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61.
Dr. Subhabrata Chaudhury Dr. Penchala Narasimharao Meka Dr. Monimoy Banerjee Caitlin N. Kent Prof. Dr. Brian S. J. Blagg 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(59):14747-14764
The 90 kDa heat shock proteins (Hsp90) are molecular chaperones that are responsible for the folding and/or trafficking of ∼400 client proteins, many of which are directly associated with cancer progression. Consequently, inhibition of Hsp90 can exhibit similar activity as combination therapy as multiple signaling nodes can be targeted simultaneously. In fact, seventeen small-molecule inhibitors that bind the Hsp90 N-terminus entered clinical trials for the treatment of cancer, all of which exhibited pan-inhibitory activity against all four Hsp90 isoforms. Unfortunately, most demonstrated undesired effects alongside induction of the pro-survival heat shock response. As a result, isoform-selective inhibitors have been sought to overcome these detriments. Described herein is a structure-based approach to design Hsp90β-selective inhibitors along with preliminary SAR. In the end, compound 5 was shown to manifest ∼370-fold selectivity for Hsp90β versus Hsp90α, and induced the degradation of select Hsp90β-dependent clients. These data support the development of Hsp90β-selective inhibitors as a new paradigm to overcome the detriments associated with pan-inhibition of Hsp90. 相似文献
62.
Sreemanta Mitra Amrita Mandal Anindya Datta Sourish Banerjee Dipankar Chakravorty 《Journal of magnetism and magnetic materials》2012
Nanosheets of nickel with thickness equal to 0.6 nm have been grown within the interlayer spaces of Na-4 mica. The sheets are made up of percolative clusters of nanodisks. Magnetization characteristics indicate a superparamagnetic behavior with a blocking temperature of 428 K. The magnetic anisotropy constant as extracted from the coercivity data has been found to be higher than that of bulk nickel by two orders of magnitude. This is ascribed to a large aspect ratio of the nickel nanophase. The Bloch exponent is also found to be considerably different from that of bulk nickel because of a size effect. The Bloch equation is still found to be valid for the two dimensional structures. 相似文献
63.
Thionyl chloride-pyridine mediated rearrangement of cylohexadienyl alcohols (2) and (8) has provided hyposantonin (3) and tetrahydronaphthalene (9), respectively, which in turn have served as potential intermediates for the synthesis of optically active and racemic occidol (6), respectively. 相似文献
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Tapas K. Paira Sanjib Banerjee Tarun K. Mandal 《Journal of polymer science. Part A, Polymer chemistry》2012,50(11):2130-2141
Well‐defined peptide‐poly(ε‐caprolactone) (Pep‐PCL) biohybrids were successfully synthesized by grafting‐from ring‐opening polymerization (ROP) of ε‐caprolactone (CL) using designed amine‐terminated sequence‐defined peptides as macroinitiators. MALDI‐TOF‐MS and 1H NMR analyses confirmed the successful attachment of peptide to the PCL chain. The gel permeation chromatography (GPC) measurement showed that the Pep‐PCL biohybrids with controllable molecular weights and low polydispersities (PDI <1.5) were obtained by this approach. The aggregation of Pep‐PCL hybrid molecules in THF solution resulted in the formation of micro/nanospheres as confirmed through FESEM, TEM, and DLS analyses. The circular dichroism study revealed that the secondary structure of peptide moiety was changed in the peptide‐PCL biohybrids. The crystallization and melting behavior of Pep‐PCL hybrids were somewhat changed compared with that of neat PCL of comparable molecular weight as revealed by DSC and XRD measurements. In Pep‐PCL biohybrids, extinction rings were observed in the PCL spherulites, in contrast with the normal spherulite morphology of the neat PCL. There was a substantial decrease (4–5 folds) in the spherulitic growth rate after the incorporation of peptide moiety at the end of PCL chain as measured by polarizing optical microscopy. Pseudomonas lipase catalyzed enzymatic degradation was studied for Pep‐PCL hybrids and neat PCL. © 2012 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012 相似文献
67.
An evaluation of the CYP2D6 and CYP3A4 inhibition potential of metoprolol metabolites and their contribution to drug–drug and drug–herb interaction by LC‐ESI/MS/MS 下载免费PDF全文
Roshan M. Borkar Murali Mohan Bhandi Ajay P. Dubey V. Ganga Reddy Prashanth Komirishetty Prajwal P. Nandekar Abhay T. Sangamwar Ahmed Kamal Sanjay K. Banerjee R. Srinivas 《Biomedical chromatography : BMC》2016,30(10):1556-1572
The aim of the present study was to evaluate the contribution of metabolites to drug–drug interaction and drug–herb interaction using the inhibition of CYP2D6 and CYP3A4 by metoprolol (MET) and its metabolites. The peak concentrations of unbound plasma concentration of MET, α‐hydroxy metoprolol (HM), O‐desmethyl metoprolol (ODM) and N‐desisopropyl metoprolol (DIM) were 90.37 ± 2.69, 33.32 ± 1.92, 16.93 ± 1.70 and 7.96 ± 0.94 ng/mL, respectively. The metabolites identified, HM and ODM, had a ratio of metabolic area under the concentration–time curve (AUC) to parent AUC of ≥0.25 when either total or unbound concentration of metabolite was considered. In vitro CYP2D6 and CYP3A4 inhibition by MET, HM and ODM study revealed that MET, HM and ODM were not inhibitors of CYP3A4‐catalyzed midazolam metabolism and CYP2D6‐catalyzed dextromethorphan metabolism. However, DIM only met the criteria of >10% of the total drug related material and <25% of the parent using unbound concentrations. If CYP inhibition testing is solely based on metabolite exposure, DIM metabolite would probably not be considered. However, the present study has demonstrated that DIM contributes significantly to in vitro drug–drug interaction. Copyright © 2016 John Wiley & Sons, Ltd. 相似文献
68.
Rahul S. Patil Dr. Debasis Banerjee Cory M. Simon Prof. Jerry L. Atwood Dr. Praveen K. Thallapally 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(36):12618-12623
Separation of xenon and krypton is of industrial and environmental concern; the existing technologies use cryogenic distillation. Thus, a cost‐effective, alternative technology for the separation of Xe and Kr and their capture from air is of significant importance. Herein, we report the selective Xe uptake in a crystalline porous organic oligomeric molecule, noria, and its structural analogue, PgC‐noria, under ambient conditions. The selectivity of noria towards Xe arises from its tailored pore size and small cavities, which allows a directed non‐bonding interaction of Xe atoms with a large number of carbon atoms of the noria molecular wheel in a confined space. 相似文献
69.
After our article, Physica A 391 (2012) 107–112, had been published online, T. Hillen told us about a theorem by Osaki, relevant for our numerical simulations. 相似文献
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