Constraining cyclic peptides to mimic protein structure motifs

TA Hill, NE Shepherd, F Diness… - Angewandte Chemie …, 2014 - Wiley Online Library
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery

E Marsault, ML Peterson - Journal of medicinal chemistry, 2011 - ACS Publications
Macrocycles occupy a unique segment of chemical space. In the past decade, their chemical
diversity expanded significantly, supported by advances in bioinformatics and synthetic …

Calpain research for drug discovery: challenges and potential

Y Ono, TC Saido, H Sorimachi - Nature Reviews Drug Discovery, 2016 - nature.com
Calpains are a family of proteases that were scientifically recognized earlier than
proteasomes and caspases, but remain enigmatic. However, they are known to participate in …

Development of α-helical calpain probes by mimicking a natural protein–protein interaction

H Jo, N Meinhardt, Y Wu, S Kulkarni, X Hu… - Journal of the …, 2012 - ACS Publications
We have designed a highly specific inhibitor of calpain by mimicking a natural protein–
protein interaction between calpain and its endogenous inhibitor calpastatin. To enable this …

Structure–function relationships in calpains

RL Campbell, PL Davies - Biochemical Journal, 2012 - portlandpress.com
Calpains are a family of complex multi-domain intracellular enzymes that share a calcium-
dependent cysteine protease core. These are not degradative enzymes, but instead carry …

Calpains and neuronal damage in the ischemic brain: The swiss knife in synaptic injury

M Curcio, IL Salazar, M Mele, LMT Canzoniero… - Progress in …, 2016 - Elsevier
The excessive extracellular accumulation of glutamate in the ischemic brain leads to an
overactivation of glutamate receptors with consequent excitotoxic neuronal death. Neuronal …

Drug delivery to the lens for the management of cataracts

TR Thrimawithana, ID Rupenthal, SS Räsch… - Advanced drug delivery …, 2018 - Elsevier
Cataracts are one of the most prevalent diseases of the lens, affecting its transparency and
are the leading cause of reversible blindness in the world. The clarity of the lens is essential …

Calpain inhibitors: a survey of compounds reported in the patent and scientific literature

IO Donkor - Expert opinion on therapeutic patents, 2011 - Taylor & Francis
Introduction: Calpain is a cysteine protease that participates in normal signal transduction
events, but deregulation of its action may result in pathologies such as neurological …

Enantioselective synthesis of α-alkenyl α-amino acids via N–H insertion reactions

JX Guo, T Zhou, B Xu, SF Zhu, QL Zhou - Chemical Science, 2016 - pubs.rsc.org
A new highly enantioselective route to α-alkenyl α-amino acid derivatives, which are
important naturally occurring compounds with attractive bioactivity and synthetic utility, was …

Dynamic docking of conformationally constrained macrocycles: methods and applications

SE Allen, NV Dokholyan, AA Bowers - ACS chemical biology, 2016 - ACS Publications
Many natural products consist of large and flexible macrocycles that engage their targets via
multiple contact points. This combination of contained flexibility and large contact area often …