Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα 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.

Read Publication

First-Generation Structure-Activity Relationship Studies of 2,3,4,9-tetrahydro-1H-carbazol-1-amines as CpxA Phosphatase Inhibitors

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

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

Read Publication

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 Infec. Dis., 2019, 5, 79.

Read Publication

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, Y; Ma, J.; Duerfeldt, A.S.

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

Read Publication

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

Read Publication

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.l.; Duerfeldt, A.S.

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

Read Publication

Recent Advances Towards Rational Antibacterial Discovery: Addressing Permeation and Efflux

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

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

Read Publication

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.

Read Publication

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.; Kizziah, J.L.; Lieberman, R.L.; Dickey, C.A.; Blagg, B.S.J.

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

Read Publication

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.

Read Publication


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, 5084–5087.

Read Publication

Stereoselective Syntheses of (–)-Pyrimidoblamic Acid and P-3A

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

J. Am. Chem. Soc., 2014, 136, 2119−2125.

Read Publication

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, 6845–6857.

Read Publication

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, 40661–40669.

Read Publication

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, 9796–9804.

Read Publication

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, 7170–7174.

Read Publication

Hsp90 Inhibition: Elimination of Shock and Stress

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

Bioorg. & Med. Chem. Lett., 2010, 20, 4983−4987.

Read Publication

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

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

Bioorg. & Med. Chem. Lett., 2009, 19, 6845−6850.

Read Publications

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

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

Org. Lett., 2009, 11, 2353−2356.

Read Publication

Hydrating for Resistance to Radicicol

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

ACS Chem. Biol., 2009, 4, 245−247.

Read Publication