Justin Meyerowitz
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View article: The Bi-steric, mTORC1-Selective Inhibitor, RMC-5552, in Advanced Solid Tumors: A Phase 1 Trial
The Bi-steric, mTORC1-Selective Inhibitor, RMC-5552, in Advanced Solid Tumors: A Phase 1 Trial Open
Purpose: PI3K/mTOR pathway activation drives oncogenesis and progression of many cancers. RMC-5552 is a bi-steric, mTOR complex 1 (mTORC1)-selective inhibitor that potently inhibits phosphorylation of key mTORC1 substrates eukaryotic initi…
View article: Small vs. Large Library Docking for Positive Allosteric Modulators of the Calcium Sensing Receptor
Small vs. Large Library Docking for Positive Allosteric Modulators of the Calcium Sensing Receptor Open
Drugs acting as positive allosteric modulators (PAMs) to enhance the activation of the calcium sensing receptor (CaSR) and to suppress parathyroid hormone (PTH) secretion can treat hyperparathyroidism but suffer from side effects including…
View article: Longitudinal clinical phenotyping of post COVID condition in Mexican adults recovering from severe COVID-19: a prospective cohort study
Longitudinal clinical phenotyping of post COVID condition in Mexican adults recovering from severe COVID-19: a prospective cohort study Open
Introduction Few studies have evaluated the presence of Post COVID-19 conditions (PCC) in people from Latin America, a region that has been heavily afflicted by the COVID-19 pandemic. In this study, we describe the frequency, co-occurrence…
View article: Supplemental Figure 2 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 2 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
In vitro response to co-inhibition of MAPK and mTOR pathways in BRAFV600E mutated AM-38 glioma cells.
View article: Supplemental Figure 2 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 2 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
In vitro response to co-inhibition of MAPK and mTOR pathways in BRAFV600E mutated AM-38 glioma cells.
View article: Supplemental Figure 3 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 3 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Combinatorial index and median-effect plots for BRAFWT cell lines.
View article: Data from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Data from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Purpose: Alteration of the BRAF/MEK/MAPK pathway is the hallmark of pediatric low-grade gliomas (PLGGs), and mTOR activation has been documented in the majority of these tumors. We investigated combinations of MEK1/2, BRAFV600E and mTOR in…
View article: Supplemental Table 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Table 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
In vitro cell line IC50 values and mutational status.
View article: Supplemental Figure 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Combinatorial index and median-effect plots for BRAFV600E mutated cell lines.
View article: Data from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Data from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Purpose: Alteration of the BRAF/MEK/MAPK pathway is the hallmark of pediatric low-grade gliomas (PLGGs), and mTOR activation has been documented in the majority of these tumors. We investigated combinations of MEK1/2, BRAFV600E and mTOR in…
View article: Supplemental Figure 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Combinatorial index and median-effect plots for BRAFV600E mutated cell lines.
View article: Supplemental Table 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Table 1 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
In vitro cell line IC50 values and mutational status.
View article: Supplemental Figure 3 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas
Supplemental Figure 3 from BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas Open
Combinatorial index and median-effect plots for BRAFWT cell lines.
View article: Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors Open
Hyperactivation of mTOR kinase by mutations in the PI3K/mTOR pathway or by crosstalk with other mutant cancer drivers, such as RAS, is a feature of many tumors. Multiple allosteric inhibitors of mTORC1 and orthosteric dual inhibitors of mT…
View article: Impact of Magnesium on Oxytocin Receptor Function
Impact of Magnesium on Oxytocin Receptor Function Open
Background and Purpose: The intranasal administration of oxytocin (OT) reduces migraine headaches through activation of the oxytocin receptor (OTR). Magnesium ion (Mg2+) concentration is critical to the activation of the OTR, and a low ser…
View article: Impact of magnesium on oxytocin receptor function
Impact of magnesium on oxytocin receptor function Open
Background and Purpose: The intranasal administration of oxytocin (OT) reduces migraine headaches through activation of the oxytocin receptor (OTR). Magnesium ion (Mg2+) concentration is critical to activation of OTR, and low serum Mg2+ co…
View article: Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists
Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists Open
The μ‐opioid receptor (μOR) is the major target for opioid analgesics. Activation of μOR initiates signaling through G protein pathways as well as through β‐arrestin recruitment. μOR agonists that are biased towards G protein signaling pat…
View article: Structure-based Evolution of G protein-biased μ-opioid Receptor Agonists
Structure-based Evolution of G protein-biased μ-opioid Receptor Agonists Open
The μ-opioid receptor (μOR) is the major target for opioid analgesics. Activation of μOR initiates signaling through G protein pathways as well as through β-arrestin recruitment. μOR agonists that are biased towards G protein signaling pat…
View article: Plasticity in Ligand Recognition at Somatostatin Receptors
Plasticity in Ligand Recognition at Somatostatin Receptors Open
Somatostatin is a signaling peptide that plays a pivotal and wide-ranging role in physiologic processes relating to metabolism and growth through its actions at somatostatin receptors (SSTRs). Members of the somatostatin receptor subfamily…
View article: Structure Determination of Inactive-State GPCRs with a Universal Nanobody
Structure Determination of Inactive-State GPCRs with a Universal Nanobody Open
Summary Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug discovery by allowing for routine determination of membrane protein structures previously intractable. However, despite representing one of the l…