Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective …
…, MD Rosen, HM Peltier, K Sepassi, MC Rizzolio… - Molecular …, 2011 - ASPET
The hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes represent novel targets
for the treatment of anemia, ulcerative colitis, and ischemic and metabolic disease inter alia…
for the treatment of anemia, ulcerative colitis, and ischemic and metabolic disease inter alia…
Design of selective and soluble inhibitors of tumor necrosis factor-α converting enzyme (TACE)
…, ML Moss, DL Musso, MC Rizzolio - Journal of Medicinal …, 2001 - ACS Publications
A program to improve upon the in vitro, in vivo, and physicochemical properties of N-hydroxyformamide
TACE inhibitor GW 3333 (1) is described. Using the primary structure of pro-TNF-…
TACE inhibitor GW 3333 (1) is described. Using the primary structure of pro-TNF-…
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists
…, M Pippel, C Woods, MC Rizzolio… - Journal of medicinal …, 2006 - ACS Publications
A high throughput screening approach to the identification of selective cholecystokinin-2
receptor (CCK-2R) ligands resulted in the discovery of a novel series of antagonists, …
receptor (CCK-2R) ligands resulted in the discovery of a novel series of antagonists, …
Discovery of a gut-restricted JAK inhibitor for the treatment of inflammatory bowel disease
…, TS Rao, JP Edwards, MC Rizzolio… - Journal of Medicinal …, 2020 - ACS Publications
To identify Janus kinase (JAK) inhibitors that selectively target gastrointestinal tissues with
limited systemic exposures, a class of imidazopyrrolopyridines with a range of physical …
limited systemic exposures, a class of imidazopyrrolopyridines with a range of physical …
Characterization of a robust enzymatic assay for inhibitors of 2-oxoglutarate-dependent hydroxylases
…, J Wu, W Yan, MD Rosen, MC Rizzolio… - Journal of …, 2009 - journals.sagepub.com
The prolyl-4-hydroxylase proteins regulate the hypoxia-inducible transcription factors (HIFs)
by hydroxylation of proline residues targeting HIF-1α for proteasomal degradation. Using the …
by hydroxylation of proline residues targeting HIF-1α for proteasomal degradation. Using the …
N-Hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1′ isobutyl substitution
…, ML Moss, MH Rabinowitz, MC Rizzolio… - Bioorganic & medicinal …, 2001 - Elsevier
N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which
have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting …
have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting …
JNJ-26070109 [(R) 4-bromo-N-[1-(2, 4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor …
…, TD Barrett, J Freedman, L Li, MC Rizzolio… - … of Pharmacology and …, 2011 - ASPET
… The supernatant was recentrifuged (26,892g for 25 min at 4C), and the final pellet was
resuspended in assay buffer. Protein concentration was determined using the BCA Protein Assay …
resuspended in assay buffer. Protein concentration was determined using the BCA Protein Assay …
[PDF][PDF] cholecystokinin 2 receptor antagonist with good oral bioavailability.
MF Morton, TD Barrett, J Freedman, L Li, MC Rizzolio… - 2011 - academia.edu
Gastrin, acting through the CCK2 receptors, regulates a number of biological functions
including gastric acid secretion, anxiety, satiety and growth of the gastrointestinal mucosa (see …
including gastric acid secretion, anxiety, satiety and growth of the gastrointestinal mucosa (see …
[HTML][HTML] Copper nitroprusside: An innovative approach for targeted cancer therapy via ROS modulation
…, M Cemazar, V Canzonieri, F Rizzolio… - Biomedicine & …, 2024 - Elsevier
… Thermal cycling reaction conditions included an initial denaturation at 95C for 10 min,
followed by 45 cycles of denaturation at 95C for 15 s and annealing at 60 C performed by …
followed by 45 cycles of denaturation at 95C for 15 s and annealing at 60 C performed by …
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl) amide, a high affinity TRPV1 (VR1 …
…, B Lord, L Gonzales, K Hoey, M Rizzolio… - Journal of medicinal …, 2005 - ACS Publications
High throughput screening using the recombinant human TRPV1 receptor was used to identify
a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration …
a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration …