Inhibition of acetylcholinesterase by hemicholiniums, conformationally constrained choline analogs. Evaluation of aryl and alkyl substituents. Comparisons with choline and (3-hydroxyphenyl)trimethylammonium

1992 ◽  
Vol 5 (3) ◽  
pp. 411-418 ◽  
Author(s):  
Bong Ho Lee ◽  
Terry C. Stelly ◽  
William J. Colucci ◽  
J. Gabriel Garcia ◽  
Richard D. Gandour ◽  
...  
Keyword(s):  
Conformationally Constrained ◽  
Choline Analogs

Conformationally Constrained Peptide Drugs Targeted at the Blood-Brain Barrier

1995 ◽  
Author(s):  
Thomas P. Davis ◽  
Thomas J. Abbruscato ◽  
Elizabeth Brownson ◽  
Victor J. Hruby
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Peptide Drugs ◽  
Conformationally Constrained ◽  
Blood Brain

Pyrrolidine nucleotides conformationally constrained via hydrogen bonding

2014 ◽  
Author(s):  
Radek Pohl ◽  
Lenka Poštová Slavětínská ◽  
Dominik Rejman
Keyword(s):  
Hydrogen Bonding ◽  
Conformationally Constrained

scholarly journals Small and Simple, yet Sturdy: Conformationally Constrained Peptides with Remarkable Properties

2021 ◽  
Vol 22 (4) ◽  
pp. 1611
Author(s):  
Krištof Bozovičar ◽  
Tomaž Bratkovič
Keyword(s):  
Chemical Space ◽  
Structure Optimization ◽  
Peptide Chain ◽  
Conformationally Constrained ◽  
Drug Candidates ◽  
Conformational Constraints ◽  
Macrocyclic Peptides ◽  
Constrained Peptides ◽  
Sheer Size

The sheer size and vast chemical space (i.e., diverse repertoire and spatial distribution of functional groups) underlie peptides’ ability to engage in specific interactions with targets of various structures. However, the inherent flexibility of the peptide chain negatively affects binding affinity and metabolic stability, thereby severely limiting the use of peptides as medicines. Imposing conformational constraints to the peptide chain offers to solve these problems but typically requires laborious structure optimization. Alternatively, libraries of constrained peptides with randomized modules can be screened for specific functions. Here, we present the properties of conformationally constrained peptides and review rigidification chemistries/strategies, as well as synthetic and enzymatic methods of producing macrocyclic peptides. Furthermore, we discuss the in vitro molecular evolution methods for the development of constrained peptides with pre-defined functions. Finally, we briefly present applications of selected constrained peptides to illustrate their exceptional properties as drug candidates, molecular recognition probes, and minimalist catalysts.

An Enantiodefined Conformationally Constrained Fatty Acid Mimetic and Potent Inhibitor of ToxT

2021 ◽  
Author(s):  
Lauren E. Markham ◽  
Jessica D. Tolbert ◽  
F. Jon Kull ◽  
Charles R. Midgett ◽  
Glenn C. Micalizio
Keyword(s):  
Fatty Acid ◽  
Potent Inhibitor ◽  
Conformationally Constrained

Insights into the Distance Dependence of Electron Transfer through Conformationally Constrained Peptides

2020 ◽  
Vol 7 (5) ◽  
pp. 1225-1237
Author(s):  
Claudio Zuliani ◽  
Fernando Formaggio ◽  
Laura Scipionato ◽  
Claudio Toniolo ◽  
Sabrina Antonello ◽  
...  
Keyword(s):  
Electron Transfer ◽  
Conformationally Constrained ◽  
Distance Dependence ◽  
Constrained Peptides

Synthesis of Conformationally Constrained Glutamic Acid Homologues and Investigation of Their Pharmacological Profiles

ChemMedChem ◽  
2007 ◽  
Vol 2 (11) ◽  
pp. 1639-1647 ◽  
Author(s):  
Paola Conti ◽  
Andrea Pinto ◽  
Lucia Tamborini ◽  
Giovanni Grazioso ◽  
Giovambattista De Sarro ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Conformationally Constrained ◽  
Pharmacological Profiles

Conformationally constrained precursors to retinoic acid analogs which stabilize the 9Z-configuration

1995 ◽  
Vol 5 (9) ◽  
pp. 953-958 ◽  
Author(s):  
Cynthia Y. Robinson ◽  
D.Vincent Waterhous ◽  
Donald D. Muccio ◽  
Wayne J. Brouillette
Keyword(s):  
Retinoic Acid ◽  
Conformationally Constrained
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