James J-W Duan
Overview
Explore the profile of James J-W Duan including associated specialties, affiliations and a list of published articles.
Author names and details appear as published. Due to indexing inconsistencies, multiple individuals may share a name, and a single author may have variations. MedLuna displays this data as publicly available, without modification or verification
Snapshot
Snapshot
Articles
37
Citations
249
Followers
0
Related Specialties
Related Specialties
Top 10 Co-Authors
Top 10 Co-Authors
Published In
Affiliations
Affiliations
Soon will be listed here.
Recent Articles
1.
Xiao H, Li N, Duan J, Jiang B, Lu Z, Ngu K, et al.
J Med Chem
. 2020 Dec;
63(23):15050-15071.
PMID: 33261314
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both the...
2.
Jiang B, Duan J, Stachura S, Karmakar A, Hemagiri H, Raut D, et al.
Bioorg Med Chem Lett
. 2020 Aug;
30(17):127392.
PMID: 32738966
A novel series of cis-3,4-diphenylpyrrolidines were designed as RORγt inverse agonists based on the binding conformation of previously reported bicyclic sulfonamide 1. Preliminary synthesis and structure-activity relationship (SAR) study established...
3.
Duan J, Jiang B, Lu Z, Stachura S, Weigelt C, Sack J, et al.
Bioorg Med Chem Lett
. 2020 Aug;
30(19):127441.
PMID: 32736080
In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6-difluorobenzyl ether series of cyclopentyl sulfones were found to be surprisingly more potent than...
4.
Cherney R, Cornelius L, Srivastava A, Weigelt C, Marcoux D, Duan J, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1221-1227.
PMID: 32551004
Novel tricyclic analogues were designed, synthesized, and evaluated as RORγt inverse agonists. Several of these compounds were potent in an IL-17 human whole blood assay and exhibited excellent oral bioavailability...
5.
Harikrishnan L, Gill P, Kamau M, Qin L, Ruan Z, OMalley D, et al.
Bioorg Med Chem Lett
. 2020 Apr;
30(12):127204.
PMID: 32334911
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in...
6.
Marcoux D, Duan J, Shi Q, Cherney R, Srivastava A, Cornelius L, et al.
J Med Chem
. 2019 Oct;
62(21):9931-9946.
PMID: 31638797
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential target...
7.
Lu Z, Duan J, Xiao H, Neels J, Wu D, Weigelt C, et al.
Bioorg Med Chem Lett
. 2019 Jul;
29(16):2265-2269.
PMID: 31257087
An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that the cyclohexane carboxylic acid group of compound 2...
8.
Duan J, Lu Z, Jiang B, Stachura S, Weigelt C, Sack J, et al.
ACS Med Chem Lett
. 2019 Mar;
10(3):367-373.
PMID: 30891142
A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide . Through a combination of structure-based design and structure-activity relationship...
9.
Gong H, Weinstein D, Lu Z, Duan J, Stachura S, Haque L, et al.
Bioorg Med Chem Lett
. 2017 Dec;
28(2):85-93.
PMID: 29233651
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity...
10.
Kempson J, Ovalle D, Guo J, Wrobleski S, Lin S, Spergel S, et al.
Bioorg Med Chem Lett
. 2017 Sep;
27(20):4622-4625.
PMID: 28927786
A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design was based on crystal structure information and...