User profiles for C Lesburg

Charles Lesburg

Odyssey Therapeutics
Verified email at odysseytx.com
Cited by 3939

Managing and manipulating carbocations in biology: terpenoid cyclase structure and mechanism

CA Lesburg, JM Caruthers, CM Paschall… - Current opinion in …, 1998 - Elsevier
… In this cyclase, substrate ionization is achieved by the protonation of a C=C double bond (Figure
5a). Site-directed mutagenesis studies [23] interpreted in conjunction with the crystal …

An orally available non-nucleotide STING agonist with antitumor activity

…, J Kopinja, BM Lacey, J Laskey, CA Lesburg… - Science, 2020 - science.org
INTRODUCTION Activation of the STING (stimulator of interferon genes) protein by its natural
ligand, cyclic guanosine monophosphate–adenosine monophosphate (cGAMP), triggers …

Crystal structure of pentalenene synthase: mechanistic insights on terpenoid cyclization reactions in biology

CA Lesburg, G Zhai, DE Cane, DW Christianson - Science, 1997 - science.org
… The structural diversity and stereochemical complexity of the C 15 -isoprenoid skeletons
of these metabolites are remarkable. Indeed, of the more than 300 cyclic sesquiterpenes that …

Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site

CA Lesburg, MB Cable, E Ferrari, Z Hong… - Nature structural …, 1999 - nature.com
Various classes of nucleotidyl polymerases with different transcriptional roles contain a
conserved core structure. Less is known, however, about the distinguishing features of these …

A kinase-cGAS cascade to synthesize a therapeutic STING activator

…, SP Miller, FR Tsay, MD Altman, CA Lesburg… - Nature, 2022 - nature.com
… at 16 C at 250 rpm with 85% RH. Cells were harvested by centrifugation at 4,000 rpm at 4 C
for 20 min and the media discarded. The cell pellets were stored at −80 C until ready for use. …

Discovery of MK-1454: a potent cyclic dinucleotide stimulator of interferon genes agonist for the treatment of cancer

W Chang, MD Altman, CA Lesburg… - Journal of Medicinal …, 2022 - ACS Publications
… lid residues such as Gly-230 and Gly-234 (Figure 2C, right), as well as several other regions
in the spectra (Figure 2C, left, for example), consistent with the pronounced changes in the …

Reversal of the hydrogen bond to zinc ligand histidine-119 dramatically diminishes catalysis and enhances metal equilibration kinetics in carbonic anhydrase II

C Huang, CA Lesburg, LL Kiefer, CA Fierke… - Biochemistry, 1996 - ACS Publications
… Optical absorption spectra were collected on 60 μM Co 2+ -E117Q CAII in 10 mM buffer (Tris,
pH 8.0, and CHES, pH 9.1 and 9.9) at 25 C with the same concentration of Zn 2+ -enzyme …

Discovery of a novel cGAMP competitive ligand of the inactive form of STING

…, T Ho, J Jewell, BM Lacey, CA Lesburg… - ACS medicinal …, 2018 - ACS Publications
Drugging large protein pockets is a challenge due to the need for higher molecular weight
ligands, which generally possess undesirable physicochemical properties. In this …

X-ray crystallographic studies of engineered hydrogen bond networks in a protein-zinc binding site

CA Lesburg, DW Christianson - Journal of the American Chemical …, 1995 - ACS Publications
… 67Similarly, D235 in cytochrome c peroxidase, which forms a hydrogen bond to proximal …
,7 The neutralization of side chain charge in D235N cytochrome c peroxidase results in a 5-fold …

Histidine→ carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity

CA Lesburg, C Huang, DW Christianson… - Biochemistry, 1997 - ACS Publications
… calculated using the Kaleidagraph 3.0 (Synergy Software) curve-fitting program with eq 4
where C ranged from 0.9 to 1.1. … c K D for dansylamide measured in 50 mM MOPS, pH 7.9, 25 …