a significant but immensely worthwhile challenge for the pharmaceutical industry. Success may be more likely through the application of nature's learnings to build intrinsic rigidity into the design of clinical candidates.

PMID:
29140691
DOI:
10.1021/acs.jmedchem.7b01120
[Indexed for MEDLINE]
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