Crystal Structure of the IMP-1 Metallo β-Lactamase from Pseudomonas aeruginosa and Its Complex with a Mercaptocarboxylate Inhibitor:  Binding Determinants of a Potent …

NO Concha, CA Janson, P Rowling, S Pearson… - Biochemistry, 2000 - ACS Publications
Metallo β-lactamase enzymes confer antibiotic resistance to bacteria by catalyzing the hydrolysis
of β-lactam antibiotics. This relatively new form of resistance is spreading unchallenged …

Identification of a series of tricyclic natural products as potent broad-spectrum inhibitors of metallo-β-lactamases

…, H Boyd, NO Concha… - Antimicrobial agents …, 2002 - Am Soc Microbiol
This work describes the discovery and characterization of a novel series of tricyclic natural
product-derived metallo-β-lactamase inhibitors. Natural product screening of the Bacillus …

[HTML][HTML] Crystal structure of the wide-spectrum binuclear zinc β-lactamase from Bacteroides fragilis

NO Concha, BA Rasmussen, K Bush, O Herzberg - Structure, 1996 - cell.com
Background: The metallo-β-lactamase from Bacteroides fragilis hydrolyzes a wide range of β-lactam
antibiotics, and is not clinically susceptible to any known β-lactamase inhibitors. B. …

[PDF][PDF] A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC

…, P McDevitt, T Ho, M Crouthamel, TK Hart, NO Concha… - Cancer cell, 2015 - cell.com
Epigenetic dysregulation has emerged as an important mechanism in cancer. Alterations in
epigenetic machinery have become a major focus for targeted therapies. The current report …

[HTML][HTML] Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality

…, PJ McDevitt, K Johanson, NO Concha… - Journal of Biological …, 2000 - ASBMB
Caspases have been strongly implicated to play an essential role in apoptosis. A critical
question regarding the role(s) of these proteases is whether selective inhibition of an effector …

[HTML][HTML] Structural basis for Chk1 inhibition by UCN-01

…, KO Johanson, SM Green, NO Concha… - Journal of Biological …, 2002 - ASBMB
Chk1 is a serine-threonine kinase that plays an important role in the DNA damage response,
including G 2 /M cell cycle control. UCN-01 (7-hydroxystaurosporine), currently in clinical …

[PDF][PDF] Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss

…, C Wagner, F Zappacosta, R Annan, NO Concha… - Cancer cell, 2019 - cell.com
Type I protein arginine methyltransferases (PRMTs) catalyze asymmetric dimethylation of
arginines on proteins. Type I PRMTs and their substrates have been implicated in human …

3-(1,1-Dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, Potent Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase

…, AN Shaw, R Bambal, D Chai, NO Concha… - Journal of medicinal …, 2006 - ACS Publications
Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high-throughput
screening (HTS) of the GlaxoSmithKline proprietary compound collection. This …

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a …

…, SY Zhang, EA Minthorn, NO Concha… - Journal of medicinal …, 2008 - ACS Publications
Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of
dominant negative AKT blocks the ability of a variety of growth factors to promote survival. …

Annexin V forms calcium-dependent trimeric units on phospholipid vesicles

NO Concha, JF Head, MA Kaetzel, JR Dedman… - FEBS letters, 1992 - Elsevier
The quaternary structure of annexin V, a calcium-dependent phospholipid binding protein,
was investigated by chemical cross-linking. Calcium was found to induce the formation of …