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» Authors » Emanuele Perola

Emanuele Perola

Explore the profile of Emanuele Perola including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 25
Citations 857
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Paul S Charifson
Tiansheng Wang
Upul K Bandarage
Wenxin Gu
Steven M Jones
Michael P Clark
Yunyi Wei
Joshua R Leeman
Christine Memmott
Mark W Ledeboer
Published In
J Med Chem
Bioorg Med Chem Lett
J Chem Inf Model
ACS Med Chem Lett
Proteins
Affiliations
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Recent Articles
1.
Evaluation of STK17B as a cancer immunotherapy target utilizing highly potent and selective small molecule inhibitors
Scheuplein F, Renner F, Campbell J, Campbell R, De Savi C, Eckmann J, et al.
Front Immunol . 2024 Nov; 15:1411395. PMID: 39502695
Introduction: The serine/threonine kinase 17B (STK17B) is involved in setting the threshold for T cell activation and its absence sensitizes T cells to suboptimal stimuli. Consequently, STK17B represents an attractive...
2.
Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer
Eno M, Brubaker J, Campbell J, De Savi C, Guzi T, Williams B, et al.
J Med Chem . 2022 Jul; 65(14):9662-9677. PMID: 35838760
While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have changed the treatment landscape for EGFR mutant (L858R and ex19del)-driven non-small-cell lung cancer (NSCLC), most patients will eventually develop...
3.
2-N-Arylthiazole inhibitors of Mycobacterium tuberculosis
Clark M, Wang T, Perola E, Deininger D, Zuccola H, Jones S, et al.
Bioorg Med Chem Lett . 2017 Aug; 27(17):3987-3991. PMID: 28778468
To develop agents for the treatment of infections caused by Mycobacterium tuberculosis, a novel phenotypic screen was undertaken that identified a series of 2-N-aryl thiazole-based inhibitors of intracellular Mycobacterium tuberculosis....
4.
Novel 2-Substituted 7-Azaindole and 7-Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza
Bandarage U, Clark M, Perola E, Gao H, Jacobs M, Tsai A, et al.
ACS Med Chem Lett . 2017 Feb; 8(2):261-265. PMID: 28197323
JNJ-63623872 () is a first-in-class, orally bioavailable compound that offers significant potential for the treatment of pandemic and seasonal influenza. Early lead optimization efforts in our 7-azaindole series focused on...
5.
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2
Farmer L, Clark M, Boyd M, Perola E, Jones S, Tsai A, et al.
ACS Med Chem Lett . 2017 Feb; 8(2):256-260. PMID: 28197322
In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the PB2 subunit of the influenza polymerase...
6.
Fragment-Based Discovery of Dual JC Virus and BK Virus Helicase Inhibitors
Bonafoux D, Nanthakumar S, Bandarage U, Memmott C, Lowe D, Aronov A, et al.
J Med Chem . 2016 Jul; 59(15):7138-51. PMID: 27385654
There are currently no treatments for life-threatening infections caused by human polyomaviruses JCV and BKV. We therefore report herein the first crystal structure of the hexameric helicase of JCV large...
7.
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors
Boyd M, Bandarage U, Bennett H, Byrn R, Davies I, Gu W, et al.
Bioorg Med Chem Lett . 2015 Apr; 25(9):1990-4. PMID: 25827523
VX-787 is a first in class, orally bioavailable compound that offers unparalleled potential for the treatment of pandemic and seasonal influenza. As a part of our routine SAR exploration, carboxylic...
8.
Novel inhibitors of cholesterol degradation in Mycobacterium tuberculosis reveal how the bacterium's metabolism is constrained by the intracellular environment
VanderVen B, Fahey R, Lee W, Liu Y, Abramovitch R, Memmott C, et al.
PLoS Pathog . 2015 Feb; 11(2):e1004679. PMID: 25675247
Mycobacterium tuberculosis (Mtb) relies on a specialized set of metabolic pathways to support growth in macrophages. By conducting an extensive, unbiased chemical screen to identify small molecules that inhibit Mtb...
9.
Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit
Byrn R, Jones S, Bennett H, Bral C, Clark M, Jacobs M, et al.
Antimicrob Agents Chemother . 2014 Dec; 59(3):1569-82. PMID: 25547360
VX-787 is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. Viral genetics and X-ray crystallography studies provide support for...
10.
A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections
Locher C, Jones S, Hanzelka B, Perola E, Shoen C, Cynamon M, et al.
Antimicrob Agents Chemother . 2014 Dec; 59(3):1455-65. PMID: 25534737
New drugs to treat drug-resistant tuberculosis are urgently needed. Extensively drug-resistant and probably the totally drug-resistant tuberculosis strains are resistant to fluoroquinolones like moxifloxacin, which target gyrase A, and most...