Small molecule active site directed tools for studying human caspases
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 …
decades ago. They play critical roles in the control of regulated cell death pathways …
Interleukin-1β converting enzyme (ICE): A comprehensive review on discovery and development of caspase-1 inhibitors
Caspase-1 is a critical mediator of the inflammatory process by activating various pro-
inflammatory cytokines such as pro-IL-1β, IL-18 and IL-33. Uncontrolled activation of …
inflammatory cytokines such as pro-IL-1β, IL-18 and IL-33. Uncontrolled activation of …
Preferred hydrogen-bonding partners of cysteine: implications for regulating Cys functions
K Mazmanian, K Sargsyan, C Grauffel… - The Journal of …, 2016 - ACS Publications
The hydrogen-bonding interactions of cysteine, which can serve as a hydrogen-bond donor
and/or acceptor, play a central role in cysteine's diverse functional roles in proteins. They …
and/or acceptor, play a central role in cysteine's diverse functional roles in proteins. They …
Cs2CO3‐Promoted Direct N‐Alkylation: Highly Chemoselective Synthesis of N‐Alkylated Benzylamines and Anilines
JC Castillo, J Orrego‐Hernández… - European Journal of …, 2016 - Wiley Online Library
Herein is described an efficient and chemoselective method for the synthesis of diversely
substituted secondary amines in yields up to 98%. Direct mono‐N‐alkylation of primary …
substituted secondary amines in yields up to 98%. Direct mono‐N‐alkylation of primary …
Palladium‐Catalyzed Synthesis of N‐Cyclohexyl Anilines from Phenols with Hydrazine or Hydroxylamine via N‐N/O Cleavage
Direct access to amines from biomass‐based phenols via deoxygenative transformation
remains greatly challenging in organic synthesis. Herein, we present a palladium‐catalyzed …
remains greatly challenging in organic synthesis. Herein, we present a palladium‐catalyzed …
Allosteric modulation of caspases
HG Häcker, MT Sisay, M Gütschow - Pharmacology & therapeutics, 2011 - Elsevier
Caspases are proteolytic enzymes mainly involved in the induction and execution phases of
apoptosis. This type of programmed cell death is an essential regulatory process required to …
apoptosis. This type of programmed cell death is an essential regulatory process required to …
New β-strand templates constrained by Huisgen cycloaddition
AD Pehere, AD Abell - Organic letters, 2012 - ACS Publications
New peptidic templates constrained into a β-strand geometry by linking acetylene and azide
containing P1 and P3 residues of a tripeptide by Huisgen cycloaddition are presented. The …
containing P1 and P3 residues of a tripeptide by Huisgen cycloaddition are presented. The …
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors
AK Bhattacharya, KC Rana - Bioorganic & medicinal chemistry, 2011 - Elsevier
We report herein, design and synthesis of vinylaminophosphonates, a novel class of
compounds as possible cysteine protease inhibitors. The synthesis of …
compounds as possible cysteine protease inhibitors. The synthesis of …
Tripeptide analogues of MG132 as protease inhibitors
AD Pehere, S Nguyen, SK Garlick, DW Wilson… - Bioorganic & Medicinal …, 2019 - Elsevier
The 26S proteasome and calpain are linked to a number of important human diseases.
Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor …
Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor …
A comprehensive panel of turn‐on caspase biosensors for investigating caspase specificity and caspase activation pathways
SS Shekhawat, ST Campbell, I Ghosh - ChemBioChem, 2011 - Wiley Online Library
Caspases play a central role in apoptosis, differentiation, and proliferation, and represent
important therapeutic targets for treating cancer and inflammatory disorders. Toward the …
important therapeutic targets for treating cancer and inflammatory disorders. Toward the …