scholarly journals Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway

2019 ◽  
Vol 14 (7) ◽  
pp. 1673-1673
Author(s):  
Jamie R. Genthe ◽  
Jaeki Min ◽  
Dana M. Farmer ◽  
Anang A. Shelat ◽  
Jose A. Grenet ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Small Molecule ◽  
Bmp Signaling ◽  
New Class

scholarly journals Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway

2017 ◽  
Vol 12 (9) ◽  
pp. 2436-2447 ◽  
Author(s):  
Jamie R. Genthe ◽  
Jaeki Min ◽  
Dana M. Farmer ◽  
Anang A. Shelat ◽  
Jose A. Grenet ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Small Molecule ◽  
Bmp Signaling ◽  
New Class

scholarly journals A New Class of Small Molecule Inhibitor of BMP Signaling

PLoS ONE ◽  
2013 ◽  
Vol 8 (4) ◽  
pp. e62721 ◽  
Author(s):  
Caroline E. Sanvitale ◽  
Georgina Kerr ◽  
Apirat Chaikuad ◽  
Marie-Christine Ramel ◽  
Agustin H. Mohedas ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Bmp Signaling ◽  
New Class ◽  
Molecule Inhibitor

Small-Molecule Antagonists of CCR5 and CXCR4: A Promising New Class of Anti-HIV-1 Drugs

2004 ◽  
Vol 10 (17) ◽  
pp. 2041-2062 ◽  
Author(s):  
Christoph Seibert ◽  
Thomas Sakmar
Keyword(s):  
Small Molecule ◽  
New Class ◽  
Anti Hiv ◽  
Hiv 1

Recent Development of Small Molecule Glutaminase Inhibitors

2018 ◽  
Vol 18 (6) ◽  
pp. 432-443 ◽  
Author(s):  
Minsoo Song ◽  
Soong-Hyun Kim ◽  
Chun Young Im ◽  
Hee-Jong Hwang
Keyword(s):  
Small Molecule ◽  
Cell Metabolism ◽  
Phase 1 ◽  
Vital Role ◽  
Glutamine Metabolism ◽  
Inhibition Mechanism ◽  
Tumor Cell Growth ◽  
X Ray ◽  
New Class ◽  
Preclinical And Clinical Studies

Glutaminase (GLS), which is responsible for the conversion of glutamine to glutamate, plays a vital role in up-regulating cell metabolism for tumor cell growth and is considered to be a valuable therapeutic target for cancer treatment. Based on this important function of glutaminase in cancer, several GLS inhibitors have been developed in both academia and industry. Most importantly, Calithera Biosciences Inc. is actively developing the glutaminase inhibitor CB-839 for the treatment of various cancers, and it is currently being evaluated in phase 1 and 2 clinical trials. In this review, recent efforts to develop small molecule glutaminase inhibitors that target glutamine metabolism in both preclinical and clinical studies are discussed. In particular, more emphasis is placed on CB-839 because it is the only small molecule GLS inhibitor being studied in a clinical setting. The inhibition mechanism is also discussed based on X-ray structure studies of thiadiazole derivatives present in glutaminase inhibitor BPTES. Finally, recent medicinal chemistry efforts to develop a new class of GLS inhibitors are described in the hopes of providing useful information for the next generation of GLS inhibitors.

DDR1 and DDR2: a review on signaling pathway and small molecule inhibitors as an anticancer agent

2021 ◽  
Vol 30 (3) ◽  
pp. 535-551
Author(s):  
Gurubasavaraja Swamy Purawarga Matada ◽  
Arka Das ◽  
Prasad Sanjay Dhiwar ◽  
Abhishek Ghara
Keyword(s):  
Signaling Pathway ◽  
Small Molecule ◽  
Anticancer Agent ◽  
Small Molecule Inhibitors

scholarly journals Small Molecule Antagonists of the Wnt/Beta-Catenin Signaling Pathway Target Breast Tumor-Initiating Cells in a Her2/Neu Mouse Model of Breast Cancer

PLoS ONE ◽  
2012 ◽  
Vol 7 (3) ◽  
pp. e33976 ◽  
Author(s):  
Robin M. Hallett ◽  
Maria K. Kondratyev ◽  
Andrew O. Giacomelli ◽  
Allison M. L. Nixon ◽  
Adele Girgis-Gabardo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Mouse Model ◽  
Signaling Pathway ◽  
Small Molecule ◽  
Breast Tumor ◽  
Beta Catenin ◽  
Tumor Initiating Cells

Abstract 17802: Ips Cells -derived Cardiac Progenitors Induce Dramatic Cardiac Regeneration and Improve Function by Cxcr4 Signaling Pathway in Infarcted Myocardium

Circulation ◽  
2014 ◽  
Vol 130 (suppl_2) ◽  
Author(s):  
Zeshan Pasha ◽  
Romana Saeed ◽  
Muhammad Ashraf
Keyword(s):  
Stem Cells ◽  
Signaling Pathway ◽  
Small Molecule ◽  
In Vivo Studies ◽  
Immunofluorescent Staining ◽  
Concomitant Treatment ◽  
Post Transplantation ◽  
Cardiac Progenitors ◽  
Cxcr4 Signaling ◽  
Infarcted Myocardium

Background: The participation of endogenous cardiac stem/progenitor cells is limited in restoring cardiac structure and function in the ischemic myocardium which is further aggravated by poor survival and propagation of transplanted stem cells of different origin in the infarcted heart. The goal of this study was to explore the survival and engraftability of newly discovered induced pluripotent stem cells (IPS) in the myocardium following infarction (MI). Methods and Results: Integration free iPS were generated from myoblasts and characterized. Cardiac progenitors (CPs) were created by treatment with a small molecule. CPs proliferation was assessed by BrdU labeling; Differentiation by both RT-PCR and immunofluorescent staining for cardiac markers Nkx2.5, actinin, and -MHC. Gene expression profiling was performed using Affymetrix array. In vivo studies were carried out by injecting CPs or nontreated IPS (3x105), into mouse model of permanent LAD. Echocardiography, histological parameters, TUNEL assay and capillary vessel density were measured 6 weeks post transplantation. Treatment of IPS with a small molecule upregulated Nkx2.5 and maintained up to 4 weeks (p<0.01 vs nontreated IPS). Expression of actinin and -MHC was also detectable at 3 weeks. Increased proliferative activity (p<0.01) evaluated by cell proliferation and Brdu assay was observed. Significant CPs survival and reduced apoptosis were noticed in the small molecule treated iPSC compared to nontreated and/or saline group. Enhanced ejection fraction and fractional shortening (p< 0.05) was observed 6 weeks post transplantation. Interestingly there was 2-3 fold upregulation of chemokines including CCL7, CXCR2, CXCR5. miR Microarray analysis showed upregulation of cardiac specific mir-133,762. Western blot analysis showed increased phospho-Akt levels as compared to nontreated IPSC (p<0.01). Survival and differentiation properties of CPs were abolished by concomitant treatment of IPS with CXR4 blocker (p<0.05). Conclusion: This study provides a novel strategy for generating CPs and their enhanced survival, engraftment and differentiation with the treatment of cardiogenic small molecule post transplantation in the infarcted myocardium through CXCR4 signaling pathway.

Effect of Tumor Growth Factor-β on Osteogenesis in Osteoporosis Rats by Regulating Bone Morphogenetic Protein Signaling Pathway

2020 ◽  
Vol 10 (12) ◽  
pp. 1884-1890
Author(s):  
Jing Tian ◽  
Qianying Zhao ◽  
Dapeng Zhou ◽  
Bing Xie
Keyword(s):  
Cell Proliferation ◽  
Signaling Pathway ◽  
Bmp Signaling ◽  
Control Group ◽  
Protein Signaling ◽  
Alp Activity ◽  
Tissue Repair And Regeneration ◽  
Tumor Growth Factor ◽  
Morphogenetic Protein ◽  
Proliferation And Differentiation

The balance of osteoblasts and osteoclasts is critical for bone formation and remodeling and imbalance causes osteoporosis (OP). TGF-β regulates bone tissue repair and regeneration, but TGF-β’s role in osteogenesis in OP has not been elucidated. OVX-induced OP rat models were constructed and rat BMSCs were isolated and assigned into control group, OP group, and TGF-β group (transfected with TGF-β1 plasmid followed by analysis of cell proliferation by MTT assay, RUNX2 and OPN expression by Real time PCR, ALP activity and secretion of TGF-β, BMP-2 and BMP-9 by ELISA. In addition, RANKL was added to induce BMSCs differentiation into to osteoclasts which were transfected with TGF-β1 followed by analysis of cell proliferation, c-Fos and TRAP expression and secretion of BMP-2 and BMP-9. OP group rats had significantly reduced secretion of TGF-β1, BMP-2 and BMP-9, reduced cell proliferation, decreased RUNX2 and OPN expression and ALP activity (P <0.05). Transfection of TGF-β1 in BMSCs of OP group rats could significantly reverse the above changes (P <0.05). TGF-β1 significantly inhibited osteoclast proliferation, decreased expression of c-Fos and TRAP, and increased secretion of BMP-2 and BMP-9 (P <0.05). TGF-β1 level in OP is decreased. Up-regulating TGF-β promotes osteoblast differentiation in OP rats by regulating BMP signaling pathway, and inhibits osteoclast proliferation and differentiation.

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