scholarly journals Recent Progress in Development of Polo-Like Kinase 1 Inhibitors: Efforts So Far

2021 ◽  
Author(s):  
Ramesh L. Sawant ◽  
Jyoti B. Wadekar ◽  
Rushikesh D. Ukirde ◽  
Ganesh D. Barkade
Keyword(s):  
Cell Proliferation ◽  
Protein Kinase ◽  
Cancer Therapy ◽  
Anticancer Agents ◽  
Clinical Studies ◽  
Recent Progress ◽  
Atp Binding Site ◽  
The Family ◽  
New Generation ◽  
Made In

Polo-like kinase 1(Plk1) plays an important role in the inhibition of cell proliferation and which is come under the family of serine/threonine-protein kinase. Which is a highly specific target for cancer therapy. In some clinical studies, Plk1 has been identified as a target for cancer. Currently, so many scientists are working on the development of the Plk1 inhibitors and so many scientists and researchers thinking about working on it. Recent strategy for Plk1 inhibition is the development of small molecule inhibitors which will inhibit the Plk1 through the ATP-binding site of the Plk. Now new generation Plk1 inhibitors being tested clinically which are targeting polo box domain. This review highlights the recent progress made in the development of Plk1 inhibitors as anticancer agents.

scholarly journals Recent Advances in the Development of Nano-Sculpted Films by Magnetron Sputtering for Energy-Related Applications

Nanomaterials ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 2039 ◽  
Author(s):  
Adriano Panepinto ◽  
Rony Snyders
Keyword(s):  
Thin Films ◽  
Magnetron Sputtering ◽  
Recent Progress ◽  
Dye Sensitized Solar Cells ◽  
Dye Sensitized ◽  
New Generation ◽  
Recent Experimental Work ◽  
Sensitized Solar Cells ◽  
Theoretical Results ◽  
Made In

In this paper, we overview the recent progress we made in the magnetron sputtering-based developments of nano-sculpted thin films intended for energy-related applications such as energy conversion. This paper summarizes our recent experimental work often supported by simulation and theoretical results. Specifically, the development of a new generation of nano-sculpted photo-anodes based on TiO2 for application in dye-sensitized solar cells is discussed.

scholarly journals Review of Therapeutic Applications of Radiolabeled Functional Nanomaterials

2019 ◽  
Vol 20 (9) ◽  
pp. 2323 ◽  
Author(s):  
Jongho Jeon
Keyword(s):  
Cancer Therapy ◽  
Anticancer Agents ◽  
Biomedical Applications ◽  
Recent Progress ◽  
Medical Science ◽  
Inorganic Nanoparticles ◽  
Original Material ◽  
Functional Nanomaterials ◽  
Therapeutic Applications ◽  
Physical And Chemical

In the last two decades, various nanomaterials have attracted increasing attention in medical science owing to their unique physical and chemical characteristics. Incorporating radionuclides into conventionally used nanomaterials can confer useful additional properties compared to the original material. Therefore, various radionuclides have been used to synthesize functional nanomaterials for biomedical applications. In particular, several α- or β-emitter-labeled organic and inorganic nanoparticles have been extensively investigated for efficient and targeted cancer treatment. This article reviews recent progress in cancer therapy using radiolabeled nanomaterials including inorganic, polymeric, and carbon-based materials and liposomes. We first provide an overview of radiolabeling methods for preparing anticancer agents that have been investigated recently in preclinical studies. Next, we discuss the therapeutic applications and effectiveness of α- or β-emitter-incorporated nanomaterials in animal models and the emerging possibilities of these nanomaterials in cancer therapy.

scholarly journals A REVIEW ON CYTOTOXIC ACTIVITY OF (GARCINIA COWA ROXB.): POTENTIAL AS AN ANTICANCER

2020 ◽  
Vol 11 (12) ◽  
pp. 1-6
Author(s):  
Nur Syakila ◽  
Aried Eriadi ◽  
Dwi Dinni Aulia Bakhtra ◽  
Ridho Asra
Keyword(s):  
Cancer Therapy ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Death Rate ◽  
Prevention And Treatment ◽  
Cytotoxic Compounds ◽  
Garcinia Cowa ◽  
Made In

Cancer is a disease of abnormal body tissue cells that turn malignant. From the data, it can be seen that new cases and the death rate from cancer continues to increase every year so that efforts are made in the search for new anticancer agents for the prevention and treatment of cancer. There are many natural ingredients that can be used for its benefits, one of which is the Asam Kandis plant (Garcinia cowa Roxb.) This plant is rich in phytochemicals. It can be an important source of natural cytotoxic compounds and has potential as an anticancer. The analysis showed that the extract or compound from the roots, bark, twigs, leaves, and fruit rind of Asam Kandis (Garcinia cowa Roxb.) has good cytotoxic activity and is active against cancer cell lines so that it can help in the development of cancer therapy.

scholarly journals Bugs as Cancer Drugs: Challenges and Opportunities

2019 ◽  
Vol 39 (15) ◽  
Author(s):  
Phillip J. Daschner ◽  
Avraham Rasooly ◽  
Jeffrey D. White
Keyword(s):  
Cancer Therapy ◽  
Solid Tumors ◽  
National Cancer Institute ◽  
Recent Progress ◽  
Cancer Therapies ◽  
Challenges And Opportunities ◽  
Bacterial Therapy ◽  
Funding Opportunities ◽  
First Time ◽  
Made In

ABSTRACT The first nonsurgical cancer therapy was bacterial therapy introduced in 1891 to treat solid tumors. Because in many cases it was harmful and ineffective, and with the emergence of radiotherapy and chemotherapy, bacterial therapy was discontinued. Motivated by the need to improve targeting of solid tumors and in light of recent progress made in developing microbial therapies, the National Cancer Institute has for the first time issued funding opportunities to stimulate research on bacterium-based cancer therapies for conditions under which current cancer therapies are inadequate.

Thrombolytic Therapy for Acute Ischemic Stroke: Past and Future

2019 ◽  
Vol 25 (3) ◽  
pp. 242-250 ◽  
Author(s):  
Keita Shibata ◽  
Terumasa Hashimoto ◽  
Takuro Miyazaki ◽  
Akira Miyazaki ◽  
Koji Nobe
Keyword(s):  
Clinical Trials ◽  
Ischemic Stroke ◽  
Thrombolytic Therapy ◽  
Clinical Studies ◽  
Recent Progress ◽  
Time Window ◽  
The Us ◽  
History Of ◽  
Ongoing Development ◽  
Made In

Background: Thromboembolic ischemic stroke, which is mainly caused by hypertension, as well as plasma dyslipidemia, arterial fibrillation and diabetes, is a leading cause of death in the US and other countries. Numerous clinical trials for thrombolytic drugs, which aimed to pharmacologically dissolve thrombi, were conducted in the 1950s, when the first thrombolytic therapy was performed. Methods: In this study, we summarize the pathophysiologic features of ischemic stroke, and the history of thrombolytic therapy, and discuss the recent progress that has been made in the ongoing development of thrombolytic drugs. Conclusion: Thrombolytic therapy is sometimes accompanied by harmful hemorrhagic insults; accordingly, a window of time wherein therapy can safely be performed has been established for this approach. Several basic and clinical studies are ongoing to develop next-generation thrombolytic drugs to expand the time window

scholarly journals In Vitro and in Silico Evaluation of Bikaverin as a Potent Inhibitor of Human Protein Kinase CK2

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1380 ◽  
Author(s):  
Samer Haidar ◽  
Dagmar Aichele ◽  
Robin Birus ◽  
Janine Hielscher ◽  
Tuomo Laitinen ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Protein Kinase ◽  
Cell Viability ◽  
Binding Site ◽  
Protein Kinase Ck2 ◽  
Potent Inhibitor ◽  
Cell Permeability ◽  
Atp Binding Site ◽  
Kinase Ck2

Protein kinase CK2 is an emerging target for therapeutic intervention in human diseases, particularly in cancer. Inhibitors of this enzyme are currently in clinical trials, indicating the druggability of human CK2. By virtual screening of the ZINC database, we found that the natural compound bikaverin can fit well in the ATP binding site of the target enzyme CK2. By further in vitro evaluation using CK2 holoenzyme, bikaverin turned to be a potent inhibitor with an IC50 value of 1.24 µM. In this work, the cell permeability of bikaverin was determined using a Caco-2 cell permeability assay as a prerequisite for cellular evaluation and the compound turned out to be cell permeable with a Papp- value of 4.46 × 10−6 cm/s. Bikaverin was tested for its effect on cell viability using a MTT assay and cell proliferation using an EdU assay in different cancer cell lines (MCF7, A427 and A431 cells). Cell viability and cell proliferation were reduced dramatically after treatment with 10 µM bikaverin for 24 h. Additionally the IncuCyte® live-cell imaging system was applied for monitoring the cytotoxicity of bikaverin in the three tested cancer cell lines. Finally, molecular dynamic studies were performed to clarify the ligand binding mode of bikaverin at the ATP binding site of CK2 and to identify the amino acids involved.

scholarly journals The inter-α-inhibitor family: from structure to regulation

1996 ◽  
Vol 315 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Jean-Philippe SALIER ◽  
Philippe ROUET ◽  
Gilda RAGUENEZ ◽  
Maryvonne DAVEAU
Keyword(s):  
Plasma Proteins ◽  
Recent Progress ◽  
Family Members ◽  
Protein Levels ◽  
The Family ◽  
Health And Disease ◽  
Structure Regulation ◽  
Uniform Nomenclature ◽  
Made In

Inter-α-inhibitor (IαI) and related molecules, collectively referred to as the IαI family, are a group of plasma protease inhibitors. They display attractive features such as precursor polypeptides that give rise to mature chains with quite distinct fates and functions, and inter-chain glycosaminoglycan bonds within the various molecules. The discovery of an ever growing number of such molecules has raised pertinent questions about their pathophysiological functions. The knowledge of this family has long been structure-oriented, whereas the structure/function and structure/regulation relationships of the family members and their genes have been largely ignored. These relationships are now being elucidated in events such as gene transcription, precursor processing, changes in plasma protein levels in health and disease and binding capacities that involve hyaluronan as well as other plasma proteins as ligands. This review presents some recent progress made in these fields that paves the way for an understanding of the functions of IαI family members in vivo. Finally, given the wealth of heterogeneous, complicated and sometimes contradictory nomenclatures and acronyms currently in use for this family, a new, uniform, nomenclature is proposed for IαI family genes, precursor polypeptides and assembled proteins.

Targeted Protein Degradation: An Emerging Therapeutic Strategy in Cancer

2020 ◽  
Vol 21 (2) ◽  
pp. 214-230 ◽  
Author(s):  
Samir H. Barghout
Keyword(s):  
Cancer Therapy ◽  
Protein Degradation ◽  
Anticancer Agents ◽  
Therapeutic Strategy ◽  
Cellular Targets ◽  
Protein Levels ◽  
Novel Approach ◽  
Major Mode ◽  
Intracellular Proteolysis ◽  
Made In

: Drug discovery in the scope of cancer therapy has been focused on conventional agents that nonselectively induce DNA damage or selectively inhibit the activity of key oncogenic molecules without affecting their protein levels. An emerging therapeutic strategy that garnered attention in recent years is the induction of Targeted Protein Degradation (TPD) of cellular targets by hijacking the intracellular proteolysis machinery. This novel approach offers several advantages over conventional inhibitors and introduces a paradigm shift in several pharmacological aspects of drug therapy. While TPD has been found to be the major mode of action of clinically approved anticancer agents such as fulvestrant and thalidomide, recent years have witnessed systematic endeavors to expand the repertoire of proteins amenable to therapeutic ablation by TPD. Such endeavors have led to three major classes of agents that induce protein degradation, including molecular glues, Proteolysis Targeting Chimeras (PROTACs) and Hydrophobic Tag (HyT)-based degraders. Here, we briefly highlight agents in these classes and key advances made in the field with a focus on clinical translation in cancer therapy.

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