William R Roush
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Explore the profile of William R Roush including associated specialties, affiliations and a list of published articles.
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192
Citations
3987
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Recent Articles
1.
Shen D, Byth K, Bertheloot D, Braams S, Bradley S, Dean D, et al.
J Med Chem
. 2025 Mar;
68(5):5529-5550.
PMID: 40036600
The discovery of DFV890 (()-), a potent and selective NLRP3 antagonist, is described. Replacement of the sulfonyl urea core from the first-generation NLRP3 antagonist CRID3 with a sulfonimidamide core afforded...
2.
Ghosh P, Schmitz M, Pandurangan T, Zeleke S, Chin Chan S, Mosior J, et al.
RSC Chem Biol
. 2024 Oct;
PMID: 39450271
The CDK12 inhibitor SR-4835 promotes the proteasomal degradation of cyclin K, contingent on the presence of CDK12 and the CUL4-RBX1-DDB1 E3 ligase complex. The inhibitor displays molecular glue activity, which...
3.
Schmitz M, Kaltheuner I, Anand K, Duster R, Moecking J, Monastyrskyi A, et al.
J Biol Chem
. 2023 Nov;
300(1):105501.
PMID: 38016516
Inhibition of cyclin-dependent kinases (CDKs) has evolved as an emerging anticancer strategy. In addition to the cell cycle-regulating CDKs, the transcriptional kinases Cdk12 and Cdk13 have become the focus of...
4.
Burger K, Fernandez M, Meads M, Sudalagunta P, Oliveira P, Canevarolo R, et al.
Cancer Res
. 2023 Sep;
83(23):3901-3919.
PMID: 37702657
Significance: CK1δ and CK1ε are attractive therapeutic targets in multiple myeloma whose expression increases with disease progression and connote poor outcomes, and that are necessary to sustain expression of genes...
5.
Choi J, Noguchi Y, Alburger J, Bayle S, Chung E, Grant W, et al.
J Med Chem
. 2023 May;
66(11):7162-7178.
PMID: 37204207
Specific inhibition of a single kinase isoform is a challenging task due to the highly conserved nature of ATP-binding sites. Casein kinase 1 (CK1) δ and ε share 97% sequence...
6.
Fuerst R, Choi J, Knapinska A, Cameron M, Ruiz C, Delmas A, et al.
Bioorg Med Chem Lett
. 2022 Oct;
76:129014.
PMID: 36202189
Starting from an already known MMP-13 inhibitor, 1, we pursued an SAR-approach focusing on optimizing interactions close to the Zn binding site of the enzyme. We found the oxetane containing...
7.
Shahoei R, Pangeni S, Sanders M, Zhang H, Mladenovic-Lucas L, Roush W, et al.
Front Mol Biosci
. 2022 Jul;
9:935375.
PMID: 35836935
Alpha/beta hydrolase domain-containing 5 (ABHD5), also termed CGI-58, is the key upstream activator of adipose triglyceride lipase (ATGL), which plays an essential role in lipid metabolism and energy storage. Mutations...
8.
Hwang D, Nilchan N, Park H, Roy R, Roush W, Rader C
Bioconjug Chem
. 2022 May;
33(6):1192-1200.
PMID: 35584359
Catalytic antibody 38C2 and its humanized version h38C2 harbor a uniquely reactive lysine at the bottom of a 11 Å deep pocket that permits site-specific conjugation of β-diketone-, β-lactam-, and...
9.
Torres S, Brol M, Magdaleno F, Schierwagen R, Uschner F, Klein S, et al.
Front Mol Biosci
. 2021 Sep;
8:715765.
PMID: 34513923
Activation of the inflammasome NLRP3 (NOD-, LRR- and pyrin domain containing 3) contributes to the development of non-alcoholic fatty liver disease (NAFLD) and progression to non-alcoholic steatohepatitis (NASH). Therefore, this...
10.
Nilchan N, Alburger J, Roush W, Rader C
Biochemistry
. 2021 Mar;
60(14):1080-1087.
PMID: 33754696
Monoclonal antibody h38C2 is a humanized catalytic antibody that has been used to generate various immunoconjugate species such as chemically programmed antibodies, antibody-drug conjugates, and antibody-siRNA conjugates. Highly efficient and...