Keap1 binds to the Nrf2 transcription factor to promote its degradation, resulting in the loss of
gene products that protect against oxidative stress. While cell-active small molecules have …

Fumarate-containing pharmaceuticals are potent therapeutic agents that influence multiple
cellular pathways. Despite proven clinical efficacy, there is a significant lack of data that …

Structure−activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123),
a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based …

In neutrophils, growth-related protein-α (CXCL1) and interleukin-8 (CXCL8), are potent
chemoattractants (Cytokine 14:27–36, 2001; Biochemistry 42:2874–2886, 2003) and can …

Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol
(EC144), is a second generation inhibitor of heat …

Retinoic acid receptor‐related orphan nuclear receptor γ ( ROR γ) orchestrates a pro‐inflammatory
gene expression programme in multiple lymphocyte lineages including T helper type …

A novel series of cyclobutenedione centered C(4)-alkyl substituted furanyl analogs was
developed as potent CXCR2 and CXCR1 antagonists. Compound 16 exhibits potent inhibitory …

The nuclear receptor RORγ plays a central role in controlling a pro-inflammatory gene
expression program in several lymphocyte lineages including TH17 cells. RORγ-dependent …

Since the early 2000s, the Aurora kinases have become major targets of oncology drug
discovery particularly Aurora-A and Aurora-B kinases (AKA/AKB) for which the selective …

RORγt is a pivotal regulator of a pro-inflammatory gene expression program implicated in
the pathology of several major human immune-mediated diseases. Evidence from mouse …