Search Results - "Mesleh, Michael F."
-
1
A High-Throughput Platform to Identify Small-Molecule Inhibitors of CRISPR-Cas9
Published in Cell (02-05-2019)“…The precise control of CRISPR-Cas9 activity is required for a number of genome engineering technologies. Here, we report a generalizable platform that provided…”
Get full text
Journal Article -
2
Three-dimensional Structure of the Channel-forming Trans-membrane Domain of Virus Protein “u” (Vpu) from HIV-1
Published in Journal of molecular biology (17-10-2003)“…The three-dimensional structure of the channel-forming trans-membrane domain of virus protein “u” (Vpu) of HIV-1 was determined by NMR spectroscopy in micelle…”
Get full text
Journal Article -
3
Characterization of the Prion Protein Binding Properties of Antisense Oligonucleotides
Published in Biomolecules (Basel, Switzerland) (18-12-2019)“…Antisense oligonucleotides (ASOs) designed to lower prion protein (PrP) expression in the brain through RNase H1-mediated degradation of PrP RNA are in…”
Get full text
Journal Article -
4
An efficient chemical synthesis of carboxylate-isostere analogs of daptomycin
Published in Organic & biomolecular chemistry (28-07-2013)“…Herein we report a direct and efficient method for the synthesis of four new carboxylate-isostere analogs of daptomycin. The side chain carboxylic acid…”
Get more information
Journal Article -
5
Structure of the Coat Protein in fd Filamentous Bacteriophage Particles Determined by Solid-State NMR Spectroscopy
Published in Proceedings of the National Academy of Sciences - PNAS (27-05-2003)“…The atomic resolution structure of fd coat protein determined by solid-state NMR spectroscopy of magnetically aligned filamentous bacteriophage particles…”
Get full text
Journal Article -
6
Discovery of a First-in-Class Inhibitor of the PRMT5–Substrate Adaptor Interaction
Published in Journal of medicinal chemistry (12-08-2021)“…PRMT5 and its substrate adaptor proteins (SAPs), pICln and Riok1, are synthetic lethal dependencies in MTAP-deleted cancer cells. SAPs share a conserved PRMT5…”
Get full text
Journal Article -
7
NMR Structural Characterization of a Minimal Peptide Antagonist Bound to the Extracellular Domain of the Corticotropin-releasing Factor1 Receptor
Published in The Journal of biological chemistry (02-03-2007)“…Natural peptide agonists of corticotrophin-releasing factor (CRF) receptors bind to the receptor by a two-site mechanism as follows: the carboxyl end of the…”
Get full text
Journal Article -
8
A drug discovery toolbox for Nuclear Magnetic Resonance (NMR) characterization of ligands and their targets
Published in Drug discovery today. Technologies (01-12-2020)“…Information about the structure, dynamics, and ligand-binding properties of biomolecules can be derived from Nuclear Magnetic Resonance (NMR) spectroscopy and…”
Get full text
Journal Article -
9
A general approach to identify cell-permeable and synthetic anti-CRISPR small molecules
Published in Nature cell biology (01-12-2022)“…The need to control the activity and fidelity of CRISPR-associated nucleases has resulted in a demand for inhibitory anti-CRISPR molecules. The small-molecule…”
Get full text
Journal Article -
10
Multimodal small-molecule screening for human prion protein binders
Published in The Journal of biological chemistry (25-09-2020)“…Prion disease is a rapidly progressive neurodegenerative disorder caused by misfolding and aggregation of the prion protein (PrP), and there are currently no…”
Get full text
Journal Article -
11
The Autophagy-Related Beclin‑1 Protein Requires the Coiled-Coil and BARA Domains To Form a Homodimer with Submicromolar Affinity
Published in Biochemistry (Easton) (26-12-2017)“…Beclin-1 (BECN1) is an essential component of macroautophagy. This process is a highly conserved survival mechanism that recycles damaged cellular components…”
Get full text
Journal Article -
12
Structure–Activity Relationship Studies of a Series of Semisynthetic Lipopeptides Leading to the Discovery of Surotomycin, a Novel Cyclic Lipopeptide Being Developed for the Treatment of Clostridium difficile-Associated Diarrhea
Published in Journal of medicinal chemistry (25-06-2015)“…Novel cyclic lipopeptides with different acyl tails were synthesized via a semisynthetic approach. Structure–activity relationship studies revealed that…”
Get full text
Journal Article -
13
Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB
Published in Bioorganic & medicinal chemistry letters (15-02-2016)“…[Display omitted] Inhibitors of the ATPase function of bacterial DNA gyrase, located in the GyrB subunit and its related ParE subunit in topoisomerase IV, have…”
Get full text
Journal Article -
14
Targeting Bacterial Cell Wall Peptidoglycan Synthesis by Inhibition of Glycosyltransferase Activity
Published in Chemical biology & drug design (01-02-2016)“…Synthesis of bacterial cell wall peptidoglycan requires glycosyltransferase enzymes that transfer the disaccharide–peptide from lipid II onto the growing…”
Get full text
Journal Article -
15
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design
Published in ACS medicinal chemistry letters (14-04-2016)“…The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA…”
Get full text
Journal Article -
16
NMR Structure Determination of a Membrane Protein with Two Transmembrane Helices in Micelles: MerF of the Bacterial Mercury Detoxification System
Published in Biochemistry (Easton) (05-04-2005)“…The three-dimensional backbone structure of a membrane protein with two transmembrane helices in micelles was determined using solution NMR methods that rely…”
Get full text
Journal Article -
17
Marmoset Fine B Cell and T Cell Epitope Specificities Mapped onto a Homology Model of the Extracellular Domain of Human Myelin Oligodendrocyte Glycoprotein
Published in Neurobiology of disease (01-03-2002)“…Aberrant association of autoantibodies with myelin oligodendrocyte glycoprotein (MOG), an integral membrane protein of the central nervous system (CNS) myelin,…”
Get full text
Journal Article -
18
Dipolar Waves as NMR maps of helices in proteins
Published in Journal of magnetic resonance (1997) (01-08-2003)“…Dipolar Waves describe the periodic variation in the magnitudes of dipolar couplings in the backbone of a protein as a function of residue number. They provide…”
Get full text
Journal Article -
19
Dipolar Waves Map the Structure and Topology of Helices in Membrane Proteins
Published in Journal of the American Chemical Society (23-07-2003)“…Dipolar waves describe the structure and topology of helices in membrane proteins. The fit of sinusoids with the 3.6 residues per turn period of ideal…”
Get full text
Journal Article -
20
Dipolar Waves as NMR Maps of Protein Structure
Published in Journal of the American Chemical Society (24-04-2002)“…The anisotropy of nuclear spin interactions results in a unique mapping of structure to the resonance frequencies and split tings observed in NMR spectra,…”
Get full text
Journal Article