Our Science

Publications 2015

Our scientific publications in high-quality journals reflect the quality of the innovative research in Entasis’ laboratories.

Foerster S, Golparian D, Jacobsson S, Hathaway L, Low N, Shafer W, Althaus C, Unemo M
Genetic resistance determinants, in vitro time-kill curve analysis and pharmacodynamic functions for the novel topoisomerase II inhibitor ETX0914 (AZD0914) in Neisseria gonorrhoeae
Frontiers in Microbiology (2015)

Su XH, Wang BX, Le WJ, Liu YR, Wan C, Li S, Alm RA, Mueller JP, Rice PA
Multidrug resistant Neisseria gonorrhoeae from Nanjing are sensitive to killing by a novel DNA gyrase inhibitor, ETX0914 (AZD0914)
Antimicrobial Agents Chemotherapy (2015)

Lancaster JW, Mahoney MV, Mandal S, Lawrence KR
Update on Treatment Options for Gonococcal Infections
Pharmacotherapy (2015)

Biedenbach DJ, Huband MD, Hackel M, de Jonge BL, Sahm DF, Bradford PA
In vitro Activity of AZD0914, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor, Against Clinically Relevant Gram-positive and Fastidious Gram-negative Pathogens
Antimicrobial Agents and Chemotherapy (2015)

Basarab GS, Kern G, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, Alm RA, Barvian K, Doig P, Galullo V, Gardner H, Gowravaram M, Huband M, Kimzey A, Morningstar M, Kutschke A, Lahiri SD, Perros M, Singh R, Schuck V, Tommasi R, Walkup G, Newman J
Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases
Nature Scientific Reports (2015)

Kern G , Palmer T, Ehmann DE, Shapiro AB, Andrews B, Basarab GS, Doig P, Fan J, Gao N, Mills SD, Mueller J, Sriram S, Thresher J, Walkup G
Inhibition of Neisseria gonorrhoeae type II Topoisomerases by the Novel Spiropyrimidinetrione AZD0914
Journal of Biological Chemistry (2015)

Basarab GS, Doig P, Galullo V, Kern G, Kimzey A, Kutschke ANewman J, Morningstar M, Mueller J, Otterson L, Vishwanathan KZhou F, Gowravaram M
Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones – Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914)
Journal of Medicinal Chemistry (2015)

Perros M
A sustainable model for antibiotics
Science (2015)

Nayar A, Dougherty T, Ferguson K, Granger B, McWilliams L, Stacey C, Narita S, Tokuda H, Miller A, Brown D, McLeod S
Novel antibacterial targets and compounds revealed by a high throughput cell wall reporter assay
ASM Journal of Bacteriology (2015)

Penwell W, Giacobbe R, Gu R, Patey S, Shapiro S, Gao N, Thresher J, McLaughlin R, Huband M, De Jonge B, Ehmann D, Miller A
The molecular mechanisms of sulbactam antibacterial activity and resistance determinants in Acinetobacter baumannii
Antimicrobial Agents and Chemotherapy (2015)

Waites KB, Crabb DM, Duffy LB, Huband MD
In Vitro Antibacterial Activity of AZD0914 Against Human Mycoplasmas and Ureaplasmas
Antimicrobial Agents and Chemotherapy (2015)

Tommasi R, Brown DG, Walkup GK, Manchester JI, Miller  AA
ESKAPing the Labyrinth of Antibacterial Discovery
Nature Reviews Drug Discovery (2015)

Zhou Y, Joubran C, Miller-Vedam L, Isabella V, Nayar A, Tentarelli S, Miller A
Thinking Outside the “Bug”:  A Unique Assay to Measure Intracellular Drug Penetration in Gram-Negative Bacteria
Analytical Chemistry (2015)

Isabella VM, Campbell AJ, Manchester J, Sylvester M, Nayar AS, Ferguson KE, Tommasi R, Miller A
Toward the Rational Design of Carbapenem Uptake in Pseudomonas aeruginosa.
Chemistry & Biology (Cell) (2015)

Unemo M, Ringlander J, Wiggins C, Fredlund H, Jacobsson S, Cole M
High in vitro susceptibility to the novel spiropyrimidinetrione ETX0914 (also known as AZD0914) among 873 contemporary clinical Neisseria gonorrhoeae isolates in 21 European countries during 2012-2014.
Antimicrobial Agents and Chemotherapy (2015)

McLeod S, Fleming P, MacCormack K, McLaughlin R, Whiteaker J, Narita S, Moric M, Tokuda H, Miller A
Small-Molecule Inhibitors of Gram-Negative Lipoprotein Trafficking Discovered by Phenotypic Screening
ASM Journal of Bacteriology (2015)

“Our scientific approach and expertise, coupled with Entasis’ strong pipeline of programs, really make us stand out in the field of antibacterial drug discovery and development.”

— Satenig Guler, Senior Scientist