Identification of Novel 2-((1-(Benzyl(2-hydroxy-2-phenylethyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamoyl)benzoic Acid Analogues as BMP-2 Stimulators

Balaramnavar, Vishal M.; Khan, Imran A.; Siddiqui, Jawed A.; Khan, Mohd Parvez; Chakravarti, Bandana; Sharan, Kunal; Swarnkar, Gaurav; Rastogi, Namrata; Siddiqui, Hefazat Hussain; Chattopadhyay, Naibedya; Saxena, Anil Kumar

doi:10.1021/jm300985d

Cited by 16 publications

(17 citation statements)

References 55 publications

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“…On the other hand, small molecule BMP agonists may overcome these limitations. Through a highthroughput screening, a stimulator of BMP signaling has been discovered, while its mode of action has not been elucidated (Balaramnavar et al 2012). Like BMP agonists, small molecule inhibitors specific for BMP signaling have been developed (Yu et al 2008a;Hong and Yu 2009;Boergermann et al 2010;Mohedas et al 2013;Sanvitale et al 2013;Tsugawa et al 2014).…”

Section: Discussionmentioning

confidence: 99%

Bone Morphogenetic Proteins

Katagiri¹,

Watabe²

2016

Cold Spring Harb Perspect Biol

389

355

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Bone morphogenetic proteins (BMPs), originally identified as osteoinductive components in extracts derived from bone, are now known to play important roles in a wide array of processes during formation and maintenance of various organs including bone, cartilage, muscle, kidney, and blood vessels. BMPs and the related "growth and differentiation factors" (GDFs) are members of the transforming growth factor b (TGF-b) family, and transduce their signals through type I and type II serine -threonine kinase receptors and their intracellular downstream effectors, including Smad proteins. Furthermore, BMP signals are finely tuned by various agonists and antagonists. Because deregulation of the BMP activity at multiple steps in signal transduction is linked to a wide variety of human diseases, therapeutic use of activators and inhibitors of BMP signaling will provide potential avenues for the treatment of the human disorders that are caused by hypo-and hyperactivation of BMP signals, respectively.

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Section: Discussionmentioning

confidence: 99%

Bone Morphogenetic Proteins

Katagiri¹,

Watabe²

2016

Cold Spring Harb Perspect Biol

389

355

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“…Using an organic synthesis method, the novel chemical compound 11, 2-((1-(benzyl(2-hydroxy-2-phenylethyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamoyl)benzoic acid, reportedly induced osteoblast differentiation in rat calvarial osteoblasts, and this effect was blocked by the BMP inhibitor noggin. The new compound also caused dose-dependent increases in nascent bone formation at the fracture site in rats (28). …”

Section: Small Molecule Mediated Bone Formationmentioning

confidence: 99%

Small-molecule based musculoskeletal regenerative engineering

Jiang

Gagnon

et al. 2014

Trends in Biotechnology

110

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Clinicians and scientists working in the field of regenerative engineering are actively investigating a wide range of methods to promote musculoskeletal tissue regeneration. Small molecule-mediated tissue regeneration is emerging as a promising strategy for regenerating various musculoskeletal tissues and a large number of small molecule compounds have been recently discovered as potential bioactive molecules for musculoskeletal tissue repair and regeneration. In this review, we summarize the recent literature encompassing the past four years in the area of small bioactive molecule for promoting repair and regeneration of various musculoskeletal tissues including bone, muscle, cartilage, tendon, and nerve.

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“…Forty adult female Sprague−Dawley (SD) rats (200 ± 20 g each) were taken for the study. Drill‐hole injury was performed in femur as described before . The front skin of the mid‐femur in rats was incised longitudinally in a straight manner at 1 cm in length under anaesthesia with ketamine and xylazine.…”

Section: Methodsmentioning

confidence: 99%