In Vitro Antimicrobials

• The contribution of neutrophils to bacteriophage clearance and pharmacokinetics in vivo. Arne E et al. JCI Insight. 2024;9(20):e181309. https://doi.org/10.1172/jci.insight.181309.
• A pleurocidin analogue with greater conformational flexibility, enhanced antimicrobial potency and in vivo therapeutic efficacy. Mango Z et al. Commun Biol. 2022 Nov;3:697. https://doi.org/10.1038/s42003-020-01420-3
• Rational design of balanced dual-targeting antibiotics with limited resistance. Nyerges A et al. PLoS Biol. 2020 Oct;18(10):e3000819. https://doi.org/10.1371/journal.pbio.3000819
• A dual-mechanism antibiotic kills gram-negative bacteria and avoids drug resistance. MARTIN II JK et al. Cell. 2020 Jun;181(7):1518-1532. https://doi.org/10.1016/j.cell.2020.05.005
• Potent LpxC Inhibitors with In vitro Activity against Multidrug-Resistant Pseudomonas aeruginosa. Krause KM et al. Antimicrob Agents Chemother. 2019 Oct;63(11):e00977-19. https://10.1128/AAC.00977-19. Print 2019 Nov.
• OG716: Designing a fit-for-purpose lantibiotic for the treatment of Clostridium difficile infections. Kers JA et al. PLoS One. 2018 Jun ;13(6):e0197467. https://doi.org/10.1371/journal.pone.0197467
• In Vitro and In Vivo Efficacy of a Novel and Long-Acting Fungicidal Azole, PC1244, on Aspergillus fumigatus Infection. Colley T et al. Antimicrob Agents Chemother. 2018 Apr;62(5):e01941-17. https://doi.org/10.1128/AAC.01941-17
• Mutacin 1140 Lantibiotic Variants Are Efficacious Against Clostridium difficile Infection. Kers JA et al. Front. Microbiol. 2018 Mar;9:415. https://doi.org/10.3389/fmicb.2018.00415
• In Vivo Biomarker Analysis of the Effects of Intranasally Dosed PC945, a Novel Antifungal Triazole, on Aspergillus fumigatus Infection in Immunocompromised Mice. Kimura G et al. Antimicrobial agents and chemotherapy. 2017 Aug;61(9):e00124-17. https://doi.org/10.1128/AAC.00124-17
• Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors. Yates CM et al. Bioorg Med Chem Lett. 2017 Aug;27(15):3243-3248. https://doi.org/10.1016/j.bmcl.2017.06.037
• In Vitro and In Vivo Antifungal Profile of a Novel and Long-Acting Inhaled Azole, PC945, on Aspergillus fumigatus Infection. Colley T et al. Antimicrob. Agents Chemother. 2017 Apr;61(5):e02280-16. https://doi.org/10.1128/AAC.02280-16

In Vivo Antimicrobials

• Vancomycin-arginine (STM-001) abrogates ESBL carrier and carbapenem-resistant Escherichia coli burden in a murine complicated urinary tract infection model. Neville LF et al. J. Antimicrob. Chemother. 2022 Jan;77(6):1706-1709. https://doi.org/10.1093/jac/dkac063
• A novel oral GyrB/ParE dual binding inhibitor effective against multidrug resistant Neisseria gonorrhoeae and other high-threat pathogens. Park S et al. bioRxiv. 2022.03.23.485573. https://doi.org/10.1101/2022.03.23.485573
• Antibacterial activity of apramycin at acidic pH warrants wide therapeutic window in the treatment of complicated urinary tract infections and acute pyelonephritis. Becker K et al. EBioMedicine. 2021 Nov;73:103652. https://doi.org/10.1016/j.ebiom.2021.103652
• Initial efficacy determination and resistance profile of anti-Acinetobacter antibiotics, turnercyclamycins. Miller BW et al. bioRxiv. 2021.11.01.466777. https://doi.org/10.1101/2021.11.01.466777
• Efficacy of Rezafungin in Prophylactic Mouse Models of Invasive Candidiasis, Aspergillosis, and Pneumocystis Pneumonia. Miesel L et al. Antimicrob Agents and Chemother. 2021 Feb;65(3):e01992-20. https://doi.org/10.1128/AAC.01992-20
• A dual-mechanism antibiotic kills gram-negative bacteria and avoids drug resistance. MARTIN II JK et al. Cell. 2020 Jun;181(7):1518-1532. https://doi.org/10.1016/j.cell.2020.05.005
• Discovery of Cephalosporin-3'-Diazeniumdiolates That Show Dual Antibacterial and Antibiofilm Effects Against Pseudomonas aeruginosa Clinical Cystic Fibrosis Isolates and Efficacy in a Murine Respiratory Infection Model. Rineh A et al. ACS Infect Dis. 2020 Jun;6(6):1460-1479. https://doi.org/10.1021/acsinfecdis.0c00070
• C1-CBP-vancomycin: Impact of a Vancomycin C-Terminus Trimethylammonium Cation on Pharmacological Properties and Insights Into Its Newly Introduced Mechanism of Action. Wu Zhi-Chen et al. J Org Chem. 2020 Feb;85(3):1365-1375. https://doi.org/10.1021/acs.joc.9b02314
• Rezafungin treatment in mouse models of invasive candidiasis and aspergillosis: Insights on the PK/PD pharmacometrics of rezafungin efficacy. Miesel L et al. Pharmacol Res Perspect. 2019 Nov;7(6):e00546. https://doi.org/10.1002/prp2.546
• Rapid evolution of reduced susceptibility against a balanced dual-targeting antibiotic through stepping-stone mutations. Szili P et al. Antimicrob Agents Chemother. 2019 Jun;63(9):e00207-19. https://doi.org/10.1128/AAC.00207-19
• Antibiotic usage promotes the evolution of resistance against gepotidacin, a novel multi-targeting drug. Wannier TM et al. Proc. Natl. Acad. Sci. 2020;117(24):13689-13698. https://doi.org/10.1101/495630
• Discovery of cationic nonribosomal peptides as Gram-negative antibiotics through global genome mining. Li XY et al. Nat Commun. 2018 Aug;9(1):3273. https://doi.org/10.1038/s41467-018-05781-6
• Cysteamine, an Endogenous Aminothiol, and Cystamine, the Disulfide Product of Oxidation, Increase Pseudomonas aeruginosa Sensitivity to Reactive Oxygen and Nitrogen Species and Potentiate Therapeutic Antibiotics against Bacterial Infection. Fraser-Pitt DJ et al. Infect Immun. 2018 May;86(6):e00947-17. https://doi.org/10.1128/IAI.00947-17
• Protein-inspired antibiotics active against vancomycin- and daptomycin-resistant bacteria. Blaskovich MAT et al. Nat Commun. 2018 Jan;9(1):22. https://doi.org/10.1038/s41467-017-02123-w
• The rumen microbiome: an underexplored resource for novel antimicrobial discovery. Oyama LB et al., NPJ Biofilms Microbiomes. 2017 Dec;3:33. https://doi.org/10.1038/s41522-017-0042-1
• Pharmacological Basis of CD101 Efficacy: Exposure Shape Matters. Lakota EA et al. Antimicrob Agents Chemother. 2017 Oct;61(11) : e00758-17. https://doi.org/10.1128/AAC.00758-17
• Efficacy of a Novel Tricyclic Topoisomerase Inhibitor in a Murine Model of Neisseria gonorrhoeae Infection. Savage VJ et al. Antimicrob Agents Chemother. 2016 Aug;60(9):5592-5594. https://doi.org/10.1128/AAC.00913-16
• Antibacterial activity of the novel semisynthetic lantibiotic NVB333 in vitro and in experimental infection models. Boakes S et al. J. Antibiot. 2016 Dec;69(12):850-857. https://doi.org/10.1038/ja.2016.47
• Preclinical development of Ramizol, an antibiotic belonging to a new class, for the treatment of Clostridium difficile colitis. Rao S et al. J. Antibiot. 2016 Dec;69(12):879-884. https://doi.org/10.1038/ja.2016.45

CNS/Pain

• Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management. Peng Y et al. Journal of medicinal chemistry. 2020 Dec;64(1):890–904. https://doi.org/10.1021/acs.jmedchem.0c01964
• Aquaporin-4 facilitator TGN-073 demonstrates novel analgesic activity. Huber VJ. bioRxiv. 2018 Oct:403311. https://doi.org/10.1101/403311

Inflammation / Allergy

• D-cycloserine effects on COPD and depression in a murine experimental model. Heresco-Levy, Uriel, et al. Frontiers in Pharmacology 16 (2025): 1554337. https://doi.org/10.3389/fphar.2025.1554337
• Probing the Role of Melanocortin Type 1 Receptor Agonists in Diverse Immunological Diseases. Spana C et al. Front. Pharmacol. 2019 Jan;9:1535. https://doi.org/10.3389/fphar.2018.01535
• Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. Soeberdt M et al. J. Med. Chem. 2017 Mar;60(6):2526-2551. https://doi.org/10.1021/acs.jmedchem.6b01868
• A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030. Palmgvist N et al. J Inflamm. 2016 Jun;13:20. https://doi.org/10.1186/s12950-016-0127-2
• G protein-coupled bile acid receptor 1 stimulation mediates arterial vasodilation through a K(Ca)1.1 (BK(Ca))-dependent mechanism. Fryer RM et al. J Pharmacol Exp Ther. 2014 Mar;348(3):421-31. https://doi.org/10.1124/jpet.113.210005

Metabolic

• Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. Chen YS et al. PLoS One. 2021 Aug;16(8):e0255405. https://doi.org/10.1371/journal.pone.0255405

In Vivo Oncology

• BC-N102 suppress breast cancer tumorigenesis by interfering with cell cycle regulatory proteins and hormonal signaling, and induction of time-course arrest of cell cycle at G1/G0 phase. Lawal B et al. Int J Biol Sci. 2021 Jul;17(12):3224-3238. https://doi.org/10.7150%2Fijbs.62808
• A novel selective AKR1C3-activated prodrug AST-3424/OBI-3424 exhibits broad anti-tumor activity. Meng F et al. Am J Cancer Res. 2021 Jul;11(7):3645-3659.
• Anti-inflammatory nitro-fatty acids suppress tumor growth by triggering mitochondrial dysfunction and activation of the intrinsic apoptotic pathway in colorectal cancer cells. Kuhn B et al. Biochem Pharmacol. 2018 Sep;155:48-60. https://doi.org/10.1016/j.bcp.2018.06.014

In Vivo PK

• Translational in vitro and in vivo PKPD modelling for apramycin against Gram-negative lung pathogens to facilitate prediction of human efficacious dose in pneumonia. Vincent AC et al. Clin. Microbiol. Infect. 2022 Oct;28(10);1367-1374. https://doi.org/10.1016/j.cmi.2022.05.003
• A selective p53 activator and anticancer agent to improve colorectal cancer therapy. Ramos H et al. Cell Rep. 2021 Apr;35(2):108982. https://doi.org/10.1016/j.celrep.2021.108982
• Betulinic acid hydroxamate prevents colonic inflammation and fibrosis in murine models of inflammatory bowel disease. Prados ME et al. Acta Pharmacol Sin. 2021 Aug;42;1124–1138. https://doi.org/10.1038/s41401-020-0497-0
• Formulation, stability, pharmacokinetic, and modeling studies for tests of synergistic combinations of orally available approved drugs against ebola virus in vivo. Finch CL et al. Microorganisms. 2021 Mar;9(3):566. https://doi.org/10.3390/microorganisms9030566
• Vitamin E Phosphate Nucleoside Prodrugs: A Platform for Intracellular Delivery of Monophosphorylated Nucleosides. Diafuku R et al. Pharmaceuticals. 2018 Feb;11(1). https://doi.org/10.3390/ph11010016
• 5-aza-2',2'-Difluoro Deoxycytidine (NUC013): A Novel Nucleoside DNA Methyl Transferase Inhibitor and Ribonucleotide Reductase Inhibitor for the Treatment of Cancer. Diafuku R et al. Pharmaceuticals. 2017 Jul 20;10(3):65. https://doi.org/10.3390/ph10030065
• BCAT1 controls metabolic reprogramming in activated human macrophages and is associated with inflammatory diseases. Papathanassiu AE et al. Nat Commun. 2017 Jul;8:16040. https://doi.org/10.1038/ncomms16040

In Vivo Safety Pharmacology

• Anti-HIV-1 Activity of pepRF1, a Proteolysis-Resistant CXCR4 Antagonist Derived from Dengue Virus Capsid Protein. Cadima-Couto I et al. ACS Infect. Dis. 2020 Dec;7(1):6-22. https://doi.org/10.1021/acsinfecdis.9b00507
• Optimization of Substrate‐Analogue Furin Inhibitors. Ivanova T et al. ChemMedChem. 2017 Oct; 12(23):1953-1968. https://doi.org/10.1002/cmdc.201700596