Monthly Archives: December 2017

Radiopharmaceuticals for diagnosis of Primary Hyperparathyroidism

Hyperparathyroidism (HPTH) is a condition in which the level of parathyroid hormone in blood is raised. Gold standard for the diagnosis of HPTH is a measurement of serum parathyroid hormone levels, accompanied by testing serum calcium levels, to differentiate between primary and secondary HPTH. The first line of treatment with primary HPTH is surgery to remove the adenoma or the tumor, whenever possible. It is in these cases that the imaging plays an important role for localization of tumor before surgery.Imaging can be anatomical that is ultrasound, CT and MRI or functional that is using nuclear medicine modalities (SPECT, SPECT/CT, PET/CT). This article reviews the nuclear medicine modalities, various radiopharmaceuticals and imaging techniques for parathyroid imaging.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/726

      

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Radiolabelled nanoparticles in cancer treatment: current status and developments

The current concepts of cancer therapy are moving towards personalized treatment regimen aiming to reduce toxicity and improve efficacy of therapeutic agents. With the development of molecular imaging and targeted therapies personalized care has received a shot in the arm. However, these developments are not without challenges. Drug delivery, metabolism, toxicity etc. challenge the effective utilization of such agents. Nanoparticles offer to overcome these hurdles with their unique physico-chemical properties which can be labeled with radionuclides and conjugated with ligands to achieve high specific activity in the intended areas. In this article, we discuss the present status of radiolabeled nanoparticles, the areas where they are being used and challenges that lie ahead. We intend to provide a basic outlook on the utilization of radiolabeled nanoparticles in cancer diagnosis and therapy.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/728

      

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Prof. Santanu Bhattacharya | Materials NanoScience Editorial Advisory Board Member

Professor S. Bhattacharya did Ph.D. from Rutgers University, New Brunswick, NJ, USA (Advisor: Prof. Robert. A. Moss) in 1988. From 1988 to 1991 he worked as Postdoctoral Research Associate at the Massachusetts Institute of Technology, Cambridge, MA, USA (Prof. Har Gobind Khorana, Nobel Laureate) and in 1991 he joined as Assistant Professor in Organic Chemistry division, Indian Institute of Science, Bangalore, India where he was promoted as Professor in 2001. He served as Chairman of department of Organic Chemistry, Indian Institute of Science from 2012 to 2015 and since April 22, 2015 he is Director and Senior Professor, Director’s Research Unit, Indian Association for the Cultivation of Science (IACS), Kolkata. India.

He has received numerous excellence awards such as
Ranbaxy Research Award, Pharmaceutical Sci., Ranbaxy Science Foundation 2013
Elected Fellow of the World Academy of Sciences 2012
TWAS Prize, The World Academy of Sciences, Trieste, Italy 2010
J. C. Bose National Fellowship, Department of Science & Technlogy 2008
Elected Fellow of Indian National Science Academy 2007
G.D. Birla Prize for Scientific Research, K.K. Birla Foundation 2007
Shanti Swarup Bhatnagar prize for the Chemical Sciences, CSIR 2003
National Bioscience Career Development Award, Department of Biotechnlogy 2002
Elected Fellow of Indian Academy of Sciences 2000
Swarnajayanti Fellowship, Department of Science & Technlogy 1998

He is associated with ‘Journal of Materials NanoScience‘ as Editorial Advisory Board Member since 2014. The journal link is http://www.pubs.iscience.in/journal/index.php/jmns

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Synthesis and Evaluation of [DUPA-6-Ahx-Lys (DOTA)-6-Ahx-RM2], a Novel, Bivalent Targeting Ligand for GRPr/PSMA Biomarkers of Prostate Cancer

In this study, we have prepared a novel, dual-biomarker, targeting ligand having high affinity and specificity for PSMA/GRPr receptors that are expressed on most prostate cancers. [DUPA-6-Ahx-Lys(DOTA)-6-Ahx-RM2] was synthesized and the new conjugate was metallated macroscopically with GaCl3, InCl3, and LuCl3 to form [DUPA-6-Ahx-Lys(M-DOTA)-6-Ahx-RM2] (where M = Ga, In, or Lu). These new agents, when radiolabeled with Ga-68, In-111, or Lu-177 hold theranostic potential for patients presenting with prostate cancer disease.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/718

      

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Synthesis and evaluation of a novel 68Ga-NODAGA-Erlotinib analogue towards PET imaging of Epidermal Growth Factor Receptor over-expressing cancers

In this paper we report the synthesis of 68Ga labeled NODAGA-Erlotinib for imaging of EGFR over-expressing tumors. NODAGA-Erlotinib conjugate was synthesized by reaction of the terminal alkyne of Erlotinib using Cu catalyzed click reaction. The conjugate was then radiolabeled with 68Ga in high radiochemical yields. The 68Ga NODAGA-Erlotinib conjugate also exhibited high in vitro stability. The log P value of 68Ga-NODAGA-Erlotinib was lower than that of 68Ga-NOTA-Erlotinib, a 68Ga based Erlotinib conjugate previously reported by our group. In the in vitro cell binding studies carried out in EGFR-positive A431 cells, 68Ga-NODAGA-erlotinib exhibited an uptake (7.8±1.3 %) lower than that of 68Ga-NOTA-Erlotinib (9.8±0.4%) showing that an increase in hydrophilicity possibly effected a decrease in cell permeability. The higher hydrophilicity of 68Ga-NODAGA-Erlotinib also led to significantly lower accumulation of 68Ga-NODAGA-Erlotinib in non-target organs in the biodistribution studies in Swiss mice. The overall properties of the 68Ga-NODAGA-Erlotinib conjugate are promising and reflect the role of hydrophilicity in reducing the non-specific uptake of the final radiotracer towards improving signal/noise ratio for further imaging studies.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/727

      

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Dr Brijesh Rathi

Dr. Brijesh Rathi,
Department of Chemistry,
Hansraj College,
University of Delhi,
Delhi-110007. India

webpage: http://hansrajcollege.ac.in/faculty-info.php?id=28

Research Interests: Medicinal Chemistry, Maleria, Drug development, synthetic organic chemistry, peptide chemistry, peptide drugs, nanomedicine.

Dr. Brijesh Rathi is a faculty of Chemistry in Hansraj College, University of Delhi and associated with Chemical Biology Letters and Applied NanoMedicine as Editorial Board Member.

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