Discovery of brain-penetrant, irreversible kynurenine aminotransferase II inhibitors for schizophrenia

…, MR Reese, SB Rong, MA Salafia… - ACS medicinal …, 2012 - ACS Publications
Kynurenine aminotransferase (KAT) II has been identified as a potential new target for the
treatment of cognitive impairment associated with schizophrenia and other psychiatric …

PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

…, LA McAllister, J Pandit, SB Rong, MA Salafia… - Bioorganic & medicinal …, 2013 - Elsevier
The structure-based design, synthesis, and biological evaluation of a new pyrazole series of
irreversible KAT II inhibitors are described herein. The modification of the inhibitor scaffold …

Structure-based design of irreversible human KAT II inhibitors: discovery of new potency-enhancing interactions

…, J Pandit, VD Parikh, BJ Rago, MA Salafia… - ACS Medicinal …, 2013 - ACS Publications
A series of aryl hydroxamates recently have been disclosed as irreversible inhibitors of
kynurenine amino transferase II (KAT II), an enzyme that may play a role in schizophrenia and …

PF-03475952: a potent and neutralizing fully human anti-CD44 antibody for therapeutic applications in inflammatory diseases

…, MA Thiede, J Zhang, RB Alpert, MA Salafia… - Advances in …, 2010 - Springer
Introduction CD44 is a cell adhesion molecule believed to play a critical role in T cell and
monocyte infiltration in the inflammatory process. The reduction of CD44 expression or its …

Quantitative translational analysis of brain kynurenic acid modulation via irreversible kynurenine aminotransferase II inhibition

…, C Li, W Horner, LE Zawadzke, MA Salafia… - Molecular …, 2018 - ASPET
Kynurenic acid (KYNA) plays a significant role in maintaining normal brain function, and
abnormalities in KYNA levels have been associated with various central nervous system …

Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics

…, S Ghosh, E Evrard, LE Zawadzke, MA Salafia… - …, 2013 - pubs.rsc.org
A series of kynurenine aminotransferase II (KAT II) inhibitors has been developed replacing
the hydroxamate motif with a bioisostere. Triazolinones or triazoles have proven to be …

[HTML][HTML] Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor

…, D Volfson, J Davoren, E Guilmette, M Salafia… - Nature …, 2018 - nature.com
Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a
therapeutic strategy for neurologic and psychiatric diseases due to the fundamental role of …

Discovery and lead optimization of atropisomer D1 agonists with reduced desensitization

…, CC Orozco, BK Rai, M Salafia… - Journal of Medicinal …, 2018 - ACS Publications
The discovery of D1 subtype-selective agonists with drug-like properties has been an
enduring challenge for the greater part of 40 years. All known D1-selective agonists are …

Dopamine D1 receptor-agonist interactions: A mutagenesis and homology modeling study

S Mente, E Guilmette, M Salafia, D Gray - Bioorganic & medicinal chemistry …, 2015 - Elsevier
The dopamine D1 receptor is a G protein-coupled receptor that regulates intracellular signaling
via agonist activation. Although the number of solved GPCR X-ray structures has been …

Genetic ablation of the src kinase p59fynT exacerbates pulmonary inflammation in an allergic mouse model

EM Kudlacz, CJ Andresen, M Salafia… - American journal of …, 2001 - atsjournals.org
p59fynT is a protein tyrosine kinase in the src family that has been associated with and believed
to function in the signaling of many receptors, including the T-cell receptor. A role for the …