Advances in the chemistry of tetrahydroquinolines

V Sridharan, PA Suryavanshi, JC Menendez - Chemical reviews, 2011 - ACS Publications
1.1. General Heterocyclic compounds, especially nitrogen heterocycles, are the most
important class of compounds in the pharmaceutical and agrochemical industries, with …

[HTML][HTML] Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors

M Siklos, M BenAissa, GRJ Thatcher - Acta Pharmaceutica Sinica B, 2015 - Elsevier
Cysteine proteases continue to provide validated targets for treatment of human diseases. In
neurodegenerative disorders, multiple cysteine proteases provide targets for enzyme …

Caspase substrates and inhibitors

M Poręba, A Stróżyk… - Cold Spring Harbor …, 2013 - cshperspectives.cshlp.org
Caspases are proteases at the heart of networks that govern apoptosis and inflammation.
The past decade has seen huge leaps in understanding the biology and chemistry of the …

Legumain protease-activated TAT-liposome cargo for targeting tumours and their microenvironment

Z Liu, M Xiong, J Gong, Y Zhang, N Bai, Y Luo… - Nature …, 2014 - nature.com
Specific targeting and cellular internalization are key properties for carriers of antitumor
therapeutic agents. Here, we develop a drug carrier through the attachment of substrate of …

The tunable functionality of α, β‐unsaturated carbonyl compounds enables their differential application in biological systems

S Amslinger - ChemMedChem, 2010 - Wiley Online Library
Abstract α, β‐Unsaturated carbonyl compounds as potential drug candidates is a
controversial topic since their potential Michael acceptor activity can lead to cell damage …

Azapeptides and their therapeutic potential

C Proulx, D Sabatino, R Hopewell… - Future medicinal …, 2011 - Taylor & Francis
Azapeptides are peptide analogs in which one or more of the amino residues is replaced by
a semicarbazide. This substitution of a nitrogen for the α-carbon center results in …

Michael acceptors as cysteine protease inhibitors

MMM Santos, R Moreira - Mini reviews in medicinal chemistry, 2007 - benthamdirect.com
Cysteine proteases selectively catalyze the hydrolysis of peptide bonds. Uncontrolled,
unregulated, or undesired proteolysis can lead to many disease states including …

Functional interplay between caspase cleavage and phosphorylation sculpts the apoptotic proteome

MM Dix, GM Simon, C Wang, E Okerberg, MP Patricelli… - Cell, 2012 - cell.com
Caspase proteases are principal mediators of apoptosis, where they cleave hundreds of
proteins. Phosphorylation also plays an important role in apoptosis, although the extent to …

Activation and regulation of caspase-6 and its role in neurodegenerative diseases

XJ Wang, Q Cao, Y Zhang, XD Su - Annual review of …, 2015 - annualreviews.org
Caspases, a family of cysteine proteases, are major mediators of apoptosis and
inflammation. Caspase-6 is classified as an apoptotic effector, and it mediates nuclear …

Small molecule active site directed tools for studying human caspases

M Poreba, A Szalek, P Kasperkiewicz, W Rut… - Chemical …, 2015 - ACS Publications
Caspases are proteases of clan CD and were described for the first time more than two
decades ago. They play critical roles in the control of regulated cell death pathways …