scholarly journals Alternative scaffolds in radionuclide diagnosis of malignancies

2019 ◽  
Vol 18 (3) ◽  
pp. 125-133
Author(s):  
O. D. Bragina ◽  
V. I. Chernov ◽  
R. V. Zeltchan ◽  
I. G. Sinilkin ◽  
A. A. Medvedeva ◽  
...  
Keyword(s):  
High Specificity ◽  
The Body ◽  
Production Costs ◽  
Good Tolerance ◽  
New Class ◽  
The Past ◽  
Radionuclide Diagnosis ◽  
Good Penetration ◽  
Preclinical And Clinical Studies ◽  
High Immunogenicity

This review discusses a relatively new class of targeted molecules that is being actively studied for radionuclide diagnosis and treatment of malignancies. The full-size antibodies used so far have non-optimal pharmacological properties, slow distribution in the body, poor penetration into the tissue and kidney excretion, and high immunogenicity, which significantly complicates their use in clinical practice. Over the past decade, a new class of targeted molecules, called “non-immunoglobulin scaffolds” have become popular; they have all the requirements for optimal delivery of a radionuclide to tumor cells. Scaffolds usually are smaller in size in comparison with antibodies, but they are larger than peptides, and are characterized by high affinity and optimal biochemical, biophysical, biological, and economic features. The advantages of such proteins are their stable structure, good penetration into tissues, the possibility of additional functionalization and expression in the bacterial system, which ensures low production costs.The results of preclinical and clinical studies for diagnosis of malignancies using such proteins as affibody, adnectin, DARPins, etc., have demonstrated their high specificity, affinity, good tolerance and low immunogenicity. 

Derrida on Pornography: Putting (It) Up for Sale

Derrida Today ◽  
2013 ◽  
Vol 6 (1) ◽  
pp. 97-114 ◽  
Author(s):  
Christopher Morris
Keyword(s):  
Cultural Studies ◽  
English Translation ◽  
The Body ◽  
The Past ◽  
French Original ◽  
Definition Of ◽  
Critical Discourses ◽  
Academic Debate

Over the past thirty years, academic debate over pornography in the discourses of feminism and cultural studies has foundered on questions of the performative and of the word's definition. In the polylogue of Droit de regards, pornography is defined as la mise en vente that is taking place in the act of exegesis in progress. (Wills's idiomatic English translation includes an ‘it’ that is absent in the French original). The definition in Droit de regards alludes to the word's etymology (writing by or about prostitutes) but leaves the referent of the ‘sale’ suspended. Pornography as la mise en vente boldly restates the necessary iterability of the sign and anticipates two of Derrida's late arguments: that there is no ‘the’ body and that performatives may be powerless. Deriving a definition of pornography from a truncated etymology exemplifies the prosthesis of origin and challenges other critical discourses to explain how pornography can be understood as anything more than ‘putting (it) up for sale’.

Receptions of the Past: Commemoration, Racism, Desire

Somatechnics ◽  
2017 ◽  
Vol 7 (2) ◽  
pp. 288-303
Author(s):  
Michael Connors Jackman
Keyword(s):  
Critical Point ◽  
Social Relations ◽  
White Privilege ◽  
Body Politic ◽  
The Body ◽  
Race And Racism ◽  
Lesbian And Gay ◽  
The Past ◽  
History Of

This article investigates the ways in which the work of The Body Politic (TBP), the first major lesbian and gay newspaper in Canada, comes to be commemorated in queer publics and how it figures in the memories of those who were involved in producing the paper. In revisiting a critical point in the history of TBP from 1985 when controversy erupted over race and racism within the editorial collective, this discussion considers the role of memory in the reproduction of whiteness and in the rupture of standard narratives about the past. As the controversy continues to haunt contemporary queer activism in Canada, the productive work of memory must be considered an essential aspect of how, when and for what reasons the work of TBP comes to be commemorated. By revisiting the events of 1985 and by sifting through interviews with individuals who contributed to the work of TBP, this article complicates the narrative of TBP as a bluntly racist endeavour whilst questioning the white privilege and racially-charged demands that undergird its commemoration. The work of producing and preserving queer history is a vital means of challenging the intentional and strategic erasure of queer existence, but those who engage in such efforts must remain attentive to the unequal terrain of social relations within which remembering forms its objects.

Body and Desire

2018 ◽  
Author(s):  
Raphael A. Cadenhead
Keyword(s):  
Full Range ◽  
The Body ◽  
Gregory Of Nyssa ◽  
The Past ◽  
Ethical Discourse ◽  
Sex And Sexuality ◽  
Diachronic Analysis

Although the reception of the Eastern father Gregory of Nyssa has varied over the centuries, the past few decades have witnessed a profound awakening of interest in his thought, particularly in relation to the contentious issues of gender, sex, and sexuality. The Body and Desire sets out to retrieve the full range of Gregory’s thinking on the challenges of the ascetic life through a diachronic analysis of his oeuvre. Exploring his understanding of the importance of bodily and spiritual maturation in the practices of contemplation and virtue, Raphael Cadenhead recovers the vital relevance of this vision of transformation for contemporary ethical discourse.

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.

Recent Development of Small Molecule Glutaminase Inhibitors

2018 ◽  
Vol 18 (6) ◽  
pp. 432-443 ◽  
Author(s):  
Minsoo Song ◽  
Soong-Hyun Kim ◽  
Chun Young Im ◽  
Hee-Jong Hwang
Keyword(s):  
Small Molecule ◽  
Cell Metabolism ◽  
Phase 1 ◽  
Vital Role ◽  
Glutamine Metabolism ◽  
Inhibition Mechanism ◽  
Tumor Cell Growth ◽  
X Ray ◽  
New Class ◽  
Preclinical And Clinical Studies

Glutaminase (GLS), which is responsible for the conversion of glutamine to glutamate, plays a vital role in up-regulating cell metabolism for tumor cell growth and is considered to be a valuable therapeutic target for cancer treatment. Based on this important function of glutaminase in cancer, several GLS inhibitors have been developed in both academia and industry. Most importantly, Calithera Biosciences Inc. is actively developing the glutaminase inhibitor CB-839 for the treatment of various cancers, and it is currently being evaluated in phase 1 and 2 clinical trials. In this review, recent efforts to develop small molecule glutaminase inhibitors that target glutamine metabolism in both preclinical and clinical studies are discussed. In particular, more emphasis is placed on CB-839 because it is the only small molecule GLS inhibitor being studied in a clinical setting. The inhibition mechanism is also discussed based on X-ray structure studies of thiadiazole derivatives present in glutaminase inhibitor BPTES. Finally, recent medicinal chemistry efforts to develop a new class of GLS inhibitors are described in the hopes of providing useful information for the next generation of GLS inhibitors.

Recent Progress in Machine Learning-based Prediction of Peptide Activity for Drug Discovery

2019 ◽  
Vol 19 (1) ◽  
pp. 4-16 ◽  
Author(s):  
Qihui Wu ◽  
Hanzhong Ke ◽  
Dongli Li ◽  
Qi Wang ◽  
Jiansong Fang ◽  
...  
Keyword(s):  
Machine Learning ◽  
Drug Discovery ◽  
Large Scale ◽  
Recent Progress ◽  
High Specificity ◽  
Learning Approaches ◽  
Anticancer Peptides ◽  
The Past ◽  
Traditional Approaches ◽  
Large Scale Screening

Over the past decades, peptide as a therapeutic candidate has received increasing attention in drug discovery, especially for antimicrobial peptides (AMPs), anticancer peptides (ACPs) and antiinflammatory peptides (AIPs). It is considered that the peptides can regulate various complex diseases which are previously untouchable. In recent years, the critical problem of antimicrobial resistance drives the pharmaceutical industry to look for new therapeutic agents. Compared to organic small drugs, peptide- based therapy exhibits high specificity and minimal toxicity. Thus, peptides are widely recruited in the design and discovery of new potent drugs. Currently, large-scale screening of peptide activity with traditional approaches is costly, time-consuming and labor-intensive. Hence, in silico methods, mainly machine learning approaches, for their accuracy and effectiveness, have been introduced to predict the peptide activity. In this review, we document the recent progress in machine learning-based prediction of peptides which will be of great benefit to the discovery of potential active AMPs, ACPs and AIPs.

scholarly journals Host–Guest Inclusion Complexes of Essential Oils with Strong Antibacterial and Antifungal Features in Beta-Cyclodextrin for Solid-State Pharmaceutical Applications

2021 ◽  
Vol 11 (14) ◽  
pp. 6597
Author(s):  
Aldo Arrais ◽  
Marta Manzoni ◽  
Alessia Cattaneo ◽  
Valentina Gianotti ◽  
Nadia Massa ◽  
...  
Keyword(s):  
Solid State ◽  
Essential Oil ◽  
Essential Oils ◽  
Inclusion Complexes ◽  
Production Costs ◽  
Good Tolerance ◽  
Actual Application ◽  
Beta Cyclodextrin ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Essential oils are widely recognized as natural alternatives to pharmaceutical antibacterial and antifungal agents. With respect to standard pharmaceutics, the advantages of essential oils are their (i) low production costs, (ii) lack of chemical and biochemical drawbacks that are intrinsic to the synthetic production process and (iii) good tolerance by humans. On the other hand, the liquid nature of essential oils poses concerns about their actual application in different therapeutic issues regarding their persistence and the ability to control or prolong drug release. In this study, two essential oils from oregano and winter savory showing antibacterial and antifungal features were complexed in a solid state with beta-cyclodextrin. Host–guest inclusion complexes were characterized using FT-IR spectroscopy, ESI-MS and GC-MS techniques. Manyfold terpenic and non-terpenic components of the oils could be observed and unambiguously identified as being included inside the carbohydrate hosts. Many of them provided a specific biocidal action. Indeed, essential oil host–guest inclusion products were tested against two Candida species and an S. aureus reference strain, showing that the oils effectively maintained their liquid performances. Solid-state tablets of the essential oil inclusion complexes embedded in polyvinylpyrrolidone could be obtained. These results pave the way for the solid-state application of essential oils in antibacterial and antifungal pharmaceutical treatments.

scholarly journals Epithelial Protein Lost in Neoplasm, EPLIN, the Cellular and Molecular Prospects in Cancers

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1038
Author(s):  
Jianyuan Zeng ◽  
Wen G. Jiang ◽  
Andrew J. Sanders
Keyword(s):  
The Body ◽  
Early Years ◽  
Actin Binding ◽  
Cell Cycle Gene ◽  
Lim Domain ◽  
The Past ◽  
Concise Review ◽  
Cancerous Cell ◽  
Cytoskeletal Dynamics ◽  
In Cells

Epithelial Protein Lost In Neoplasm (EPLIN), also known as LIMA1 (LIM Domain And Actin Binding 1), was first discovered as a protein differentially expressed in normal and cancerous cell lines. It is now known to be key to the progression and metastasis of certain solid tumours. Despite a slow pace in understanding the biological role in cells and body systems, as well as its clinical implications in the early years since its discovery, recent years have witnessed a rapid progress in understanding the mechanisms of this protein in cells, diseases and indeed the body. EPLIN has drawn more attention over the past few years with its roles expanding from cell migration and cytoskeletal dynamics, to cell cycle, gene regulation, angiogenesis/lymphangiogenesis and lipid metabolism. This concise review summarises and discusses the recent progress in understanding EPLIN in biological processes and its implications in cancer.

2,2-Dialkylacetic Acids -A New Class of Naturally Occurring Lipid Constituents

1995 ◽  
Vol 50 (1-2) ◽  
pp. 123-126 ◽  
Author(s):  
Gottfried Raab ◽  
Jürgen Jacob
Keyword(s):  
Retention Time ◽  
Relative Retention Time ◽  
Methyl Esters ◽  
South American ◽  
Time Data ◽  
New Class ◽  
The Past ◽  
Relative Retention ◽  
Naturally Occurring ◽  
Acetic Acids

Abstract The uropygial gland waxes of the South American red-legged Seriema (Cariama cristata (L., 1766)) were found to be composed of unbranched alcohols and 2,2′-dialkyl-substituted acetic acids which so far have not been found in skin lipids. When used as a chemosystematic character, the occurrence of this lipid class separates the order Cariamiformes (Seriemas) from all other avian orders hitherto investigated, especially from the Gruiformes (cranes and rails) to which they have been tentatively attributed in the past. From the GC retention time data now available for a series of 2-alkyl-substituted fatty acid methyl esters relative retention time indices for other compounds may be predicted.

scholarly journals Epigenetic Regulation of Cannabinoid-Mediated Attenuation of Inflammation and Its Impact on the Use of Cannabinoids to Treat Autoimmune Diseases

2021 ◽  
Vol 22 (14) ◽  
pp. 7302
Author(s):  
Bryan Latrell Holloman ◽  
Mitzi Nagarkatti ◽  
Prakash Nagarkatti
Keyword(s):  
Autoimmune Diseases ◽  
Chronic Inflammation ◽  
Cannabinoid Receptors ◽  
T Regulatory Cells ◽  
Neurological Diseases ◽  
Suppressor Cells ◽  
The Body ◽  
New Class ◽  
Wide Range ◽  
Clinical Disorders

Chronic inflammation is considered to be a silent killer because it is the underlying cause of a wide range of clinical disorders, from cardiovascular to neurological diseases, and from cancer to obesity. In addition, there are over 80 different types of debilitating autoimmune diseases for which there are no cure. Currently, the drugs that are available to suppress chronic inflammation are either ineffective or overtly suppress the inflammation, thereby causing increased susceptibility to infections and cancer. Thus, the development of a new class of drugs that can suppress chronic inflammation is imperative. Cannabinoids are a group of compounds produced in the body (endocannabinoids) or found in cannabis (phytocannabinoids) that act through cannabinoid receptors and various other receptors expressed widely in the brain and immune system. In the last decade, cannabinoids have been well established experimentally to mediate anti-inflammatory properties. Research has shown that they suppress inflammation through multiple pathways, including apoptosis and inducing immunosuppressive T regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSCs). Interestingly, cannabinoids also mediate epigenetic alterations in genes that regulate inflammation. In the current review, we highlight how the epigenetic modulations caused by cannabinoids lead to the suppression of inflammation and help identify novel pathways that can be used to target autoimmune diseases.

Sign in / Sign up

Export Citation Format

Share Document