Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor
C Rojas, M Stathis, AG Thomas… - Anesthesia & …, 2008 - journals.lww.com
BACKGROUND: Palonosetron is a 5-HT 3-receptor antagonist (5-HT 3-RA) that has been
shown to be superior to other 5-HT 3-RAs in phase III clinical trials for the prevention of
acute, delayed, and overall chemotherapy-induced nausea and vomiting. The improved …
shown to be superior to other 5-HT 3-RAs in phase III clinical trials for the prevention of
acute, delayed, and overall chemotherapy-induced nausea and vomiting. The improved …
Palonosetron triggers 5-HT3 receptor internalization and causes prolonged inhibition of receptor function
C Rojas, AG Thomas, J Alt, M Stathis, J Zhang… - European journal of …, 2010 - Elsevier
Palonosetron is a 5-HT 3 receptor antagonist that has demonstrated superiority in
preventing both acute and delayed emesis when compared to older first generation 5-HT 3
receptor antagonists. The objective of this work was to determine if palonosetron exhibits …
preventing both acute and delayed emesis when compared to older first generation 5-HT 3
receptor antagonists. The objective of this work was to determine if palonosetron exhibits …
Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1, 2, 4-thiadiazol-2-yl) ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors
K Shukla, DV Ferraris, AG Thomas… - Journal of medicinal …, 2012 - ACS Publications
Bis-2-(5-phenylacetamido-1, 2, 4-thiadiazol-2-yl) ethyl sulfide (BPTES) is a potent and
selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular
probe to determine the therapeutic potential of GLS inhibition. In an attempt to identify more …
selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular
probe to determine the therapeutic potential of GLS inhibition. In an attempt to identify more …
The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo
C Rojas, Y Li, J Zhang, M Stathis, J Alt… - Journal of pharmacology …, 2010 - ASPET
Palonosetron is the only 5-HT 3 receptor antagonist approved for the treatment of delayed
chemotherapy-induced nausea and vomiting (CINV) in moderately emetogenic
chemotherapy. Accumulating evidence suggests that substance P (SP), the endogenous …
chemotherapy-induced nausea and vomiting (CINV) in moderately emetogenic
chemotherapy. Accumulating evidence suggests that substance P (SP), the endogenous …
Synthesis and biological evaluation of low molecular weight fluorescent imaging agents for the prostate-specific membrane antigen
Y Chen, M Pullambhatla, SR Banerjee… - Bioconjugate …, 2012 - ACS Publications
Targeted near-infrared (NIR) optical imaging can be used in vivo to detect specific tissues,
including malignant cells. A series of NIR fluorescent ligands targeting the prostate-specific
membrane antigen (PSMA) was synthesized and each compound was tested for its ability to …
including malignant cells. A series of NIR fluorescent ligands targeting the prostate-specific
membrane antigen (PSMA) was synthesized and each compound was tested for its ability to …
Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects
M Stathis, C Pietra, C Rojas, BS Slusher - European journal of …, 2012 - Elsevier
Netupitant is a potent and selective NK 1 receptor antagonist under development in
combination with a fixed dose of palonosetron for the prevention of chemotherapy induced
nausea and vomiting. Palonosetron is a 5-HT 3 receptor antagonist approved for both the …
combination with a fixed dose of palonosetron for the prevention of chemotherapy induced
nausea and vomiting. Palonosetron is a 5-HT 3 receptor antagonist approved for both the …
Regional brain distribution of translocator protein using [11C]DPA-713 PET in individuals infected with HIV
Imaging the brain distribution of translocator protein (TSPO), a putative biomarker for glial
cell activation and neuroinflammation, may inform management of individuals infected with
HIV by uncovering regional abnormalities related to neurocognitive deficits and enable non …
cell activation and neuroinflammation, may inform management of individuals infected with
HIV by uncovering regional abnormalities related to neurocognitive deficits and enable non …
[HTML][HTML] Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties
M Figuera-Losada, M Stathis, JM Dorskind… - PloS one, 2015 - journals.plos.org
Ceramide is a bioactive lipid that plays an important role in stress responses leading to
apoptosis, cell growth arrest and differentiation. Ceramide production is due in part to
sphingomyelin hydrolysis by sphingomyelinases. In brain, neutral sphingomyelinase 2 …
apoptosis, cell growth arrest and differentiation. Ceramide production is due in part to
sphingomyelin hydrolysis by sphingomyelinases. In brain, neutral sphingomyelinase 2 …
Inhibition of glutamate carboxypeptidase II (GCPII) activity as a treatment for cognitive impairment in multiple sclerosis
KA Rahn, CC Watkins, J Alt, R Rais… - Proceedings of the …, 2012 - National Acad Sciences
Half of all patients with multiple sclerosis (MS) experience cognitive impairment, for which
there is no pharmacological treatment. Using magnetic resonance spectroscopy (MRS), we
examined metabolic changes in the hippocampi of MS patients, compared the findings to …
there is no pharmacological treatment. Using magnetic resonance spectroscopy (MRS), we
examined metabolic changes in the hippocampi of MS patients, compared the findings to …
Allosteric glutaminase inhibitors based on a 1, 4-di (5-amino-1, 3, 4-thiadiazol-2-yl) butane scaffold
SC Zimmermann, EF Wolf, A Luu… - ACS medicinal …, 2016 - ACS Publications
A series of allosteric kidney-type glutaminase (GLS) inhibitors were designed and
synthesized using 1, 4-di (5-amino-1, 3, 4-thiadiazol-2-yl) butane as a core scaffold. A
variety of modified phenylacetyl groups were incorporated into the 5-amino group of the two …
synthesized using 1, 4-di (5-amino-1, 3, 4-thiadiazol-2-yl) butane as a core scaffold. A
variety of modified phenylacetyl groups were incorporated into the 5-amino group of the two …