Blaise Lippa

Challenges of an active metabolite: The potential of disproportionate human exposure and the complex kinetics upon drug-drug interactions

Inese Smukste, Austin Sun, James J. Dowling, Andrew Mcteague et autres

Model-based exploration of parent-metabolite kinetics of MT-202: Nonclinical characterization and feasibility of clinical metabolite exposure prediction

Austin Sun, Inese Smukste, James J. Dowling, T. Andrew McTeague et autres

SAT-095 Selective targeting of integrin avβ8 effectively suppresses tumor growth in the new PSC-associated cholangiocarcinoma model (SB CCA.Mdr2-/- mouse)

Pinzhu Huang, Wen Xiu Gao, Heansika Matta, Zaur Abilov et autres

Exploring Integrin α5β1 as a Potential Therapeutic Target for Pulmonary Arterial Hypertension: Insights From Comprehensive Multicenter Preclinical Studies

Sarah-Eve S Lemay, Mónica S. Montesinos, Yann Grobs, Tetsuro Yokokawa et autres

BACKGROUND: Pulmonary arterial hypertension (PAH) is characterized by obliterative vascular remodeling of the small pulmonary arteries (PAs) and progressive increase in pulmonary vascular resistance leading to right ventricular failure. Although several drugs are approved for the treatment of PAH, mortality rates remain …

jp, ca (code pays fourni par la source)

Abstract 4139465: Integrin α5β1 represents a novel therapeutic target to improve vascular remodeling in pulmonary arterial hypertension

Sarah-Eve S Lemay, Mónica S. Montesinos, Yann Grobs, Tetsuro Yokokawa et autres

Introduction: Pulmonary arterial hypertension (PAH) is characterized by progressive obstruction and decreased compliance of pulmonary arteries (PA), leading to right ventricular failure and premature death. Sustained proliferation and resistance to apoptosis of PAs smooth muscle and endothelial cells (PASMCs, PAECs) and accumulation …

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Abstract 4139456: Integrin α5β1 contributes to pathological remodeling of the right ventricle in pulmonary arterial hypertension

Sarah-Eve S Lemay, Mónica S. Montesinos, Yann Grobs, Alice Bourgeois et autres

Introduction: Right ventricular (RV) function is an important prognosis factor in pulmonary arterial hypertension (PAH). In response to pressure overload, the RV undergoes morphological changes driven by the accumulation of extracellular matrix (ECM) elements and cardiomyocyte hypertrophy. Integrins (Itg) are members of …

ca (code pays fourni par la source)

Abstract 4139371: Treatment of pulmonary arterial hypertension by blocking integrin a5b1, a potential disease-modifying strategy

Mónica S. Montesinos, Sarah-Eve S Lemay, Hailey Rapisardi, Minh‐Hai Nguyen et autres

Introduction: Pulmonary arterial hypertension (PAH) is marked by pathological remodeling of distal arteries, driven by hyperplasia of pulmonary arterial smooth muscle cells (PASMCs), dysfunction of pulmonary arterial endothelial cells (PAECs), and increased deposition of the extracellular matrix (ECM). Hypothesis: Considering the crucial …

ca (code pays fourni par la source)

The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis

Bryce A. Harrison, James J. Dowling, Matthew G. Bursavich, Dawn M. Troast et autres

Inhibition of integrin αvβ6 is a promising approach to the treatment of fibrotic disease such as idiopathic pulmonary fibrosis. Screening a small library combining head groups that stabilize the bent-closed conformation of integrin αIIbβ3 with αv integrin binding motifs resulted in the …

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Identification of integrin a5b1 inhibition as a potentially disease-modifying approach for the treatment of pulmonary arterial hypertension

Mónica S. Montesinos, Sarah-Eve S Lemay, Parmita Saxena, Hailey Rapisardi et autres

Pulmonary arterial hypertension (PAH) is characterized by pathogenic remodeling of the distal arteries arising from pulmonary arterial smooth muscle cell (PASMC) hyperplasia, pulmonary arterial endothelial cell (PAEC) dysfunction, and increased deposition of extracellular matrix (ECM). Given the central role of the ECM …

ca (code pays fourni par la source)

Implication of Integrin α5β1 in right ventricular failure associated with pulmonary arterial hypertension

Sarah-Eve S Lemay, Mónica S. Montesinos, Yann Grobs, Charlie Théberge et autres

Right ventricular (RV) function is an important prognosis factor in pulmonary arterial hypertension (PAH). In response to pressure overload, the RV undergoes morphological changes driven by the accumulation of extracellular matrix (ECM) elements and cardiomyocyte hypertrophy. Integrins (ITG) are members of the …

Exploring Integrin α5β1 as a Potential Therapeutic Target for Pulmonary Arterial Hypertension: Insights from Comprehensive Multicenter Preclinical Studies

Sarah-Eve S Lemay, Mónica S. Montesinos, Yann Grobs, Tetsuro Yokokawa et autres

Pulmonary arterial hypertension (PAH) is characterized by obliterative vascular remodeling of the small pulmonary arteries (PA) and progressive increase in pulmonary vascular resistance (PVR) leading to right ventricular (RV) failure. Although several drugs are approved for the treatment of PAH, mortality remains …

us (code pays fourni par la source)

Sa1761 PREDICTIVE TRANSLATIONAL BLOOD BIOMARKER DYNAMICS OF SMALL MOLECULE α4β7 INHIBITION IN NONHUMAN PRIMATE

Jamie Wong, Dooyoung Lee, Huidong Chen, Maloy Mangada et autres