Kanchan Chauhan, Ashutosh Arun, Saurabh Singh, Murli Manohar, Krishna Chuttani, Rituraj Konwar, Anila Dwivedi, Ravi Soni, Ajai Kumar Singh, Anil K. Mishra, and Anupama Datta
Bioconjugate Chem., Articles ASAP (As Soon As Publishable)
Publication Date (Web): March 21, 2016 (Article)
DOI: 10.1021/acs.bioconjchem.6b00024
The synthesis of estradiol based bivalent ligand [(EST)2DT] is reported and its potential for targeted imaging and therapy of ER(+) tumors has been evaluated. For the purpose, ethinylestradiol was functionalized with an azidoethylamine moiety via click ...
Daniel S. Albrecht, Cristina Granziera, Jacob M. Hooker, and Marco L. Loggia
ACS Chem. Neurosci., Articles ASAP (As Soon As Publishable)
Publication Date (Web): March 17, 2016 (Review)
DOI: 10.1021/acschemneuro.6b00056
Neuroinflammation is implicated in the pathophysiology of a growing number of human disorders, including multiple sclerosis, chronic pain, traumatic brain injury, and amyotrophic lateral sclerosis. As a result, interest in the development of novel methods ...
Pritam Thapa, Mengjie Li, Moses Bio, Pallavi Rajaputra, Gregory Nkepang, Yajing Sun, Sukyung Woo, and Youngjae You
J. Med. Chem., 2016, 59 (7), pp 3204–3214
Publication Date (Web): March 14, 2016 (Article)
DOI: 10.1021/acs.jmedchem.5b01971
Paclitaxel (PTX) is one of the most useful chemotherapeutic agents approved for several cancers, including ovarian, breast, pancreatic, and nonsmall cell lung cancer. However, it causes systemic side effects when administered parenterally. Photodynamic ...
J. S. Dileep Kumar, Mark D. Underwood, Norman R. Simpson, Suham A. Kassir, Jaya Prabhakaran, Vattoly J. Majo, Mihran J. Bakalian, Ramin V. Parsey, J. John Mann, and Victoria Arango
ACS Med. Chem. Lett., Articles ASAP (As Soon As Publishable)
Publication Date (Web): March 13, 2016 (Letter)
DOI: 10.1021/acsmedchemlett.5b00499
[18F]FECUMI-101 ([18F]1) is a 5HT1AR ligand demonstrating specific binding in brain regions corresponding to the distribution of 5-HT1AR in baboons. However, we detected moderate uptake of [18F]1 in baboon thalamus, a brain region lacking 5-HT1AR. We ...
Gaurav Malviya, Tapan Nayak, Christian Gerdes, Rudi A.J.O. Dierckx, Alberto Signore, and Erik F. J. de Vries
Mol. Pharmaceutics, 2016, 13 (4), pp 1329–1338
Publication Date (Web): March 10, 2016 (Article)
DOI: 10.1021/acs.molpharmaceut.5b00947
A noninvasive in vivo imaging method for NK cell trafficking is essential to gain further understanding of the pathogenesis of NK cell mediated immune response to the novel cancer treatment strategies, and to discover the homing sites and physiological ...
Yunquan Zheng, Yun Zhang, Deshan Chen, Haijun Chen, Ling Lin, Chengzhuo Zheng, and Yanghao Guo
J. Agric. Food Chem., 2016, 64 (12), pp 2541–2548
Publication Date (Web): March 8, 2016 (Article)
DOI: 10.1021/acs.jafc.5b05343
The Monascus pigment, rubropunctatin, was extracted and purified from red mold rice (RMR), and its cytotoxic activities against human cervical carcinoma HeLa cells were studied under the conditions with or without light irradiation. The IC50 value of ...
Florian Brulfert, Samir Safi, Aurélie Jeanson, Ernesto Martinez-Baez, Jérôme Roques, Catherine Berthomieu, Pier-Lorenzo Solari, Sandrine Sauge-Merle, and Éric Simoni
Inorg. Chem., 2016, 55 (6), pp 2728–2736
Publication Date (Web): March 8, 2016 (Article)
DOI: 10.1021/acs.inorgchem.5b02440
Because of their presence in the nuclear fuel cycle, neptunium and uranium are two actinides of main interest in case of internal contamination. Complexation of UVI and NpV by the target protein calmodulin (CaMWT) was therefore studied herein. Both ...
The interaction site of neptunyl with the calmodulin and electronic density. The complexation of uranium(VI) and neptunium(V) was investigated with recombinant one-site variant of the calmodulin N-terminal domain, denoted CaM-WT. The combination of experimental results (UV−vis and extended X-ray absorption fine structure spectroscopy) and density functional theory (DFT) calculations revealed that the coordination sphere of uranyl is pH dependent, while netunyl’s stays the same at every pH studied. The DFT calculations showed that at physiological pH the complex formed between the protein and the netunyl is more stable than the one formed with uranyl.
Xiaoxi Zhuang, Xiaowei Ma, Xiangdong Xue, Qiao Jiang, Linlin Song, Luru Dai, Chunqiu Zhang, Shubin Jin, Keni Yang, Baoquan Ding, Paul C. Wang, and Xing-Jie Liang
ACS Nano, 2016, 10 (3), pp 3486–3495
Publication Date (Web): March 7, 2016 (Article)
DOI: 10.1021/acsnano.5b07671
Photodynamic therapy (PDT) offers an alternative for cancer treatment by using ultraviolet or visible light in the presence of a photosensitizer and molecular oxygen, which can produce highly reactive oxygen species that ultimately leading to the ablation ...
W. Shirangi Fernando, André F. Martins, Piyu Zhao, Yunkou Wu, Garry E. Kiefer, Carlos Platas-Iglesias, and A. Dean Sherry
Inorg. Chem., 2016, 55 (6), pp 3007–3014
Publication Date (Web): March 3, 2016 (Article)
DOI: 10.1021/acs.inorgchem.5b02850
EuDOTA-tetraamide complexes as paraCEST agents offer an attractive platform for designing biological sensors and responsive agents. The early versions of these agents showed low sensitivity at temperature and power levels suitable for in vivo applications ...
Physical-chemical factors known to influence water exchange rates in EuDOTA-tetraamide complexes were used to design new paraCEST agents with record slow water exchange kinetics. The solution structure of the complexes as determined by analysis of lanthanide-induced paramagnetic shifts compared favorably to the structures determined by DTF calculations. In vitro CEST experiments demonstrated that these slow water exchange systems translated to optimal CEST imaging of one of the complexes in mouse kidneys.
Yeong Ah Cheon, Jun Hyuk Bae, and Bong Geun Chung
Langmuir, 2016, 32 (11), pp 2731–2736
Publication Date (Web): March 1, 2016 (Article)
DOI: 10.1021/acs.langmuir.6b00315
The protein-functionalized reduced graphene oxide (rGO) nanosheet is of great interest in stimuli-responsive drug delivery and controlled release applications. We developed doxorubicin (DOX)-loaded bovine serum albumin (BSA)-functionalized rGO (DOX-BSA-...
Roberto Improta, Fabrizio Santoro, and Lluís Blancafort
Chem. Rev., 2016, 116 (6), pp 3540–3593
Publication Date (Web): March 1, 2016 (Review)
DOI: 10.1021/acs.chemrev.5b00444
The photophysics and photochemistry of DNA is of great importance due to the potential damage of the genetic code by UV light. Quantum mechanical studies have played a key role in interpretating the results of modern time-resolved pump–probe spectroscopy, ...
Shoushan Wang, Peiwen Zhao, Changzhe Zhang, and Yuxiang Bu
J. Phys. Chem. B, 2016, 120 (10), pp 2649–2657
Publication Date (Web): February 25, 2016 (Article)
DOI: 10.1021/acs.jpcb.5b11432
Experimental studies showed that high energy radiation induced base release and DNA backbone breaks mainly occur at the neighboring 5′ nucleotide when a single-stranded DNA is modified by radiosensitizing 5-halogenated deoxyuridines. However, no mechanism ...
Dalong Ni, Zhiwei Shen, Jiawen Zhang, Chen Zhang, Renhua Wu, Jianan Liu, Meizhi Yi, Jing Wang, Zhenwei Yao, Wenbo Bu, and Jianlin Shi
ACS Nano, 2016, 10 (3), pp 3783–3790
Publication Date (Web): February 24, 2016 (Article)
DOI: 10.1021/acsnano.6b00462
In recent decades, extensive attention has been paid to developing anatomic and functional imaging contrast agents that could provide a wealth of complementary bioimaging information. Among them, dual-mode nanoprobes that combine anatomic magnetic ...
Afaf R. Genady, Nancy Janzen, Laura Banevicius, Mahmoud El-Gamal, Mohamed E. El-Zaria, and John F. Valliant
J. Med. Chem., 2016, 59 (6), pp 2660–2673
Publication Date (Web): February 19, 2016 (Article)
DOI: 10.1021/acs.jmedchem.5b01881
The feasibility of developing a single agent that can deliver radioactive iodine and also direct cellular immune function by engaging endogenous antibodies as an antibody-recruiting small molecule (ARM) was determined. A library of new prostate-specific ...
Carmen Seidl, Jan Ungelenk, Eva Zittel, Thomas Bergfeldt, Jonathan P. Sleeman, Ute Schepers, and Claus Feldmann
ACS Nano, 2016, 10 (3), pp 3149–3157
Publication Date (Web): February 19, 2016 (Article)
DOI: 10.1021/acsnano.5b03060
The nanoparticulate inorganic photosensitizer β-SnWO4 is suggested for photodynamic therapy (PDT) of near-surface tumors via reiterated 5 min blue-light LED illumination. β-SnWO4 nanoparticles are obtained via water-based synthesis and comprise excellent ...
J. S. Dileep Kumar, Mary Walker, Mathivanan Packiarajan, Vrej Jubian, Jaya Prabhakaran, Gamini Chandrasena, Mali Pratap, Ramin V. Parsey, and J. John Mann
ACS Chem. Neurosci., Articles ASAP (As Soon As Publishable)
Publication Date (Web): February 17, 2016 (Letter)
DOI: 10.1021/acschemneuro.5b00315
Neuropeptide Y receptor type 5 (NPY5R) is a G-protein coupled receptor (GPCR) that belongs to the subfamily of neuropeptide receptors (NPYR) that mediate the action of endogenous neuropeptide Y (NPY). Animal models and preclinical studies indicate a role ...
Sophie Poty, Eleni Gourni, Pauline Désogère, Frédéric Boschetti, Christine Goze, Helmut R. Maecke, and Franck Denat
Bioconjugate Chem., 2016, 27 (3), pp 752–761
Publication Date (Web): February 17, 2016 (Article)
DOI: 10.1021/acs.bioconjchem.5b00689
CXCR4 is a G protein-coupled receptor (GPCR), which is overexpressed in numerous diseases, particularly in multiple cancers. Therefore, this receptor represents a valuable target for imaging and therapeutic purposes. Among the different approaches, which ...
Sumit Kumar and Ashu Bhan Tiku
J. Agric. Food Chem., 2016, 64 (8), pp 1676–1685
Publication Date (Web): February 16, 2016 (Article)
DOI: 10.1021/acs.jafc.5b05067
The present study was aimed to evaluate the radioprotective effects of naringenin in vivo using Swiss albino mice as a model system. Oral administration of 50 mg/kg body weight of naringenin for 7 days prior to radiation exposure protected mice against ...
Joseph Lau, Zhengxing Zhang, Silvia Jenni, Hsiou-Ting Kuo, Zhibo Liu, Daniela Vullo, Claudiu T. Supuran, Kuo-Shyan Lin, and François Bénard
Mol. Pharmaceutics, 2016, 13 (3), pp 1137–1146
Publication Date (Web): February 11, 2016 (Article)
DOI: 10.1021/acs.molpharmaceut.5b00934
Carbonic anhydrase IX (CA-IX) is a HIF-1-inducible enzyme that is overexpressed in many cancer subtypes to promote survival and invasion in hypoxic niches. Pharmacologic inhibition of CA-IX is achievable through sulfonamide-based inhibitors and has been ...
Guohao Wang, Fan Zhang, Rui Tian, Liwen Zhang, Guifeng Fu, Lily Yang, and Lei Zhu
ACS Appl. Mater. Interfaces, 2016, 8 (8), pp 5608–5617
Publication Date (Web): February 10, 2016 (Research Article)
DOI: 10.1021/acsami.5b12400
Phototherapy is a light-triggered treatment for tumor ablation and growth inhibition via photodynamic therapy (PDT) and photothermal therapy (PTT). Despite extensive studies in this area, a major challenge is the lack of selective and effective ...
