[HTML][HTML] BRD4 inhibition for the treatment of pathological organ fibrosis

MS Stratton, SM Haldar, TA McKinsey - F1000Research, 2017 - ncbi.nlm.nih.gov
F1000Research, 2017ncbi.nlm.nih.gov
Fibrosis is defined as excess deposition of extracellular matrix, resulting in tissue scarring
and organ dysfunction. It is estimated that 45% of deaths in the developed world are due to
fibrosis-induced organ failure. Despite the well-accepted role of fibrosis in the pathogenesis
of numerous diseases, there are only two US Food and Drug Administration–approved anti-
fibrotic therapies, both of which are currently restricted to the treatment of pulmonary fibrosis.
Thus, organ fibrosis represents a massive unmet medical need. Here, we review recent …
Abstract
Fibrosis is defined as excess deposition of extracellular matrix, resulting in tissue scarring and organ dysfunction. It is estimated that 45% of deaths in the developed world are due to fibrosis-induced organ failure. Despite the well-accepted role of fibrosis in the pathogenesis of numerous diseases, there are only two US Food and Drug Administration–approved anti-fibrotic therapies, both of which are currently restricted to the treatment of pulmonary fibrosis. Thus, organ fibrosis represents a massive unmet medical need. Here, we review recent findings suggesting that an epigenetic regulatory protein, BRD4, is a nodal effector of organ fibrosis, and we highlight the potential of small-molecule BRD4 inhibitors for the treatment of diverse fibrotic diseases.
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