A5041716513- Cancer, Hypoxia, and Metabolism
- RNA Interference and Gene Delivery
- Synthesis and Biological Evaluation
- Cancer-related Molecular Pathways
- Biochemical and Molecular Research
- Cancer therapeutics and mechanisms
- DNA and Nucleic Acid Chemistry
- Advanced biosensing and bioanalysis techniques
- Synthesis and Biological Activity
- RNA modifications and cancer
- Protein Kinase Regulation and GTPase Signaling
- Computational Drug Discovery Methods
- Genomics, phytochemicals, and oxidative stress
- Antibiotic Resistance in Bacteria
- Cancer, Lipids, and Metabolism
- Cancer Cells and Metastasis
- Protein Structure and Dynamics
- Peptidase Inhibition and Analysis
- HIV/AIDS drug development and treatment
- RNA and protein synthesis mechanisms
- Glycosylation and Glycoproteins Research
- Monoclonal and Polyclonal Antibodies Research
- Epigenetics and DNA Methylation
- Bacteriophages and microbial interactions
- TGF-β signaling in diseases
Rutgers, The State University of New Jersey
2011-2024
Brown University
2024
Providence College
2024
Rutgers Cancer Institute of New Jersey
2006-2016
Johnson University
2003-2013
Rutgers Sexual and Reproductive Health and Rights
2013
Brunswick (United States)
2012-2013
Cancer Institute of Florida
2004-2013
University of Bristol
2000
University of South Alabama
1996-2000
Abstract Doxorubicin is among the most effective and widely used anticancer drugs in clinic. However, cardiotoxicity one of life-threatening side effects doxorubicin-based therapy. Dexrazoxane (Zinecard, also known as ICRF-187) has been clinic a cardioprotectant against doxorubicin cardiotoxicity. The molecular basis for cardioprotective effect dexrazoxane, however, not fully understood. In present study, we showed that dexrazoxane specifically abolished DNA damage signal γ-H2AX induced by...
Abstract Rapidly proliferating tumors attempt to meet the demands for nucleotide biosynthesis by upregulating folate pathways that provide building blocks pyrimidine and purine biosynthesis. In particular, key role of mitochondrial enzymes in providing formate de novo synthesis one-carbon moiety thymidylate has been recognized recent studies. We have shown a significant correlation between upregulation enzymes, high proliferation rates, sensitivity antagonist methotrexate (MTX). Burkitt...
As we enter the era of precision medicine, characterization cancer genomes will directly influence therapeutic decisions in clinic. Here describe a platform enabling functionalization rare gene mutations through their high-throughput construction, molecular barcoding and delivery to models for vivo tumour driver screens. We apply these technologies identify oncogenic drivers pancreatic ductal adenocarcinoma (PDAC). This approach reveals activity aberrations genes including NAD Kinase (NADK),...
Current prostate cancer management calls for identifying novel and more effective therapies. Self-renewing tumor-initiating cells (TICs) hold intrinsic therapy resistance account tumor relapse progression. As BMI-1 regulates stem cell self-renewal, impairing function TIC-tailored therapies appears to be a promising approach.We have previously developed combined immunophenotypic time-of-adherence assay identify CD49bhiCD29hiCD44hi as human TICs. We utilized this with patient-derived xenograft...
The prevalence of multidrug resistance among clinically significant bacterial pathogens underscores a critical need for the development new classes antibiotics with novel mechanisms action. Here we describe synthesis and evaluation guanidinomethyl biaryl compound {1-((4'-(tert-butyl)-[1,1'-biphenyl]-3-yl)methyl)guanidine} that targets cell division protein FtsZ. In vitro studies various FtsZ proteins reveal alters dynamics self-polymerization via stimulatory mechanism, while minimally...
Using the X-ray crystal structure of human topoisomerase I (TOP1)−DNA cleavable complex, we have developed a general model for ternary drug−DNA−TOP1 complex formed with camptothecin (CPT) and its analogues. This has drug intercalated between −1 +1 base pairs, E-ring pointing into minor groove A-ring directed toward major groove. The is stabilized by an array hydrogen bonding hydrophobic interactions both enzyme DNA. Significantly, proposed consistent current body experimental mutation,...
ABSTRACT Aromatic dicationic compounds, such as pentamidine, have potent antimicrobial activities. Clinical use of these compounds has been restricted, however, by their toxicity and limited oral activity. A novel approach, using amidoxime derivatives prodrugs, recently proposed to overcome limitations. Although results were presented for only one diamidine, the authors in original proposal claimed that would work effective prodrugs all pharmacologically active diamidines. Nine synthesized...
Studies described here were initiated to develop a model of glycoprotein hormone receptor structure and function. We found that the region links lutropin leucine-rich repeat domain (LRD) its transmembrane (TMD) has substantial roles in ligand binding signaling, hence we term it signaling specificity (SSD). Theoretical considerations indicated short SSDs marmoset salmon follitropin receptors have KH folds. assembled models lutropin, follitropin, thyrotropin by aligning their LRD, TMD,...
Various amino acid and peptide thioesters were tested as substrates for human proteinase 3 the best substrate is Boc‐Ala‐Ala‐Nva‐SBzl with a k cal / K m value of 1.0 × 10 6 nM it‐1 s Boc‐Ala‐Ala‐AA‐SBzl (AA = Val, Ala, or Met) are also good values (1‐4) 5 M −1 . Substituted isocoumarins potent inhibitors 7‐amino‐4‐chloro‐3‐(2‐bromoethoxy)isocoumarin 3.4‐dichloroisocoumarin (DCI) obs /[I] 4700 2600 , respectively. isocoumarins. phosphonates chloromethyl ketones inhibited less potently than...
G-quadruplex stabilizers such as telomestatin and HXDV bind with exquisite specificity to G-quadruplexes, but not triplex, duplex, or single-stranded DNAs. Studies have suggested that the antiproliferative possibly anti-tumor activities of these compounds are linked their inhibitory effect on telomerase and/or telomere function. In current studies, we show HXDV, a synthetic analog telomestatin, exhibits activity against both telomerase-positive -negative cells induces robust apoptosis within...
NAD<sup>+</sup> kinase (NADK) is the only known cytosolic enzyme that converts to NADP<sup>+</sup>, which subsequently reduced NADPH. The demand for NADPH in cancer cells elevated as reducing equivalents are required high levels of nucleotide, protein, and fatty acid synthesis found proliferating well neutralizing reactive oxygen species (ROS). We determined whether inhibition NADK activity a valid anticancer strategy alone combination with chemotherapeutic drugs induce ROS. In vitro vivo...
Dihydrofolate reductase (DHFR), because of its essential role in DNA synthesis, has been targeted for the treatment a wide variety human diseases, including cancer, autoimmune and infectious diseases. Methotrexate (MTX), tight binding inhibitor DHFR, is one most widely used drugs cancer especially effective acute lymphocytic leukemia, non-Hodgkin's lymphoma, osteosarcoma. Limitations to use include natural resistance acquired due decreased cellular uptake retention impaired polyglutamylate...
Alternate transcripts from a single gene locus greatly enhance the combinatorial flexibility of human transcriptome. Different patterns exon usage have been observed when comparing normal tissue to cancers, suggesting that variant may play role in tumor phenotype.Ribonucleic acid-sequencing (RNA-seq) data breast cancer samples was used identify an intronic start transcript Acyl-CoA oxidase 2, ACOX2 (ACOX2-i9). Difference expression between Estrogen Receptor (ER) positive and ER negative...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMechanism-Based Isocoumarin Inhibitors for Blood Coagulation Serine Proteases. Effect of the 7-Substituent in 7-Amino-4-chloro-3-(isothioureidoalkoxy)isocoumarins on Inhibitory and Anticoagulant PotencyChih-Min Kam, John E. Kerrigan, R. Richard Plaskon, Edward J. Duffy, Pete Lollar, F. L. Suddath, James C. PowersCite this: Med. Chem. 1994, 37, 9, 1298–1306Publication Date (Print):April 1, 1994Publication History Published online1 May 2002Published...
The 21 cm transition from neutral Hydrogen promises to be the best observational probe of Epoch Reionisation (EoR). This has led construction low-frequency radio interferometric arrays, such as Reionization Array (HERA), aimed at systematically mapping this emission for first time. Precision calibration, however, is a requirement in observations. Due spatial compactness HERA, array prone effects mutual coupling, which inevitably lead non-smooth calibration errors that contaminate data. When...