Viral macrodomains: a structural and evolutionary assessment of the pharmacological potential [PDF]
Viral macrodomains possess the ability to counteract host ADP-ribosylation, a post-translational modification implicated in the creation of an antiviral environment via immune response regulation.
Johannes Gregor Matthias Rack +5 more
doaj +6 more sources
Mitochondrial ceramide-rich macrodomains functionalize Bax upon irradiation. [PDF]
BACKGROUND:Evidence indicates that Bax functions as a "lipidic" pore to regulate mitochondrial outer membrane permeabilization (MOMP), the apoptosis commitment step, through unknown membrane elements.
Hyunmi Lee +14 more
doaj +4 more sources
Macrodomain ADP-ribosylhydrolase and the pathogenesis of infectious diseases. [PDF]
Anthony K L Leung +2 more
doaj +4 more sources
Structure-Based Rational Design of a Selective Hydrolase Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus-2 Nsp3 Macrodomain. [PDF]
Structure‐guided design of a sulfamoyl‐modified analog of GS‐441524 yielded a selective, high‐affinity inhibitor of the SARS‐CoV‐2 macrodomain Nsp3b. The compound occupies the phosphate‐binding pocket, forming a stabilizing hydrogen‐bond network that enhances binding affinity (K_D = 0.86 μM).
Krishnathas R +13 more
europepmc +2 more sources
Macrodomains: Structure, Function, Evolution, and Catalytic Activities [PDF]
Recent developments indicate that macrodomains, an ancient and diverse protein domain family, are key players in the recognition, interpretation, and turnover of ADP-ribose (ADPr) signaling. Crucial to this is the ability of macrodomains to recognize ADPr either directly, in the form of a metabolic derivative, or as a modification covalently bound to ...
Johannes Gregor Matthias Rack +2 more
+5 more sources
Viral macrodomains, which can bind to and/or hydrolyze adenine diphosphate ribose (ADP-ribose or ADPr) from proteins, have been suggested to counteract host immune response and be viable targets for the development of antiviral drugs. Therefore, developing high-throughput screening (HTS) techniques for macrodomain inhibitors is of great interest ...
Ananya Anmangandla +9 more
openaire +2 more sources
Molecular docking study and molecular dynamics simulation of spice metabolites against main protease enzymes and NSP3 macrodomain SARS CoV-2 [PDF]
COVID-19 is still a global pandemic. The transmission is very fast and wide. Its prevalence continues to increase. There is no specific antiviral drug for SARS CoV 2 yet.
Purwaniati Purwaniati, Asep Roni
doaj +1 more source
PARG: A Macrodomain in Disguise [PDF]
Our understanding of poly-ADP-ribosylation as a posttranslational modification was limited by the lack of structural information on poly-ADP-ribose (PAR) hydrolysing enzymes. A recent study in Nature (Slade et al., 2011) reports the structure of PAR glycohydrolase (PARG), revealing unexpected similarity to the ubiquitous ADP-ribose-binding macrodomains.
Markus Hassler +2 more
openaire +2 more sources
Since the emergence of SARS-CoV-2, many genetic variations within its genome have been identified, but only a few mutations have been found in nonstructural proteins (NSPs).
Behnaz Yazdani +3 more
doaj +1 more source
The SARS-CoV-2 conserved macrodomain is a mono-ADP-ribosylhydrolase [PDF]
ABSTRACT Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and other SARS-like-CoVs encode 3 tandem macrodomains within non-structural protein 3 (nsp3). The first macrodomain, Mac1, is conserved throughout CoVs, and binds to and hydrolyzes mono-ADP-ribose (MAR) from target proteins.
Yousef M.O. Alhammad +12 more
openaire +3 more sources

