scholarly journals Compounds from Natural Sources as Protein Kinase Inhibitors

Biomolecules ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 1546
Author(s):  
Andrea Baier ◽  
Ryszard Szyszka
Keyword(s):  
Computational Analysis ◽  
Kinase Inhibitors ◽  
Natural Compounds ◽  
Lower Number ◽  
Protein Kinase Inhibitors ◽  
The Past ◽  
Sar Studies ◽  
Naturally Occurring ◽  
Starting Point ◽  
Microbial Infections

The advantage of natural compounds is their lower number of side-effects when compared to most synthetic substances. Therefore, over the past several decades, the interest in naturally occurring compounds is increasing in the search for new potent drugs. Natural compounds are playing an important role as a starting point when developing new selective compounds against different diseases. Protein kinases play a huge role in several diseases, like cancers, neurodegenerative diseases, microbial infections, or inflammations. In this review, we give a comprehensive view of natural compounds, which are/were the parent compounds in the development of more potent substances using computational analysis and SAR studies.

scholarly journals 3P089 Computational Analysis on Selectivity of Protein Kinase Inhibitors(Protein: Function,The 48th Annual Meeting of the Biophysical Society of Japan)

2010 ◽  
Vol 50 (supplement2) ◽  
pp. S160
Author(s):  
Noriyuki Futatsugi ◽  
Noriaki Okimoto ◽  
Atsushi Suenaga ◽  
Hideyosi Fuji ◽  
Tetsu Narumi ◽  
...  
Keyword(s):  
Protein Kinase ◽  
Annual Meeting ◽  
Protein Function ◽  
Computational Analysis ◽  
Kinase Inhibitors ◽  
Protein Kinase Inhibitors ◽  
Biophysical Society

Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders

2021 ◽  
Vol 13 (1) ◽  
pp. 45-62
Author(s):  
Cong-Cong Jia ◽  
Wang Chen ◽  
Zi-Li Feng ◽  
Zhao-Peng Liu
Keyword(s):  
Protein Kinase ◽  
Cellular Proliferation ◽  
Kinase Inhibitors ◽  
Biological Activities ◽  
Point Mutations ◽  
Protein Kinase Inhibitors ◽  
Binding Modes ◽  
The Past ◽  
Recent Developments ◽  
Key Aspects

RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers. This review summarizes the developments of a diversity of small molecule RET protein kinase inhibitors in the past 10 years. These RET inhibitors are classified according to their hinge binder chemotypes as: pyrimidines, including the pyrazolopyrimidines, pyrimidine oxazines, quinazolines, 4-aminopyrimidines and 4-aminopyridines; indolinones; 5-aminopyrazole-4-carboxamides; 3-trifluoromethylanilines; imidazopyridines, imidazopyridazines and pyrazopyridines; nicotinonitriles; pyridones and 1,2,4-triazoles. In each section, the biological activities of the inhibitors, their structure–activity relationships and possible binding modes with the RET kinase are introduced.

Holism, Chinese Medicine and Systems Ideologies: Rewriting the Past to Imagine the Future

2018 ◽  
Author(s):  
Volker Scheid
Keyword(s):  
Eighteenth Century ◽  
Chinese Medicine ◽  
Medical Humanities ◽  
Science And Technology Studies ◽  
Human Beings ◽  
The Past ◽  
Starting Point ◽  
The Us ◽  
Shared Objective ◽  
Definition Of

This chapter explores the articulations that have emerged over the last half century between various types of holism, Chinese medicine and systems biology. Given the discipline’s historical attachments to a definition of ‘medicine’ that rather narrowly refers to biomedicine as developed in Europe and the US from the eighteenth century onwards, the medical humanities are not the most obvious starting point for such an inquiry. At the same time, they do offer one advantage over neighbouring disciplines like medical history, anthropology or science and technology studies for someone like myself, a clinician as well as a historian and anthropologist: their strong commitment to the objective of facilitating better medical practice. This promise furthermore links to the wider project of critique, which, in Max Horkheimer’s definition of the term, aims at change and emancipation in order ‘to liberate human beings from the circumstances that enslave them’. If we take the critical medical humanities as explicitly affirming this shared objective and responsibility, extending the discipline’s traditional gaze is not a burden but becomes, in fact, an obligation.

Stress management: Corpus-based insights into vernacular interpretations of stress

2014 ◽  
Vol 10 (1) ◽  
pp. 81-93
Author(s):  
Laurel Smith Stvan
Keyword(s):  
Traumatic Stress ◽  
American English ◽  
Physical Symptom ◽  
The Body ◽  
Post Traumatic Stress ◽  
The Past ◽  
Academic Texts ◽  
Naturally Occurring ◽  
Post Traumatic ◽  
Semantic Shift

Examination of the term stress in naturally occurring vernacular prose provides evidence of three separate senses being conflated. A corpus analysis of 818 instances of stress from non-academic texts in the Corpus of Contemporary American English (COCA) and the Corpus of American Discourses on Health (CADOH) shows a negative prosody for stress, which is portrayed variously as a source outside the body, a physical symptom within the body and an emotional state. The data show that contemporary speakers intermingle the three senses, making more difficult a discussion between doctors and patients of ways to ‘reduce stress’, when stress might be interpreted as a stressor, a symptom, or state of anxiety. This conflation of senses reinforces the impression that stress is pervasive and increasing. In addition, a semantic shift is also refining a new sense for stress, as post-traumatic stress develops as a specific subtype of emotional stress whose use has increased in circulation in the past 20 years.

Cyber Peacekeeping: Critical Evaluation of Digital Blue Helmets Program

2020 ◽  
pp. 17-27
Author(s):  
Fahad Nabeel
Keyword(s):  
United Nations ◽  
Critical Evaluation ◽  
Threat Detection ◽  
Information And Communications Technologies ◽  
The Past ◽  
Research Article ◽  
Un Peacekeeping ◽  
Starting Point ◽  
Communications Technologies ◽  
Future Potential

In 2016, the United Nations (UN) launched the Digital Blue Helmets (DBH) program under its Office of Information and Communications Technologies (OICT). The launching of DBH was a continuation of a series of steps that the UN and its related agencies and departments have undertaken over the past decade to incorporate cyberspace within their working methodologies. At the time of inception, DBH was envisioned as a team capacitated to act as a replica of a physical peacekeeping force but for the sole purpose of overseeing cyberspace(s). Several research studies have been published in the past few years, which have conceptualized cyber peacekeeping in various ways. Some scholars have mentioned DBH as a starting point of cyber peacekeeping while some have proposed models for integration of cyber peacekeeping within the current UN peacekeeping architecture. However, no significant study has attempted to look at how DBH has evolved since its inception. This research article aims to examine the progress of DBH since its formation. It argues that despite four years since its formation, DBH is still far away from materializing its declared objectives. The article also discusses the future potential roles of DBH, including its collaboration with UN Global Pulse for cyber threat detection and prevention, and embedding the team along with physical peacekeepers.

Therapeutic Perspectives of Food Bioactive Peptides: A Mini Review

2019 ◽  
Vol 26 (9) ◽  
pp. 664-675
Author(s):  
Sulochana Priya
Keyword(s):  
Bioactive Peptides ◽  
Marine Organism ◽  
Biological Effects ◽  
Amide Bond ◽  
Therapeutic Effects ◽  
Specific Sequence ◽  
The Past ◽  
Cancer Immunity ◽  
Microbial Infections ◽  
Diverse Origin

Bioactive peptides are short chain of amino acids (usually 2-20) that are linked by amide bond in a specific sequence which have some biological effects in animals or humans. These can be of diverse origin like plant, animal, fish, microbe, marine organism or even synthetic. They are successfully used in the management of many diseases. In recent years increased attention has been raised for its effects and mechanism of action in various disease conditions like cancer, immunity, cardiovascular disease, hypertension, inflammation, diabetes, microbial infections etc. Bioactive peptides are more bioavailable and less allergenic when compared to total proteins. Food derived bioactive peptides have health benefits and its demand has increased tremendously over the past decade. This review gives a view on last two years research on potential bioactive peptides derived from food which have significant therapeutic effects.

Sign in / Sign up

Export Citation Format

Share Document