Brock Brown

Targeting of a Bile Acid Receptor, Takeda G Protein Receptor 5 [TGR5], by a Novel First-in-Class Competitive Antagonist, SBI-364, Diminishes Hepatic and Renal Cystogenesis in Polycystic Liver and Kidney Disease

Tatyana V. Masyuk, Anatoliy I. Masyuk, Christy E. Trussoni, Maria Lorenzo-Pisarello et autres

High Resolution Image Download MS PowerPoint Slide Polycystic kidney disease (PKD) and associated polycystic liver disease (PLD) are genetic disorders with limited therapeutic options. In this work, we report SBI-364, a novel first in-class competitive antagonist of a G protein-coupled bile acid …

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Discovery of small molecule positive allosteric modulators of the secretin receptor

Daniela G. Dengler, Kaleeckal G. Harikumar, Sirkku Pollari, Qing Sun et autres

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Development of a Testing Funnel for Identification of Small-Molecule Modulators Targeting Secretin Receptors

Daniela G. Dengler, Qing Sun, John P. Holleran, Sirkku Pollari et autres

The secretin receptor (SCTR), a prototypical class B G protein-coupled receptor (GPCR), exerts its effects mainly by activating Gαs proteins upon binding of its endogenous peptide ligand secretin. SCTRs can be found in a variety of tissues and organs across species, including …

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Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11

Jing Li, Tanya Yakushi, Francesco Parlati, Andrew L. MacKinnon et autres

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Functional Antagonists of EBI-2

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

A robust antibody response is essential for efficient identification and eradication of pathogenic microbes and toxins, whereas dysregulation of the antibody response can lead to autoimmune disease. Specific antigen encounter by B lymphocytes induces clonal expansion that encompasses several distinct stages of …

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Table 5, Summary of in vitro ADME Properties of EBI2 inhibitor probe ML401 (MLS-0472527)

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

Figure 1, EBI2 antagonist GSK682753

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

Figure 5, Potency of ML401 inhibition in EBI2 beta-arrestin and RS11846 cell chemotaxis assays

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

Figure 3, Stability of ML401 in 1×

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

Figure 6, Eurofins Panel for ML401

Robert Ardecky, Eduard Sergienko, Jiwen Zou, Santhi Ganji et autres

Figure 4, Stability of ML340 in PBS at ambient temperature

Robert Ardecky, Gavin Magnuson, Jiwen Zou, Santhi Ganji et autres

Table 6, SAR explorations of ML340

Robert Ardecky, Gavin Magnuson, Jiwen Zou, Santhi Ganji et autres