Duane D. Miller
University of Tennessee Health Science Center
Biological activityCancerInternal medicineEndocrinologyReceptorChemistryStructure–activity relationshipIn vitroIn vivoMelanomaAgonistProstate cancerCancer researchBiochemistryAndrogen receptorStereochemistryMedicineTubulinBiologyPharmacology
473Publications
69H-index
12kCitations
Publications 472
Newest
#1Souvik Banerjee (University of Arkansas – Fort Smith)H-Index: 11
#2Shalini Yadav (Shiv Nadar University)H-Index: 1
Last. Kshatresh Dutta Dubey (Shiv Nadar University)H-Index: 13
view all 14 authors...
COVID-19, an acute viral pneumonia, has emerged as a devastating pandemic. Drug repurposing allows researchers to find different indications of FDA-approved or investigational drugs. In this current study, a sequence of pharmacophore and molecular modeling-based screening against COVID-19 Mpro (PDB: 6LU7) suggested a subset of drugs, from the Drug Bank database, which may have antiviral activity. A total of 44 out of 8823 of the most promising virtual hits from the Drug Bank were subjected to mo...
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#1Souvik Banerjee (University of Arkansas – Fort Smith)H-Index: 11
#2Foyez Mahmud (UTHSC: University of Tennessee Health Science Center)H-Index: 1
Last. Zhongzhi Wu (UTHSC: University of Tennessee Health Science Center)H-Index: 4
view all 17 authors...
Small molecules that interact with the colchicine binding site in tubulin have demonstrated therapeutic efficacy in treating cancers. We report the design, syntheses, and antitumor efficacies of new analogues of pyridopyrimidine and hydroquinoxalinone compounds with improved drug-like characteristics. Eight analogues, 5j, 5k, 5l, 5m, 5n, 5r, 5t, and 5u, showed significant improvement in metabolic stability and demonstrated strong antiproliferative potency in a panel of human cancer cell lines, i...
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#1Chuanhe YangH-Index: 9
#2Yinan WangH-Index: 9
Last. Lawrence M. PfefferH-Index: 61
view all 6 authors...
Glioblastoma (GBM) is a deadly and incurable brain cancer with limited therapeutic options. PFI-3 is a small-molecule bromodomain (BRD) inhibitor of the BRM/BRG1 subunits of the SWI/SNF chromatin remodeling complex. The objective of this study is to determine the efficacy of PFI-3 as a potential GBM therapy. We report that PFI-3 binds to these BRDs when expressed in GBM cells. PFI-3 markedly enhanced the antiproliferative and cell death-inducing effects of temozolomide (TMZ) in TMZ-sensitive GBM...
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#6Yong Li (St. Jude Children's Research Hospital)H-Index: 7
We previously reported a potent tubulin inhibitor CH-2-77. In this study, we optimized the structure of CH-2-77 by blocking metabolically labile sites and synthesized a series of CH-2-77 analogues. Two compounds, 40a and 60c, preserved the potency while improving the metabolic stability over CH-2-77 by 3- to 4-fold (46.8 and 29.4 vs 10.8 min in human microsomes). We determined the high-resolution X-ray crystal structures of 40a (resolution 2.3 A) and 60c (resolution 2.6 A) in complex with tubuli...
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#1Monica L Brown Lobbins (UTHSC: University of Tennessee Health Science Center)H-Index: 1
#2Imara-Safi O. Scott (UTHSC: University of Tennessee Health Science Center)
Last. Tejesh Patel (UTHSC: University of Tennessee Health Science Center)H-Index: 15
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Systemic sclerosis (SSc; scleroderma) is a chronic fibrotic disease involving TGF-β1. Low serum vitamin D (vit D) correlates with the degree of fibrosis and expression of TGF-β1. This study was designed to determine whether the noncalcemic vit D analog, 17,20S(OH)2pD, suppresses fibrosis and mediators of the TGF-β1 pathway in the bleomycin (BLM) model of fibrosis. Fibrosis was induced into the skin of female C57BL/6 mice by repeated injections of BLM (50 μg/100 μL) subcutaneously. Mice received ...
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#1Najah Albadari (UTHSC: University of Tennessee Health Science Center)H-Index: 2
#2Shanshan Deng (UTHSC: University of Tennessee Health Science Center)H-Index: 7
Last. Wei Li (UTHSC: University of Tennessee Health Science Center)H-Index: 55
view all 9 authors...
Abstract null null The survivin (BIRC5) expression is very low in normal differentiated adult tissues, but it is one of the most widely upregulated genes in tumor cells. The overexpression of survivin in many cancer types has been positively correlated with resistance to chemotherapy, tumor metastasis, and poor patient survival. Survivin is considered to be a cancer specific biomarker and serves as a potential cancer drug target. In this report, we describe the design and syntheses of a series o...
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#1Yali He (UTHSC: University of Tennessee Health Science Center)H-Index: 10
#2Dong Jin Hwang (UTHSC: University of Tennessee Health Science Center)H-Index: 20
Last. Duane D. Miller (UTHSC: University of Tennessee Health Science Center)H-Index: 69
view all 7 authors...
A series of propanamide derivatives were designed, synthesized, and pharmacologically characterized as selective androgen receptor degraders (SARDs) and pan-antagonists that exert a broad-scope androgen receptor (AR) antagonism. Incorporating different basic heteromonocyclic B-ring structural elements in the common A-ring-linkage-B-ring nonsteroidal antiandrogen general pharmacophore contributed to a novel scaffold of small molecules with SARD and pan-antagonist activities even compared to our r...
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#1Wen Shuai (Sichuan University)H-Index: 1
#2Guan Wang (Sichuan University)H-Index: 10
Last. Yuxi Wang (Sichuan University)H-Index: 18
view all 9 authors...
Microtubules play a crucial role in multiple cellular functions including mitosis, cell signaling, and organelle trafficking, which makes the microtubule an important target for cancer therapy. Despite the great successes of microtubule-targeting agents in the clinic, the development of drug resistance and dose-limiting toxicity restrict their clinical efficacy. In recent years, multitarget therapy has been considered an effective strategy to achieve higher therapeutic efficacy, in particular du...
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#1Shanshan DengH-Index: 7
#2Raisa KrutilinaH-Index: 10
Last. Tiffany N. SeagrovesH-Index: 24
view all 7 authors...
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#1Hongmei Cui (UTHSC: University of Tennessee Health Science Center)H-Index: 6
#2Qinghui WangH-Index: 10
Last. Wei LiH-Index: 55
view all 4 authors...
Melanoma is one of the deadliest skin cancers having a five-year survival rate around 15-20%. An overactivated MAPK/AKT pathway is well-established in BRAF mutant melanoma. Vemurafenib (Vem) was the first FDA-approved BRAF inhibitor and gained great clinical success in treating late-stage melanoma. However, most patients develop acquired resistance to Vem within 6-9 months. Therefore, developing a new treatment strategy to overcome Vem-resistance is highly significant. Our previous study reporte...
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