AR antagonists(Androgen Receptor antagonists), SIRT1 stimulants(NAD-dependent deacetylase sirtuin 1 stimulants), SREBF1 inhibitors(Sterol regulatory element binding transcription factor 1 inhibitors)

+ [1]

Therapeutic Areas

NeoplasmsImmune System DiseasesInfectious Diseases+ [2]

Active Indication

Prostatic CancerAIDS-Associated NephropathyDiabetic Nephropathies

Inactive Indication-

Originator Organization

Texas A&M University

Active Organization

Chinese People's Liberation Army General HospitalLong Island University, Brooklyn,

Icahn School of Medicine at Mount Sinai

Inactive Organization

Texas A&M University

Thomas Jefferson UniversityUniversity of Kansas Medical Center Auxiliary, Inc.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H21BCl2O2

InChIKeyQQAGHMVHZOMHPO-AATRIKPKSA-N

CAS Registry1333375-02-2

100 Clinical Results associated with BF-175

100 Translational Medicine associated with BF-175

100 Patents (Medical) associated with BF-175

Literatures (Medical) associated with BF-175

01 Apr 2021·Kidney InternationalQ1 · MEDICINE

Low expression of HIV genes in podocytes accelerates the progression of diabetic kidney disease in mice

Q1 · MEDICINE

Article

Author: He, John Cijiang ; Li, Huilin ; Xie, Liyi ; Jiang, Hongli ; Xiao, Wenzhen ; Feng, Jie ; Bao, Li ; Wang, Xuan ; Li, Zhengzhe ; Lu, Wanhong ; Chen, Yuqiang ; Lee, Kyung

With the widespread use combination antiretroviral therapy, there has been a dramatic decrease in HIV-associated nephropathy. However, although the patients living with HIV have low or undetectable viral load, the prevalence of chronic kidney disease (CKD) in this population remains high. Additionally, improved survival is associated with aging-related comorbidities such as diabetes and cardiovascular disease. A faster progression of CKD is associated with concurrent HIV infection and diabetes than with HIV infection or diabetes alone. To explore the potential pathogenic mechanisms that synergistically drive CKD progression by diabetes and HIV infection, we generated a new mouse model with a relatively low expression of HIV-1 proviral genes specifically in podocytes (pod-HIV mice) to better mimic the setting of kidney injury in patients living with HIV. While no apparent kidney phenotypes were observed at baseline in pod-HIV mice, the induction of mild diabetic kidney disease with streptozotocin led to significant worsening of albuminuria, glomerular injury, podocyte loss, and kidney dysfunction as compared to the mice with diabetes alone. Mechanistically, diabetes and HIV-1 synergistically increased the glomerular expression of microRNA-34a (miR-34a), thereby reducing the expression of Sirtuin-1 (SIRT1) deacetylase. These changes were also associated with increased acetylation and activation of p53 and p65 NF-κB and with enhanced expression of senescence and inflammatory markers. The treatment of diabetic pod-HIV mice with the specific Sirtuin-1 agonist BF175 significantly attenuated albuminuria and glomerulopathy. Thus, our study highlights the reduction in Sirtuin-1 as a major basis of CKD progression in diabetic patients living with HIV and suggests Sirtuin-1 agonists as a potential therapy.

01 Mar 2021·Molecular and Cellular EndocrinologyQ2 · MEDICINE

BF175 inhibits endometrial carcinoma through SREBP-regulated metabolic pathways in vitro

Q2 · MEDICINE

Article

Author: Das, Bhaskar C ; Hu, Ruofan ; Li, Weihua ; Gu, Weiting ; Yang, Fajun ; Wang, Chenguang ; Ji, Junyuan ; Wang, Qiong ; Zhou, Jie ; Tai, Yanhong

Elevated lipogenesis is an important metabolic hallmark of rapidly proliferating tumor such as endometrial carcinoma (EC). The sterol regulatory element-binding protein 1 (SREBP1) is a master regulator of lipogenesis and involved in EC proliferation. BF175 is a novel chemical inhibitor of SREBP pathway, and has shown potent anti-lipogenic effects. However, the effect of BF175 on EC cells are yet to be determined. In the present study, we found that BF175 decreased cell viability, colony formation and migratory capacity, inducing autophagy and mitochondrial related apoptosis in EC cell line AN3CA. Z-VAD-FMK partially attenuated the effect of BF175 on AN3CA. In addition, BF175 significantly downregulated SREBPs and their downstream genes. The levels of free fatty acids and total cholesterol were also inhibited. Microarray analysis suggested BF175 treatment obviously affected lipid metabolic pathways in EC. Taken together, we validated BF175 exhibited anti-tumor activity by targeting SREBP-dependent lipogenesis and inducing apoptosis which mitochondrial pathway involved in, suggesting that it's potential as a novel therapeutic reagent for EC.

01 Aug 2020·American Journal of Physiology-Renal PhysiologyQ3 · MEDICINE

Role of SIRT1 in HIV-associated kidney disease

Q3 · MEDICINE

Article

Author: Hyink, Deborah P. ; Wang, Andrew ; Zhang, Weijia ; He, John Cijiang ; Das, Gokul C. ; Wang, Xuan ; Li, Zhengzhe ; Das, Bhaskar ; Lee, Kyung ; Yuan, Weijie ; Klotman, Paul E. ; Liu, Ruijie

Human immunodeficiency virus (HIV) infection of kidney cells can lead to HIV-associated nephropathy (HIVAN) and aggravate the progression of other chronic kidney diseases. Thus, a better understanding of the mechanisms of HIV-induced kidney cell injury is needed for effective therapy against HIV-induced kidney disease progression. We have previously shown that the acetylation and activation of key inflammatory regulators, NF-κB p65 and STAT3, were increased in HIVAN kidneys. Here, we demonstrate the key role of sirtuin 1 (SIRT1) deacetylase in the regulation of NF-κB and STAT3 activity in HIVAN. We found that SIRT1 expression was reduced in the glomeruli of human and mouse HIVAN kidneys and that HIV-1 gene expression was associated with reduced SIRT1 expression and increased acetylation of NF-κB p65 and STAT3 in cultured podocytes. Interestingly, SIRT1 overexpression, in turn, reduced the expression of negative regulatory factor in podocytes stably expressing HIV-1 proviral genes, which was associated with inactivation of NF-κB p65 and a reduction in HIV-1 long terminal repeat promoter activity. In vivo, the administration of the small-molecule SIRT1 agonist BF175 or inducible overexpression of SIRT1 specifically in podocytes markedly attenuated albuminuria, kidney lesions, and expression of inflammatory markers in Tg26 mice. Finally, we showed that the reduction in SIRT1 expression by HIV-1 is in part mediated through miR-34a expression. Together, our data provide a new mechanism of SIRT1 regulation and its downstream effects in HIV-1-infected kidney cells and indicate that SIRT1/miR-34a are potential drug targets to treat HIV-related kidney disease.

100 Deals associated with BF-175

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Preclinical	United States	Long Island University, Brooklyn,	28 Apr 2025
AIDS-Associated Nephropathy	Preclinical	United States	Icahn School of Medicine at Mount Sinai	19 Oct 2020
Diabetic Nephropathies	Preclinical	China	Chinese People's Liberation Army General Hospital	31 Oct 2017
Diabetic Nephropathies	Preclinical	United States	Icahn School of Medicine at Mount Sinai	31 Oct 2017
Neoplasms	Discovery	-	Thomas Jefferson University	-
Neoplasms	Discovery	-	University of Kansas Medical Center Auxiliary, Inc.	-
Neoplasms	Discovery	-	Texas A&M University	-

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