Researchers from Bristol Myers Squibb Co. disclosed the structure and presented preclinical data for the dual inhibitor of diacylglycerol kinases (DGK) α and ζ, BMS-986408. Optimization of a DGK-α-selective hit led to the synthesis of dual DGK-α and -ζ inhibitors.
George Medicines Ltd. has published positive data from two phase III studies showing GMRx2, a low-dose triple-drug combination treatment for hypertension, is superior to dual combinations of its components.
Aging is part of the life cycle and, although the effects are not manifest until after adulthood, it actually occurs from birth. The concept of senescence has traditionally been associated with aging. However, an embryo has senescent cells. In that case, what is aging, how can it be measured, and from what point in the life cycle?
Aging is part of the life cycle and, although the effects are not manifest until after adulthood, it actually occurs from birth. The concept of senescence has traditionally been associated with aging. However, an embryo has senescent cells. In that case, what is aging, how can it be measured, and from what point in the life cycle?
Genetic or pharmacologic inhibition of casein kinase 1α (CK1α) has proven effective in suppressing the proliferation of acute myeloid leukemia (AML) cell lines with wild-type TP53. Researchers from Bristol Myers Squibb Co. recently presented the discovery and preclinical characterization of BMS-986397, a cereblon E3 ligase modulatory drug (CELMoD) designed as a molecular glue degrader of CK1α.
The valosin-containing protein (VCP) modulator KUS-121 from Kyoto University is in phase II development as an intravitreal treatment for nonarteritic central retinal artery occlusion, but its efficacy in atherosclerosis is unknown.
Repolarization abbreviation with the antiarrhythmic drug mexiletine has been found to normalize the QTc interval and reduce the rate of events in long QT syndrome type 3 (LQT3), but it is only partially efficacious in other malignant forms, including LQT2 and LQT8. There are compounds that have not been tested, such as hERG channel agonists, which are capable of shortening repolarization. The potent hERG agonist ICA-105574 was thus tested in a clinically relevant porcine model of LQT8.
At the recent European Society of Cardiology meeting, Anacardio AB and Helsinn Healthcare SA presented data on their oral small-molecule ghrelin receptor agonist and first-in-class calcium sensitizing inotrope, AC-01, in preclinical models of heart failure.
Keros Therapeutics Inc. has presented preclinical data on the activin receptor type IIB ligand trap RKER-012 (a research version of KER-012 [cibotercept]) in a preclinical pulmonary arterial hypertension model.
Plexium Inc. has described the efforts that led to the discovery of PLX-4545, an orally bioavailable molecular glue degrader of IKZF2 for the treatment of cancer that is currently undergoing evaluation in a phase I study in healthy volunteers.
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