scholarly journals Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends

2021 ◽  
Vol 28 (1) ◽  
Author(s):  
Kunal Nepali ◽  
Jing-Ping Liou
Keyword(s):  
Small Molecule ◽  
Clinical Stage ◽  
Cancer Therapeutics ◽  
Epigenetic Therapy ◽  
Antitumor Effects ◽  
Emerging Trends ◽  
Epigenetic Drug ◽  
Enzyme Isoforms ◽  
Recent Developments ◽  
Combination Regimens

AbstractEpigenetic drug discovery field has evidenced significant advancement in the recent times. A plethora of small molecule inhibitors have progressed to clinical stage investigations and are being explored exhaustively to ascertain conclusive benefits in diverse malignancies. Literature precedents indicates that substantial amount of efforts were directed towards the use of epigenetic tools in monotherapy as well as in combination regimens at the clinical level, however, the preclinical/preliminary explorations were inclined towards the identification of prudent approaches that can leverage the anticancer potential of small molecule epigenetic inhibitors as single agents only. This review article presents an update of FDA approved epigenetic drugs along with the epigenetic inhibitors undergoing clinical stage investigations in different cancer types. A detailed discussion of the pragmatic strategies that are expected to steer the progress of the epigenetic therapy through the implementation of emerging approaches such as PROTACS and CRISPR/Cas9 along with logical ways for scaffold fabrication to selectively approach the enzyme isoforms in pursuit of garnering amplified antitumor effects has been covered. In addition, the compilation also presents the rational strategies for the construction of multi-targeting scaffold assemblages employing previously identified pharmacophores as potential alternatives to the combination therapy.

Schottky diodes based on 2D materials for environmental gas monitoring: a review on emerging trends, recent developments and future perspectives

2021 ◽  
Author(s):  
Minu Mathew ◽  
Chandra Sekhar Rout
Keyword(s):  
Gas Sensing ◽  
2D Materials ◽  
Schottky Diodes ◽  
High Sensitivity ◽  
Future Perspectives ◽  
Working Temperature ◽  
Emerging Trends ◽  
Gas Sensing Properties ◽  
Recent Developments ◽  
Sensitivity And Selectivity

This review details the fundamentals, working principles and recent developments of Schottky junctions based on 2D materials to emphasize their improved gas sensing properties including low working temperature, high sensitivity, and selectivity.

Novel Nanolipoidal Systems for the Management of Skin Cancer

2020 ◽  
Vol 14 (2) ◽  
pp. 108-125
Author(s):  
Apoorva Singh ◽  
Nimisha
Keyword(s):  
Skin Cancer ◽  
Survival Rates ◽  
Cancer Therapeutics ◽  
The Body ◽  
Surgical Removal ◽  
The Novel ◽  
Skin Cancers ◽  
Recent Developments ◽  
Abnormal Cells ◽  
The Stability

: Skin cancer, among the various kinds of cancers, is a type that emerges from skin due to the growth of abnormal cells. These cells are capable of spreading and invading the other parts of the body. The occurrence of non-melanoma and melanoma, which are the major types of skin cancers, has increased over the past decades. Exposure to ultraviolet radiations (UV) is the main associative cause of skin cancer. UV exposure can inactivate tumor suppressor genes while activating various oncogenes. The conventional techniques like surgical removal, chemotherapy and radiation therapy lack the potential for targeting cancer cells and harm the normal cells. However, the novel therapeutics show promising improvements in the effectiveness of treatment, survival rates and better quality of life for patients. Different methodologies are involved in the skin cancer therapeutics for delivering the active ingredients to the target sites. Nano carriers are very efficient as they have the ability to improve the stability of drugs and further enhance their penetration into the tumor cells. The recent developments and research in nanotechnology have entitled several targeting and therapeutic agents to be incorporated into nanoparticles for an enhancive treatment of skin cancer. To protect the research works in the field of nanolipoidal systems various patents have been introduced. Some of the patents acknowledge responsive liposomes for specific targeting, nanocarriers for the delivery or co-delivery of chemotherapeutics, nucleic acids as well as photosensitizers. Further recent patents on the novel delivery systems have also been included here.

scholarly journals Glycosaminoglycans: Carriers and Targets for Tailored Anti-Cancer Therapy

Biomolecules ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 395
Author(s):  
Aikaterini Berdiaki ◽  
Monica Neagu ◽  
Eirini-Maria Giatagana ◽  
Andrey Kuskov ◽  
Aristidis M. Tsatsakis ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Targeted Delivery ◽  
Academic Research ◽  
Cancer Therapeutics ◽  
Disease Evolution ◽  
Structure Changes ◽  
Recent Developments ◽  
Distribution Composition ◽  
Membrane Components ◽  
Cancer Tissues

The tumor microenvironment (TME) is composed of cancerous, non-cancerous, stromal, and immune cells that are surrounded by the components of the extracellular matrix (ECM). Glycosaminoglycans (GAGs), natural biomacromolecules, essential ECM, and cell membrane components are extensively altered in cancer tissues. During disease progression, the GAG fine structure changes in a manner associated with disease evolution. Thus, changes in the GAG sulfation pattern are immediately correlated to malignant transformation. Their molecular weight, distribution, composition, and fine modifications, including sulfation, exhibit distinct alterations during cancer development. GAGs and GAG-based molecules, due to their unique properties, are suggested as promising effectors for anticancer therapy. Considering their participation in tumorigenesis, their utilization in drug development has been the focus of both industry and academic research efforts. These efforts have been developing in two main directions; (i) utilizing GAGs as targets of therapeutic strategies and (ii) employing GAGs specificity and excellent physicochemical properties for targeted delivery of cancer therapeutics. This review will comprehensively discuss recent developments and the broad potential of GAG utilization for cancer therapy.

A ratiometric colorimetric detection of the folate receptor based on terminal protection of small-molecule-linked DNA

The Analyst ◽  
2015 ◽  
Vol 140 (4) ◽  
pp. 1260-1264 ◽  
Author(s):  
Yanhong Zhu ◽  
Guangfeng Wang ◽  
Liang Sha ◽  
Yuwei Qiu ◽  
Hong Jiang ◽  
...  
Keyword(s):  
Small Molecule ◽  
Crucial Role ◽  
Folate Receptor ◽  
Low Cost ◽  
Colorimetric Detection ◽  
Cancer Therapeutics ◽  
Selective Detection

Development of strategies for the sensitive and selective detection of the folate receptor (FR) that are simple and low cost is of great importance for assessing cancer therapeutics due to its crucial role in physiological, pharmacological and pathological processes.

scholarly journals Focal adhesion kinase inhibitor TAE226 combined with Sorafenib slows down hepatocellular carcinoma by multiple epigenetics effects

2021 ◽  
Author(s):  
Ilaria Romito ◽  
Manuela Porru ◽  
Maria Rita Braghini ◽  
Luca Pompili ◽  
Nadia Panera ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Focal Adhesion Kinase ◽  
Focal Adhesion ◽  
Kinase Inhibitor ◽  
Malignant Tumours ◽  
Nurd Complex ◽  
Antitumor Effects ◽  
Combination Regimens

Abstract Background Hepatocellular carcinoma (HCC) is one of the most common and lethal malignant tumours worldwide. Sorafenib (SOR) is one of the most effective single-drug systemic therapy against advanced HCC, but the identification of novel combination regimens for a continued improvement in overall survival is a big challenge. Recent studies highlighted the crucial role of focal adhesion kinase (FAK) in HCC growth. The aim of this study was to investigate the antitumor effects of three different FAK inhibitors, alone or in combination with SOR, using in vitro and in vivo models of HCC. Methods The effect of PND1186, PF431396, TAE226 on cell viability was compared to SOR. Among them TAE226, emerging as the most effective FAKi, was then tested alone or in combination with SOR using 2D/3D human HCC cell line cultures and HCC xenograft murine models. The mechanisms of action were assessed by gene/protein expression and imaging approaches, combined with high-throughput methods. Results TAE226 emerged as the more effective FAKi to be combined with SOR against HCC. Combined TAE226 and SOR treatment reduced HCC growth both in vitro and in vivo by affecting tumour-promoting gene expression and inducing epigenetic changes via dysregulation of the nuclear interactome of FAK. We characterized a novel nuclear functional interaction between FAK and the NuRD complex. TAE226-mediated FAK depletion and SOR-promoted MAPK down-modulation causing an increase of histone H3 lysine 27 acetylation, counteracting its trimethylation by decreasing the nuclear amount of HDAC1/2. Conclusions Altogether, our findings provide the first evidence that TAE226 combined with SOR efficiently reduce HCC growth in vitro and in vivo. Our data also highlight that deep analysis of FAK nuclear interactome may lead to the identification of new promising therapeutic approaches for HCC.

Click and release: bioorthogonal approaches to “on-demand” activation of prodrugs

2019 ◽  
Vol 48 (4) ◽  
pp. 1077-1094 ◽  
Author(s):  
Xingyue Ji ◽  
Zhixiang Pan ◽  
Bingchen Yu ◽  
Ladie Kimberly De La Cruz ◽  
Yueqin Zheng ◽  
...  
Keyword(s):  
Small Molecule ◽  
Bioorthogonal Chemistry ◽  
On Demand ◽  
Recent Developments

This review summarizes recent developments in using bioorthogonal chemistry in prodrug design for the delivery of traditional small molecule- and gasotransmitter-based therapeutics.

scholarly journals Small molecule PIKfyve inhibitors as cancer therapeutics: Translational promises and limitations

2019 ◽  
Vol 383 ◽  
pp. 114771
Author(s):  
Ognian C. Ikonomov ◽  
Diego Sbrissa ◽  
Assia Shisheva
Keyword(s):  
Small Molecule ◽  
Cancer Therapeutics
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