| Title |
A Hypoxia-Targeted Boron Neutron Capture Therapy Agent for the Treatment of Glioma
|
|---|---|
| Published in |
Pharmaceutical Research, July 2016
|
| DOI | 10.1007/s11095-016-1977-2 |
| Pubmed ID | |
| Authors |
Micah John Luderer, Barbara Muz, Pilar de la Puente, Sanmathi Chavalmane, Vaishali Kapoor, Raymundo Marcelo, Pratim Biswas, Dinesh Thotala, Buck Rogers, Abdel Kareem Azab |
| Abstract |
Boron neutron capture therapy (BNCT) has the potential to become a viable cancer treatment modality, but its clinical translation has been limited by the poor tumor selectivity of agents. To address this unmet need, a boronated 2-nitroimidazole derivative (B-381) was synthesized and evaluated for its capability of targeting hypoxic glioma cells. B-381 has been synthesized from a 1-step reaction. Using D54 and U87 glioma cell lines, the in vitro cytotoxicity and cellular accumulation of B-381 has been evaluated under normoxic and hypoxic conditions compared to L-boronophenylalanine (BPA). Furthermore, tumor retention of B-381 was evaluated in vivo. B-381 had low cytotoxicity in normal and cancer cells. Unlike BPA, B-381 illustrated preferential retention in hypoxic glioma cells compared to normoxic glioma cells and normal tissues in vitro. In vivo, B-381 illustrated significantly higher long-term tumor retention compared to BPA, with 9.5-fold and 6.5-fold higher boron levels at 24 and 48 h, respectively. B-381 represents a new class of BNCT agents in which their selectivity to tumors is based on hypoxic tumor metabolism. Further studies are warranted to evaluate B-381 and similar compounds as preclinical candidates for future BNCT clinical trials for the treatment of glioma. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 37 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 6 | 16% |
| Student > Bachelor | 4 | 11% |
| Other | 4 | 11% |
| Student > Doctoral Student | 3 | 8% |
| Student > Ph. D. Student | 3 | 8% |
| Other | 8 | 22% |
| Unknown | 9 | 24% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 8 | 22% |
| Chemistry | 7 | 19% |
| Engineering | 3 | 8% |
| Physics and Astronomy | 2 | 5% |
| Psychology | 2 | 5% |
| Other | 7 | 19% |
| Unknown | 8 | 22% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 13 July 2016.
All research outputs
#20,335,770
of 22,880,691 outputs
Outputs from Pharmaceutical Research
#2,648
of 2,860 outputs
Outputs of similar age
#308,242
of 354,317 outputs
Outputs of similar age from Pharmaceutical Research
#41
of 43 outputs
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