Benjamin P Fauber
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Explore the profile of Benjamin P Fauber including associated specialties, affiliations and a list of published articles.
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25
Citations
655
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Recent Articles
1.
Wei B, Robarge K, Labadie S, Chen J, Corson L, DiPasquale A, et al.
Bioorg Med Chem Lett
. 2022 Jan;
59:128576.
PMID: 35065235
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement...
2.
Purkey H, Robarge K, Chen J, Chen Z, Corson L, Ding C, et al.
ACS Med Chem Lett
. 2016 Oct;
7(10):896-901.
PMID: 27774125
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with...
3.
Rene O, Fauber B, Barnard A, Chapman K, Deng Y, Eidenschenk C, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(18):4455-4461.
PMID: 27524313
Modification of the δ-sultam ring of RORc inverse agonist 2 led to the discovery of more polar oxa-sultam 65. The less lipophilic inverse agonist (65) displayed high potency in a...
4.
Rene O, Stepek I, Gobbi A, Fauber B, Gaines S
J Org Chem
. 2015 Sep;
80(20):10218-25.
PMID: 26378765
A palladium(0)-catalyzed rearrangement of piperidones and piperidines bearing a spirocyclopropane ring was developed. The ring expansion reaction led to a variety of functionalized caprolactam and azepane products in good to...
5.
Fauber B, Gobbi A, Savy P, Burton B, Deng Y, Everett C, et al.
Bioorg Med Chem Lett
. 2015 Sep;
25(19):4109-13.
PMID: 26321361
A high-throughput screen of the Genentech/Roche compound collection using a retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) biochemical assay revealed a N-sulfonyl-tetrahydroquinoline hit. Herein, we describe the...
6.
Fauber B, Rene O, Deng Y, Devoss J, Eidenschenk C, Everett C, et al.
J Med Chem
. 2015 Jun;
58(13):5308-22.
PMID: 26061388
Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed...
7.
Fauber B, Gobbi A, Robarge K, Zhou A, Barnard A, Cao J, et al.
Bioorg Med Chem Lett
. 2015 Jun;
25(15):2907-12.
PMID: 26048793
The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in...
8.
Rene O, Fauber B, De Leon Boenig G, Burton B, Eidenschenk C, Everett C, et al.
ACS Med Chem Lett
. 2015 Mar;
6(3):276-81.
PMID: 25815138
A minor structural change to tertiary sulfonamide RORc ligands led to distinct mechanisms of action. Co-crystal structures of two compounds revealed mechanistically consistent protein conformational changes. Optimized phenylsulfonamides were identified...
9.
Rutz S, Kayagaki N, Phung Q, Eidenschenk C, Noubade R, Wang X, et al.
Nature
. 2014 Dec;
518(7539):417-21.
PMID: 25470037
T-helper type 17 (TH17) cells that produce the cytokines interleukin-17A (IL-17A) and IL-17F are implicated in the pathogenesis of several autoimmune diseases. The differentiation of TH17 cells is regulated by...
10.
Fauber B, Dragovich P, Chen J, Corson L, Ding C, Eigenbrot C, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(24):5683-5687.
PMID: 25467161
A series of 3,6-disubstituted dihydropyrones were identified as inhibitors of human lactate dehydrogenase (LDH)-A. Structure activity relationships were explored and a series of 6,6-spiro analogs led to improvements in LDHA...