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Targeting the ANGPT–TIE2 pathway in malignancy
This Review presents an encompassing picture of what the authors know about this important axis in tumour biology and the various options for therapeutic intervention to identify the best path forwards. Expand
Chemical generation of bispecific antibodies
A bispecific antibody is developed that binds both vascular endothelial growth factor and angiopoietin-2 simultaneously, inhibits their function, shows efficacy in tumor xenograft studies, and greatly augments the antitumor effects of standard chemotherapy. Expand
Failure of atriopeptin II to cause arterial vasodilation in the conscious rat.
Data suggest that atriopeptin II infusion markedly attenuated cardiac output in the conscious spontaneously hypertensive rats, and total and regional vascular resistances were increased, possibly through reflex compensatory mechanisms, to maintain arterial pressure in the face of decreased cardiac output. Expand
Demonstration of vasorelaxant activity with an A1-selective adenosine agonist in porcine coronary artery: involvement of potassium channels.
The vasodilator activity of adenosine has been associated with selective stimulation of A2 receptors and no elevation in cyclic GMP levels could be observed in tissues stimulated with CPA or DPMA, indicating the A1-selective nature of this agonist. Expand
Specifically Targeting Angiopoietin-2 Inhibits Angiogenesis, Tie2-Expressing Monocyte Infiltration, and Tumor Growth
CovX-Bodies provide an elegant solution to overcome the pharmacokinetic–pharmacodynamic problems of peptides and will be useful as single agents and in combination with standard-of-care agents. Expand
Development of a Novel Long-Acting Antidiabetic FGF21 Mimetic by Targeted Conjugation to a Scaffold Antibody
CVX-343, created by linkage of the CovX scaffold antibody to the engineered residue A129C of FGF21 protein, demonstrated superior preclinical pharmacodynamics by extending serum half-life of F GF21 while preserving full therapeutic functionality. Expand
Prevention and reversal of cerebral vasospasm by an endothelin-converting enzyme inhibitor, CGS 26303, in an experimental model of subarachnoid hemorrhage.
The findings demonstrate that inhibiting the conversion of Big ET-1 to ET- 1 via intravenous administration of an ECE inhibitor can be an effective strategy for limiting angiographic vasospasm after SAH and provides further support for the role of ET in the establishment of cerebral vasospasms. Expand
Novel and potent BK channel openers: CGS 7181 and its analogs
This article discloses the identification of a novel series of the opener of the large‐conductance Ca2+‐activated K+ (BK) channel, CGS 7181, and its analogs, CGS 7184, CGS 7590, and CGS 7725. TheExpand
Systemic administration of an inhibitor of endothelin-converting enzyme for attenuation of cerebral vasospasm following experimental subarachnoid hemorrhage.
This study provides the first evidence that systemic administration of an inhibitor of ECE is capable of preventing cerebral vasospasm after SAH and indicates that blocking the conversion of Big ET-1 to its activeET-1 form using CGS 26303 may represent a feasible strategy for ameliorating cerebral vasOSPasm. Expand
Selective Adenosine-2 Agonist Produces Both Direct and Reflex Tachycardia in Normotensive Rats
The data indicate that anesthesia potentiates the depressor actions of DPMA and stimulation of A2 receptors increases HR through both direct and indirect mechanisms of action. Expand