Publications

Guiding the Way: Traditional Medicinal Chemistry Inspiration for Rational Gram-Negative Drug Design

Stoorza, A.M. and Duerfeldt, A.S. 

J. Med. Chem., 2024, 67, 65.

Design, Synthesis, and Structure-Activity Relationships of Biaryl Anilines as Subtype-Selective PPAR-alpha Agonists

Lee, J.J.; Hu, Z.; Wang, Y.A.; Nath, D.; Liang, W.; Cui, Y.; Ma, J.X.; Duerfeldt, A.S. 

ACS Med. Chem. Lett., 2023, 14, 766.

The cGAS-STING Pathway in Diabetic Retinopathy and Age-related Macular Degeneration

Hu, B; Ma, J.X.; Duerfeldt, A.S.

Future Med. Chem., 2023, 15, 717.

Structure–Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens

Hu, Z.; Leus, I.V.; Chandar, B.; Sherborne, B.S.; Avila, Q.P.; Rybenkov, V.V.; Zgurskaya, H.I.; Duerfeldt, A.S.

J. Med. Chem., 2022, 65, 14144.

Property Space Mapping of Pseudomonas aeruginosa Permeability to Small Molecules

Leus, I.V.; Weeks, J.W.; Bonifay, V.; Shen, Y.; Yang, L.; Cooper, C.J.; Nash, D.; Duerfeldt, A.S.; Smith, J.C.; Parks, J.M.; Rybenkov, V.V.; Zgurskaya, H.I.

Sci. Rep., 2022, 12, 8220.

CpxA Phosphatase Inhibitor Activates CpxRA and Is a Potential Treatment for Uropathogenic Escherichia coli in a Murine Model of Infection

Fortney, K.R.; Smith, S.N.; van Rensburg, J.J.; Brothwell, J.A.; Gardner, J.J.; Katz, B.P.; Ahsan, N.; Duerfeldt, A.S.; Mobley, H.L.T.; Spinola, S.M.

Microbiol. Spectrum, 2022, 10 (2), e02430-21.

Identification of ClpP Dual Isoform Disruption as an Antisporulation Strategy for Clostridioides difficile

Bishop, C.E.; Shadid, T.M.; Lavey N.P.; Kempher, M.L.; Ballard, J.D.; Duerfeldt, A.S.

J. Bacteriol., 2022, 204, e00411-21.

Small Molecule Modulation of PPARs for the Treatment of Prevalent Vascular Retinal Diseases

Dou, X.; Duerfeldt, A.S.

Int. J. Mol. Sci., 2020, 21, 9251.

Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPAR-alpha Agonists as Leads for Retinal Disorders

Dou, X.; Nath, D.; Shin, H.; Nurmemmedov, E.; Bourne, P.C.; Ma, J.X.; Duerfeldt, A.S.

J. Med. Chem., 2020, 63, 2854.

First-Generation Structure-Activity Relationship Studies of 2,3,4,9-Tetrahydro-1H-carbazole-1-amines and CpxA Phosphatase Inhibitors

Li. Y.; Gardner, J.J.; Fortney, K.R.; Leus, I.V.; Bonifay, V.; Zgurskaya, H.I.; Pletnev, A.A.; Zhang, Z.Y.; Gribble, G.W.; Spinola, S.M.; Duerfeldt, A.S.

Bioorg. Med. Chem. Lett., 2019, 29, 1836.

Clostridium difficile ClpP Homologues are Capable of Uncoupled Activity and Exhibit Different Levels of Susceptibility to Acyldepsipeptide Modulation

Lavey, N.P.; Shadid, T.; Ballard, J.D.; Duerfeldt, A.S.

ACS Infect. Dis., 2019, 5, 79.

Structure-Guided Evolution of a 2-Phenyl-4-Carboxyquinoline Chemotype into PPAR-alpha Selective Agonists: New Leads for Oculovascular Conditions

Dou, X.; Nath, D.; Shin, H.; Ma, J.X.; Duerfeldt, A.S.

Bioorg. Med. Chem. Lett., 2018, 28, 2717.

Structure-Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 to Optimize Paralog-Specific Binding

Que, N.L.S.; Crowley, V.M.; Duerfeldt, A.S.; Zhao, J.; Kent, C.N.; Blagg, B.S.J.; Gewirth, D.T.

J. Med. Chem., 2018, 61, 2793.

Consequences of Depsipeptide Substitution on the ClpP Activation Activity of Antibacterial Acyldepsipeptides

Li, Y.; Lavey, N.P.; Coker, J.A.; Knobbe, J.E.; Truong, D.C.; Yu, H.; Lin, Y.S.; Nimmo, S.I.; Duerfeldt, A.S.

ACS Med. Chem. Lett., 2017, 8, 1171.

Recent Advances Towards Rational Antibacterial Discovery: Addressing Permeation and Efflux

Avila, Q.P.; Zgurskaya, H.I.; Duerfeldt, A.S.

ACS Med. Chem. Rev., 2017, 52, 319.

Sclerotiamide: The First Non-Peptide-Based Natural Product Activator of Bacterial Caseinolytic Protease P

Lavey, N.P.; Coker, J.A.; Ruben, E.A.; Duerfeldt, A.S.

J. Nat. Prod., 2016, 79, 1193.

Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide Scaffold

Crowley, V.M.; Khandelwal, A.; Mishra, S.; Stothert, A.R.; Huard, D.J.E.; Zhao, J.; Muth, A.; Duerfeldt, A.S.; Kizzian, J.L.; Lieberman, R.L.; Dickey, C.A.; Blagg, B.S.J.

J. Med. Chem., 2016, 59, 3471.

Grp94 Delivers Gamma-Aminobutyric Acid Type A (GABA) Receptors to HRD1-Mediated Endoplasmic Reticulum-Associated Degradation

Di, X.J.; Wang, Y.J.; Han, D.Y.; Fu, Y.L.; Duerfeldt, A.S.; Blagg, B.S.J.; Mu, T.W.

J. Biol. Chem., 2016, 291, 9526.

Cycloadditions of Noncomplementary Substituted 1,2,3-Triazines

Anderson, E.A.; Duerfeldt, A.S.; Zhu, K.; Glinkerman, C.M.; Boger, D.L.

Org. Lett., 2014, 16, 5084.

Stereoselective Synthesis of (-)-Pyrimidoblamic Acid and P-3A

Duerfeldt, A.S.; Boger, D.L.

J. Am. Chem. Soc.. 2014, 136, 2119.

Fundamental Relationship between Hydrophobic Properties and Biological Activity for the Duocarmycin Class of DNA Alkylating Antitumor Drugs: Hydrophobic Binding-Driven-Bonding

Wolfe, A.L.; Duncan, K.K.; Lajiness, J.P.; Zhu, K.; Duerfeldt, A.S.; Boger, D.L.

J. Med. Chem., 2013, 56, 6857.

Glucose-Regulated Protein 94 Triage of Mutant Myocilin through Endoplasmic Reticulum-Associated Degradation Subverts a More Efficient Autophagic Clearance Mechanism

Suntharalingam, A.; Abisambra, J.F.; O’Leary, J.C.; Koren III, J.; Zhang. B.; Kuk Joe, M.; Blair, L.J.; Hill, S.E.; Jinwal, U.K.; Cockman, M.; Duerfeldt, A.S.; Tomarev, S.; Blagg, B.S.J.; Lieberman, R.L.; Dickey, C.A. 

J. Biol. Chem., 2012, 287, 40661.

Development of a Grp94 Inhibitor

Duerfeldt, A.S.; Peterson, L.B.; Maynard, J.C.; Ng, C.L.; Eletto, D.; Ostrovsky, O.; Shinogle, H.E.; Moore, D.S.; Argon, Y.; Nicchitta, C.V.; Blagg, B.S.J. 

J. Am. Chem. Soc., 2012, 134, 9796.

Synthesis and Biological Evaluation of Arylated Novobiocin Analogs as Hsp90 Inhibitors

Kusuma, B.R.; Duerfeldt, A.S.; Blagg, B.S.J. 

Bioorg. Med. Chem. Lett., 2011, 21, 7170.

Hsp90 Inhibition: Elimination of Shock and Stress

Duerfeldt, A.S.; Blagg, B.S.J. 

Bioorg. Med. Chem. Lett., 2010, 20, 4983.

Design, Synthesis, and Biological Activity of Bicyclic Radester Analogs as Hsp90 Inhibitors

Jadhav, V.; Duerfeldt, A.S.; Blagg, B.S.J. 

Bioorg. Med. Chem. Lett., 2009, 19, 6845.

Design, Synthesis and Biological Evaluation of Conformationally Constrained cis-Amide Hsp90 Inhibitors

Duerfeldt, A.S.; Brandt, G.E.L.; Blagg, B.S.J. 

Org. Lett., 2009, 11, 2353.

Hydrating for Resistance to Radicicol

Duerfeldt, A.S.; Blagg, B.S.J. 

ACS Chem. Biol., 2009, 4, 245.