Studies of Hemoglobin and Allosteric Enzymes Under Artificial Conformational Constraints

1978 ◽  
pp. 373-379 ◽  
Author(s):  
D. Guillochon ◽  
C. Bourdillon ◽  
D. Thomas
Keyword(s):  
Conformational Constraints ◽  
Allosteric Enzymes

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.

Using Conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability

2021 ◽  
pp. 128086
Author(s):  
Dirk Tourwé ◽  
Antonis D. Tsiailanis ◽  
Nikolaos Parisis ◽  
Baydaa Hirmiz ◽  
Mark Del Borgo ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Conformational Constraints ◽  
Proteolytic Stability

Conformational constraints in the reactions of surface bonded intermediates

1981 ◽  
Vol 26 (6) ◽  
pp. 687-689
Author(s):  
A.F. Diaz ◽  
M. Genies
Keyword(s):  
Conformational Constraints

Synthesis of supramolecular precision polymers: Crystallization under conformational constraints

2017 ◽  
Vol 55 (22) ◽  
pp. 3736-3748 ◽  
Author(s):  
Sophie Reimann ◽  
Varun Danke ◽  
Mario Beiner ◽  
Wolfgang H. Binder
Keyword(s):  
Conformational Constraints

Chemical and Structural Implications of 1‘,2‘- versus 2‘,4‘- Conformational Constraints in the Sugar Moiety of Modified Thymine Nucleosides

2007 ◽  
Vol 72 (13) ◽  
pp. 4716-4726 ◽  
Author(s):  
Oleksandr Plashkevych ◽  
Subhrangsu Chatterjee ◽  
Dmytro Honcharenko ◽  
Wimal Pathmasiri ◽  
Jyoti Chattopadhyaya
Keyword(s):  
Sugar Moiety ◽  
Conformational Constraints

Peptide with built-in conformational constraints: structure of Z-(Aib)7-O t Bu

1993 ◽  
Vol 49 (3) ◽  
pp. 560-564 ◽  
Author(s):  
M. Vlassi ◽  
H. Brueckner ◽  
M. Kokkinidis
Keyword(s):  
Conformational Constraints

scholarly journals A Novel Organization of ACT Domains in Allosteric Enzymes Revealed by the Crystal Structure of Arabidopsis Aspartate Kinase

2006 ◽  
Vol 18 (7) ◽  
pp. 1681-1692 ◽  
Author(s):  
Corine Mas-Droux ◽  
Gilles Curien ◽  
Mylène Robert-Genthon ◽  
Mathieu Laurencin ◽  
Jean-Luc Ferrer ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Aspartate Kinase ◽  
Allosteric Enzymes

scholarly journals The hydrogen peroxide hypersensitivity of OxyR2 inVibrio vulnificusdepends on conformational constraints

2017 ◽  
Vol 292 (17) ◽  
pp. 7223-7232 ◽  
Author(s):  
Inseong Jo ◽  
Dukyun Kim ◽  
Ye-Ji Bang ◽  
Jinsook Ahn ◽  
Sang Ho Choi ◽  
...  
Keyword(s):  
Hydrogen Peroxide ◽  
Conformational Constraints
Sign in / Sign up

Export Citation Format

Share Document