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Interview with Anthony DiGiorgio
Anthony Joseph DiGiorgio
Jan 01, 0001
In his February 20, 2015 interview with Daniel Lee, Anthony DiGiorgio recollects the impact Hurricane Hugo had on Winthrop University and the Rock Hill Community. DiGiorgio discusses weather reports leading up to the hurricane...
President Hurricane power outage Tillman Stewart House Trees Breazeale Hall environmental damage Oral History
Published by: Winthrop University
Allosteric Targeting of Aurora A Kinase Using Small Molecules
BACKGROUND: Aurora A (AurA) kinase is a key mitotic protein implicated in cancer. Several small molecule inhibitors targeting the ATP binding site of this enzyme are in various stages of clinical development. However, these...
AURKA AurA-TPX2 inhibition Aurora A TPX2 allosteric inhibition Kinase inhibitors proteinprotein
interaction type IV inhibitors. Allosteric Regulation Allosteric Site Anacardic Acids Aurora Kinase A Cell Cycle Proteins Cell Line Tumor Felodipine Humans Microtubule-Associated Proteins Nuclear Proteins Protein Binding Protein Kinase Inhibitors
Fragment-based approaches to TB drugs.
Mass spectrometry for fragment screening.
Fragment-based approaches in chemical biology and drug discovery have been widely adopted worldwide in both academia and industry. Fragment hits tend to interact weakly with their targets, necessitating the use of sensitive...
Fragment-based drug discovery ligand-observed mass spectrometry native mass spectrometry Calorimetry Combinatorial Chemistry Techniques Crystallography X-Ray Drug Design Drug Discovery Fluorometry High-Throughput Screening Assays Humans Ligands Magnetic Resonance Spectroscopy Mass Spectrometry Protein Binding Proteins Small Molecule Libraries Structure-Activity Relationship
Reminiscences of Anthony J. Campo
The Rockefeller University
Jan 01, 0001
OCCASIONAL PAPERS by the faculty and staff of The Rockefeller University are published at irregular intervals by The Rockefeller University Press, New York, N. Y. This is Occasional Paper Fifteen of which five hundred have been...
Published by: The Rockefeller University Press
Spirooxindoles as novel 3D-fragment scaffolds
Covalent inactivation of Mycobacterium thermoresistibile inosine-5'-monophosphate dehydrogenase (IMPDH).
Ana Trapero, Angela Pacitto, Daniel Shiu-Hin Chan, Chris Abell, Tom L Blundell, David B Ascher, Anthony G Coyne
Nov 15, 2019
Inosine-5'-monophosphate dehydrogenase (IMPDH) is a rate-limiting enzyme involved in nucleotide biosynthesis. Because of its critical role in purine biosynthesis, IMPDH is a drug design target for immunosuppressive, anticancer...
Small-molecule inhibitors that target protein-protein interactions in the RAD51 family of recombinases.
Duncan E Scott, Anthony G Coyne, Ashok Venkitaraman, Tom L Blundell, Chris Abell, Marko Hyvönen
Dec 16, 2014
BRCA2 RAD51 biophysics homologous recombination INHIBITORS protein-protein interactions Amino Acid Motifs BRCA2 Protein Binding Sites Drug Design Humans Molecular Dynamics Simulation Protein Binding Protein Structure Tertiary Pyrococcus furiosus Rad51 Recombinase Small Molecule Libraries Structure-Activity Relationship Thermodynamics
G-Quadruplexes
Guanine (G)-rich sequences in nucleic acids can assemble into G-quadruplex structures that involve G-quartets linked by loop nucleotides. The structural and topological diversity of G-quadruplexes have attracted great attention...
Fragment-Based Design of Mycobacterium tuberculosis InhA Inhibitors.
Mohamad Sabbah, Vitor Mendes, Robert G Vistal, David MG Dias, Monika Záhorszká, Katarína Mikušová, Jana Korduláková, Anthony G Coyne, Tom L Blundell, Chris Abell
Apr 06, 2020
Tuberculosis (TB) remains a leading cause of mortality among infectious diseases worldwide. InhA has been the focus of numerous drug discovery efforts as this is the target of the first line pro-drug isoniazid. However, with...
THE CONCISE GUIDE TO PHARMACOLOGY 2019/20
Stephen Ph Alexander, Arthur Christopoulos, Anthony P Davenport, Eamonn Kelly, Alistair Mathie, John A Peters, Emma L Veale, Jane F Armstrong, Elena Faccenda, Simon D Harding, Adam J Pawson, Joanna L Sharman, Christopher Southan, Jamie A Davies, CGTP Collaborators
Dec 12, 2019
The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective...
Synthesis of Novel Regenerable 13X Zeolite-Polyimide Adsorbent Foams
A new generic synthesis method is presented for the production of a polyimide (PI)/adsorbent (80 wt% 13X zeolite) regenerable foam filter. The method uses a dual parallel reaction foaming process comprising CO 2...
Adsorbent foam Adsorption Air Filters Isotherms modelling Polyimide /dk/atira/pure/subjectarea/asjc/1600/1600 name=General Chemistry /dk/atira/pure/subjectarea/asjc/2300/2304 name=Environmental Chemistry /dk/atira/pure/subjectarea/asjc/1500/1500 name=General Chemical Engineering /dk/atira/pure/subjectarea/asjc/2200/2209 name=Industrial and Manufacturing Engineering
Substrate Fragmentation for the Design of M. tuberculosis CYP121 Inhibitors.
Madeline E Kavanagh, Janine L Gray, Sophie H Gilbert, Anthony G Coyne, Kirsty J McLean, Holly J Davis, Andrew W Munro, Chris Abell
Aug 02, 2016
Drug Discovery Enzymes fragment-based methods substrate analogues Tuberculosis Anti-Bacterial Agents Crystallography X-Ray Cytochrome P-450 Enzyme System Dipeptides Dose-Response Relationship Drug Drug Design Enzyme Inhibitors Microbial Sensitivity Tests Models Molecular Molecular Conformation Mycobacterium tuberculosis Structure-Activity Relationship
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18
Stephen Ph Alexander, Arthur Christopoulos, Anthony P Davenport, Eamonn Kelly, Neil V Marrion, John A Peters, Elena Faccenda, Simon D Harding, Adam J Pawson, Joanna L Sharman, Christopher Southan, Jamie A Davies, CGTP Collaborators
Nov 16, 2017
The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access...
Remote stereocontrol in [3,3]-sigmatropic rearrangements
The Ireland - Claisen [3,3]-sigmatropic rearrangement has been used to access biologically important β,β′-dihydroxy α-amino acids. The rearrangement reported is highly stereoselective and offers excellent levels of remote...
Synthesis of Novel Regenerable 13X Zeolite-Polyimide Adsorbent Foams
A new generic synthesis method is presented for the production of a polyimide (PI)/adsorbent (80 wt% 13X zeolite) regenerable foam filter. The method uses a dual parallel reaction foaming process comprising CO 2...
Adsorbent foam Adsorption Air Filters Isotherms modelling Polyimide /dk/atira/pure/subjectarea/asjc/1600/1600 name=General Chemistry /dk/atira/pure/subjectarea/asjc/2300/2304 name=Environmental Chemistry /dk/atira/pure/subjectarea/asjc/1500/1500 name=General Chemical Engineering /dk/atira/pure/subjectarea/asjc/2200/2209 name=Industrial and Manufacturing Engineering
Fragment-Based Approach to Targeting Inosine-5'-monophosphate Dehydrogenase (IMPDH) from Mycobacterium tuberculosis.
Ana Trapero, Angela Pacitto, Vinayak Singh, Mohamad Sabbah, Anthony G Coyne, Valerie Mizrahi, Tom L Blundell, David B Ascher, Chris Abell
Jun 06, 2018
Tuberculosis (TB) remains a major cause of mortality worldwide, and improved treatments are needed to combat emergence of drug resistance. Inosine 5'-monophosphate dehydrogenase (IMPDH), a crucial enzyme required for de novo...
RNA promotes phase separation of glycolysis enzymes into yeast G bodies in hypoxia.
Gregory G Fuller, Ting Han, Mallory A Freeberg, James J Moresco, Amirhossein Ghanbari Niaki, Nathan P Roach, John R Yates, Sua Myong, John K Kim
Apr 17, 2020
In hypoxic stress conditions, glycolysis enzymes assemble into singular cytoplasmic granules called glycolytic (G) bodies. G body formation in yeast correlates with increased glucose consumption and cell survival. However, the...
Remote stereocontrol in [3,3]-sigmatropic rearrangements
The Ireland - Claisen [3,3]-sigmatropic rearrangement has been used to access biologically important β,β′-dihydroxy α-amino acids. The rearrangement reported is highly stereoselective and offers excellent levels of remote...
Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor.
Theoretical models of G protein-coupled receptor (GPCR) concentration-response relationships often assume an agonist producing a single functional response via a single active state of the receptor. These models have largely...
Structure-guided fragment-based drug discovery at the synchrotron
Sherine E Thomas, Patrick Collins, Rory Hennell James, Vitor Mendes, Sitthivut Charoensutthivarakul, Chris Radoux, Chris Abell, Anthony G Coyne, R Andres Floto, Frank von Delft, Tom L Blundell
Apr 03, 2019
Mycobacterium abscessus SAICAR synthetase (PurC) Fragment-based drug discovery Structure-guided synchrotron Bacterial Proteins Binding Sites Drug Discovery High-Throughput Screening Assays History 20th Century History 21st Century Humans Models Molecular Mycobacterium abscessus Peptide Fragments Peptide Synthases Synchrotrons
Targeting of Fumarate Hydratase from Mycobacterium tuberculosis Using Allosteric Inhibitors with a Dimeric-Binding Mode.
Andrew J Whitehouse, M Daben J Libardo, Monica Kasbekar, Paul D Brear, Gerhard Fischer, Craig J Thomas, Clifton E Barry, Helena IM Boshoff, Anthony G Coyne, Chris Abell
Sep 16, 2019
With the growing worldwide prevalence of antibiotic-resistant strains of tuberculosis (TB), new targets are urgently required for the development of treatments with novel modes of action. Fumarate hydratase (fumarase), a...
Structural insights into Escherichia coli phosphopantothenoylcysteine synthetase by native ion mobility-mass spectrometry.
Daniel Shiu-Hin Chan, Jeannine Hess, Elen Shaw, Christina Spry, Robert Starley, Claudio Dagostin, Marcio VB Dias, Ramesh Kale, Vitor Mendes, Tom L Blundell, Anthony G Coyne, Chris Abell
Sep 13, 2019
CoaBC, part of the vital coenzyme A biosynthetic pathway in bacteria, has recently been validated as a promising antimicrobial target. In this work, we employed native ion mobility-mass spectrometry to gain structural insights...
Structural Characterization of Mycobacterium abscessus Phosphopantetheine Adenylyl Transferase Ligand Interactions
Sherine E Thomas, William J McCarthy, Jamal El Bakali, Karen P Brown, So Yeon Kim, Michal Blaszczyk, Vítor Mendes, Chris Abell, R Andres Floto, Anthony G Coyne, Tom L Blundell
Jun 14, 2022
Anti-microbial resistance is a rising global healthcare concern that needs urgent attention as growing number of infections become difficult to treat with the currently available antibiotics. This is particularly true for...
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