scholarly journals Targeting N-myristoylation for therapy of B-cell lymphomas

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Erwan Beauchamp ◽  
Megan C. Yap ◽  
Aishwarya Iyer ◽  
Maneka A. Perinpanayagam ◽  
Jay M. Gamma ◽  
...  
Keyword(s):  
B Cell ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cell Receptor ◽  
B Cell Lymphomas ◽  
Cancer Cell Death ◽  
Anti Cancer ◽  
Xenograft Models ◽  
Patients Experience

Abstract Myristoylation, the N-terminal modification of proteins with the fatty acid myristate, is critical for membrane targeting and cell signaling. Because cancer cells often have increased N-myristoyltransferase (NMT) expression, NMTs were proposed as anti-cancer targets. To systematically investigate this, we performed robotic cancer cell line screens and discovered a marked sensitivity of hematological cancer cell lines, including B-cell lymphomas, to the potent pan-NMT inhibitor PCLX-001. PCLX-001 treatment impacts the global myristoylation of lymphoma cell proteins and inhibits early B-cell receptor (BCR) signaling events critical for survival. In addition to abrogating myristoylation of Src family kinases, PCLX-001 also promotes their degradation and, unexpectedly, that of numerous non-myristoylated BCR effectors including c-Myc, NFκB and P-ERK, leading to cancer cell death in vitro and in xenograft models. Because some treated lymphoma patients experience relapse and die, targeting B-cell lymphomas with a NMT inhibitor potentially provides an additional much needed treatment option for lymphoma.

scholarly journals OvirusTdb: A Repository of Oncolytic Viruses used in Cancer Treatment

2020 ◽  
Author(s):  
Anjali Lathwal ◽  
Rajesh Kumar ◽  
Gajendra P.S. Raghava
Keyword(s):  
Cancer Treatment ◽  
Cancer Cell ◽  
Oncolytic Virus ◽  
Cancer Cell Line ◽  
Chemotherapeutic Agents ◽  
Oncolytic Viruses ◽  
Virus Species ◽  
Cancer Cell Death ◽  
Anti Cancer ◽  
Fight Against Cancer

AbstractOne of the emerging technologies to fight against cancer is oncolytic virus-based immunotherapy which directly lysis tumor cells. Recently, the FDA approved an oncolytic virus named T-vec for the treatment of melanoma; several hundred other viruses are in clinical trials. In order to facilitate the scientific community to fight against cancer, we build a repository of oncolytic viruses called OvirusTdb (https://webs.iiitd.edu.in/raghava/ovirustdb/). This is a manually curated repository where information is curated from research papers and patents. The current version of the repository maintains comprehensive information on therapeutically important oncolytic viruses with 5927 records where each record has 25 fields such as the virus species, cancer cell line, synergism with anti-cancer drugs, and many more. It stores information on 09 types of DNA and 15 types of RNA viruses; 300 recombinant and 09 wildtype viral strains; tested against 124 cancer types and 427 cancer cell lines. Approximately, 1047 records show improved anti-cancer response using combinatorial approach of chemotherapeutic agents with virus strains. Nearly, 3243 and 1506 records show cancer cell death via apoptosis induction and immune activation, respectively. In summary, a user-friendly web repository of oncolytic viruses for information retrieval and analysis have been developed to facilitate researchers in designing and discovering new oncolytic viruses for effective cancer treatment.

scholarly journals Data on the in vitro and in vivo anti-tumor effects of itraconazole, paclitaxel, and the two in combination in HT-29 and YM-1 cancer cell line and HT-29 colon cancer xenograft models

Data in Brief ◽  
2021 ◽  
Vol 35 ◽  
pp. 106862
Author(s):  
Mahdi Ghadi ◽  
Seyed Jalal Hosseinimehr ◽  
Fereshteh Talebpour Amiri ◽  
Alireza Mardanshahi ◽  
Zohreh Noaparast
Keyword(s):  
Colon Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Xenograft Models ◽  
Ht 29

scholarly journals Generation of KS-58 as the first K-Ras(G12D)-inhibitory peptide presenting anti-cancer activity in vivo

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Kotaro Sakamoto ◽  
Teruaki Masutani ◽  
Takatsugu Hirokawa
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Human Lung Cancer ◽  
Human Pancreatic Cancer ◽  
Inhibitory Peptide ◽  
Anti Cancer ◽  
Cancer Activity

AbstractRas mutations (e.g., occur in K-Ras, N-Ras, and H-Ras) are one of the most desirable and promising drug targets in chemotherapy treatments for cancer. However, there are still no approved drugs directly targeting mutated Ras. In 2017, an artificial cyclic peptide, KRpep-2d, was discovered as the first selective inhibitor of K-Ras(G12D), the most frequent K-Ras mutation. Here, we report the generation of KS-58, a KRpep-2d derivative that is identified as a bicyclic peptide and possess unnatural amino acid structures. Our in vitro data and molecular dynamics simulations suggest that KS-58 enters cells and blocks intracellular Ras–effector protein interactions. KS-58 selectively binds to K-Ras(G12D) and suppresses the in vitro proliferation of the human lung cancer cell line A427 and the human pancreatic cancer cell line PANC-1, both of which express K-Ras(G12D). Moreover, KS-58 exhibits anti-cancer activity when given as an intravenous injection to mice with subcutaneous or orthotropic PANC-1 cell xenografts. The anti-cancer activity is further improved by combination with gemcitabine. To the best of our knowledge, this is the first report of K-Ras(G12D)-selective inhibitory peptide presenting in vivo anti-cancer activity. KS-58 is an attractive lead molecule for the development of novel cancer drugs that target K-Ras(G12D).

scholarly journals Anti-Cancer Activity of Cayratia Auriculata Ethanolic Extracts Against Cancer Cell Line A549 An In Vitro Analysis

2020 ◽  
Vol 13 (2) ◽  
pp. 495-499
Author(s):  
Lalitha S Lalitha ◽  
Anusha D Anusha ◽  
Yogeshkumar Murkunde ◽  
Viji Devanand ◽  
Maheshkumar K Maheshkumar
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Anti Cancer ◽  
Ethanolic Extracts ◽  
Vitro Analysis ◽  
Cancer Activity ◽  
In Vitro Analysis

Fulvic acid promotes extracellular anti-cancer mediators from RAW 264.7 cells, causing to cancer cell death in vitro

2016 ◽  
Vol 36 ◽  
pp. 241-248 ◽  
Author(s):  
Rajapaksha Gedara Prasad Tharanga Jayasooriya ◽  
Matharage Gayani Dilshara ◽  
Chang-Hee Kang ◽  
Seungheon Lee ◽  
Yung Hyun Choi ◽  
...  
Keyword(s):  
Cell Death ◽  
Fulvic Acid ◽  
Cancer Cell ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Cancer Cell Death ◽  
Anti Cancer

scholarly journals Investigating the Effect of Loading Curcuminoids Using PCL-PU-βCD Nano-Composites on Physico-Chemical Properties, In-Vitro Release, and Ex-Vivo Breast Cancer Cell-Line

2021 ◽  
Vol 12 (3) ◽  
pp. 4074-4102
Keyword(s):  
Cancer Cell ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Cancer Cell Line ◽  
Preparation Technique ◽  
Polymeric Nanocomposites ◽  
Physico Chemical ◽  
Anti Cancer

Recently, cancer is deemed the main reason for death. Although most anti-cancer drugs have potent anti-cancer activity, their applications are greatly obstructed due to their flimsy solubility, stability, and high toxicity. Nanotechnology is considered the major distinctive tool for achieving highly safe and effective drug-delivery carriers. This survey studied the synthesis of poly-caprolactone polyurethane β-cyclodextrin (PCL-PU-βCD) amphiphilic copolymer and using such polymer with synthesized C5-curcuminoids as drug type to prepare polymeric-nano micelles by following two modified techniques, with confirming the synthesis of C5-curcuminoids, PCL, and PCL-PU-βCD, and the formation of polymeric-nanocomposites plus studying the formed nanocomposites; encapsulations, release patterns and kinetics, morphologies, physico-chemical properties and finally evaluating the death efficacy of these Curcuminoids-PCL-PU-βCD polymeric-nanocomposites on cancer cell cultures. The research results showed a successfully prepared C5-curcuminoid drug, PCL-PU-βCD polymer and Curcuminoids-PCL-PU-βCD polymeric-nanocomposites revealing; adequate encapsulations, controlled sustained releasing, promising physico-chemical properties, low cytotoxicity, and an auspicious IC50% on breast tumor cell-culture that were higher for the second preparation technique nanocomposites comparatively to the first preparation technique, despite such variation, both preparation techniques resulted in variances that were not significantly different (p>0.05).

Functionalized Nano-graphene Oxide as Multi-modal Clinic for Effective Drug Delivery

2017 ◽  
Vol 10 (4) ◽  
pp. 3768-3771
Author(s):  
Soumitra Satapathi ◽  
Rutusmita Mishra ◽  
Manisha Chatterjee ◽  
Partha Roy ◽  
Somesh Mohapatra
Keyword(s):  
Drug Delivery ◽  
Graphene Oxide ◽  
Cancer Cell ◽  
High Surface ◽  
High Surface Area ◽  
Cancer Cell Line ◽  
Xrd Analysis ◽  
Graphene Derivatives ◽  
Nano Graphene

Nano-materials based drug delivery modalities to specific organs and tissues has become one of the critical endeavors in pharmaceutical research. Recently, two-dimensional graphene has elicited considerable research interest because of its potential application in drug delivery systems. Here we report, the drug delivery applications of PEGylated nano-graphene oxide (nGO-PEG), complexed with a multiphoton active and anti-cancerous diarylheptanoid drug curcumin. Specifically, graphene-derivatives were used as nanovectors for the delivery of the hydrophobic anticancer drug curcumin due to its high surface area and easy surface functionalization. nGO was synthesized by modified Hummer’s method and confirmed by XRD analysis. The formation of nGO, nGO-PEG and nGO-PEG-Curcumin complex were monitored through UV-vis, IR spectroscopy. MTT assay and AO/EB staining found that nGO-PEG-Curcumin complex afforded highly potent cancer cell killing in vitro with a human breast cancer cell line MCF7.

New Platinum (II) Ternary Complexes of Formamidine and Pyrophosphate: Synthesis, Characterization and DFT Calculations and In vitro Cytotoxicity

2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Theoretical Calculations ◽  
Thermal Analyses ◽  
Cancer Cell Line ◽  
Cellular Growth ◽  
Planar Geometry ◽  
Square Planar ◽  
Vis Spectroscopy

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.

Sign in / Sign up

Export Citation Format

Share Document