Hallelujah Moments

2020 ◽  
Author(s):  
Eugene H. Cordes
Keyword(s):  
Drug Discovery ◽  
Weight Control ◽  
Metabolic Diseases ◽  
Biomedical Science ◽  
Parasitic Diseases ◽  
Cardiovascular Medicine ◽  
Step Process ◽  
Medical Need ◽  
Chemical Background ◽  
Creative Problem

This work provides eleven stories of drug discovery and features the scientists who made them. The outcome of the discovery work has provided novel therapies in cancer, cardiovascular medicine, antibacterial and antiviral infectious diseases, parasitic diseases, metabolic diseases, and weight control. Each story begins with the basic biomedical science that revealed the pathway to effective drug therapy and continues with the step-by-step process that leads from insight to a product in clinical practice meeting a defined medical need. The tales feature creative problem-solving by clever and dedicated scientists as they overcame roadblocks to success, hallelujah moments. Each drug discovery story reflects the interface between basic science, medicine, and drug discovery. Embedded in these tales are the societal and medical environments in which drug discovery takes place, the discovery of agents to treat HIV/AIDS, for example. Finally, a series of appendices provides basic chemical background for non-scientists.

The modern role of boron as a 'magic element' in biomedical science: Chemistry perspective

2021 ◽  
Author(s):  
SAURAV CHATTERJEE ◽  
NITESH MANI Mani TRIPATHI ◽  
Anupam Bandyopadhyay
Keyword(s):  
Drug Discovery ◽  
Boronic Acid ◽  
Toxic Element ◽  
Biomedical Science ◽  
Boronic Acid Derivatives

The boron was misconstrued as a toxic element for animals, which retarded the growth of boron-containing drug discovery in the last century. Nevertheless, modern applications of boronic acid derivatives are...

Drug Discovery and Development: The Road from an Idea to Promoting Human Health

2014 ◽  
Author(s):  
Eugene H. Cordes
Keyword(s):  
Drug Discovery ◽  
Two Dimensions ◽  
Human Medicine ◽  
Entry Point ◽  
Actual Process ◽  
Drug Discovery And Development ◽  
The Road ◽  
Medical Need ◽  
Entry Points ◽  
Long Time

We are almost where we need to be to grasp the tales of drug discovery that make up the final seven chapters of this book. The three previous chapters have laid the necessary scientific foundation. Here is my take on what you still need to know to understand drug discovery and development: the process of getting from an idea to a product that meets a medical need—from the laboratory to the bedside. We begin with a look at the process from 35,000 feet. Realize one thing at the outset: there is more than one way of getting from an idea to approval of a new drug for use in human medicine. The process described in this chapter captures the essential features of getting this done. However, each drug discovery effort poses specific problems, and getting around them may have an effect on the actual process followed. Nonetheless, what is described here is well worth understanding. Imagine running a maze that may have more than two dimensions, a huge number of entry points, and a very small number of exits or perhaps no exit at all, depending on your entry point. Have a look at Figure 5.1 to get the idea. You can see the external features but have no clue what awaits you inside. You can wander in this maze for a long time without getting very far. This pretty well symbolizes what happens during a lot of drug discovery projects. In target-based drug discovery, described in the next section, each entry point in the maze corresponds to a molecule chosen as a starting place to begin work. Most of these entry points are dead ends. No matter what you do or how hard you try, the only exit from the maze is the place you entered—nothing gained. The journey may be long, there may be encouraging signs along the way, but at the end of the day, you are back where you started.

scholarly journals Human beige adipocytes for drug discovery and cell therapy in metabolic diseases

2020 ◽  
Vol 11 (1) ◽  
Author(s):  
Amar M. Singh ◽  
Liang Zhang ◽  
John Avery ◽  
Amelia Yin ◽  
Yuhong Du ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cell Therapy ◽  
Metabolic Diseases ◽  
Beige Adipocytes

scholarly journals Perspective: The promises of a holistic view of proteins—impact on antibody engineering and drug discovery

2019 ◽  
Vol 39 (1) ◽  
Author(s):  
Ser-Xian Phua ◽  
Kwok-Fong Chan ◽  
Chinh Tran-To Su ◽  
Jun-Jie Poh ◽  
Samuel Ken-En Gan
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Antibody Engineering ◽  
Rational Drug Design ◽  
Biomedical Science ◽  
Great Promise ◽  
Holistic View ◽  
Rational Drug ◽  
Big Picture ◽  
Reductionist Approach

AbstractThe reductionist approach is prevalent in biomedical science. However, increasing evidence now shows that biological systems cannot be simply considered as the sum of its parts. With experimental, technological, and computational advances, we can now do more than view parts in isolation, thus we propose that an increasing holistic view (where a protein is investigated as much as a whole as possible) is now timely. To further advocate this, we review and discuss several studies and applications involving allostery, where distant protein regions can cross-talk to influence functionality. Therefore, we believe that an increasing big picture approach holds great promise, particularly in the areas of antibody engineering and drug discovery in rational drug design.

scholarly journals New Perspectives on Innovative Drug Discovery: An Overview

2010 ◽  
Vol 13 (3) ◽  
pp. 450 ◽  
Author(s):  
Si Yuan Pan ◽  
Shan Pan ◽  
Zhi-Ling Yu ◽  
Dik-Lung Ma ◽  
Si-Bao Chen ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Wide Spectrum ◽  
Therapeutic Interventions ◽  
Biomedical Science ◽  
Innovative Drug ◽  
Alternative Medicines ◽  
Traditional Remedies ◽  
Available Information ◽  
Rate Of Success ◽  
Total Sales

Despite advances in technology, drug discovery is still a lengthy, expensive, difficult, and inefficient process, with a low rate of success. Today, advances in biomedical science have brought about great strides in therapeutic interventions for a wide spectrum of diseases. The advent of biochemical techniques and cutting-edge bio/chemical technologies has made available a plethora of practical approaches to drug screening and design. In 2010, the total sales of the global pharmaceutical market will reach 600 billion US dollars and expand to over 975 billion dollars by 2013. The aim of this review is to summarize available information on contemporary approaches and strategies in the discovery of novel therapeutic agents, especially from the complementary and alternative medicines, including natural products and traditional remedies such as Chinese herbal medicine.

scholarly journals Retrospective Study of Clinical Cases in Ruminants at the UFRGS Veterinary Teaching Hospital

2019 ◽  
Vol 47 (1) ◽  
Author(s):  
Aline Moreira Borowsky ◽  
Carlos Afonso De Castro Beck ◽  
Eneder Rosana Oberst ◽  
Beatriz Riet Correa Rivero ◽  
Luciano Cavalheiro Melo ◽  
...  
Keyword(s):  
Retrospective Study ◽  
Metabolic Diseases ◽  
Specific Area ◽  
Production Costs ◽  
Parasitic Diseases ◽  
Prophylactic Measures ◽  
Control And Prevention ◽  
Foreign Body Obstruction ◽  
Large Animals ◽  
Conclusive Diagnosis

Background: The pillars of animal production are sanity, genetics and nutrition. Sanitary control of the herd is important to reduce production costs and maintain health. The Veterinary Clinics Hospital (HCV) of the Federal University of Rio Grande do Sul (UFRGS), located in Porto Alegre - RS, is the place of greatest casuistry of the state, with 20.000 annual attendances, between small and large animals. In view of this scenario, the present study aimed to determine the frequency and characterize the ruminants attended at HCV, in order to help in the future, in the construction of control and prevention strategies of diseases found. Materials, Methods & Results: The documents of ruminant care between January 2007 and May 2018 were searched in the archives of the Hospital of Veterinary Clinics of UFRGS. Data on species, race, sex, age and diagnosis were collected. Diagnoses were classified as conclusive and inconclusive and the cases with conclusive diagnosis were classified according to etiology: infectious and parasitic diseases, metabolic and nutritional diseases, reproductive and obstetric diseases, toxic diseases, traumatic diseases. The prevalence of diseases and characteristics of ruminants attended (species, sex, category) was calculated. During the study period, between January 2007 and May 2018, 341 ruminants were attended, with emphasis on sheep (42%), goats (39%) and cattle (18%). In addition, a camel with foreign body obstruction, a sambar deer with fracture of the first thoracic vertebra and a buffalo with ruminal impaction were attended. The care profile was mapped, with predominance of females (57%) and adults (59%). Most of the animals did not present a defined breed, but among the breeds stands out Texel, of cutting aptitude, in sheeps and Saanen and Holstein, of dairy aptitude, in goats and cattle, respectively. In the retrospective study, the diseases with infectious and parasitic etiology presented the highest prevalence with 27.5% of the attendances, followed by reproductive (17.5%), traumatic (13.5%), metabolic (10%), others (10%) and toxic (2.5%). Sixty-six animals had inconclusive diagnosis (19.5%). Discussion: The highest prevalences were infectious and parasitic diseases, with emphasis on myiasis and verminosis. So, it is perceived that management corrections are sufficient to reduce the number of occurrences of diseases and prophylactic measures such as vaccination protocol, vermifugation and adequate nutritional management are allied in this walk. Among the reproductive diseases, dystocia (42.85%), which is one of the main causes of mortality in the peripartum period, has been highlighted. Dog attack was the major cause of traumas in ruminants and urolithiasis was highlighted in metabolic diseases. In toxic diseases, copper intoxication was the most important. Sheep are extremely sensitive to this intoxication, as they tend to accumulate copper in the organism. The retrospective study made it possible to visualize the panorama of HCV UFRGS visits to ruminants in the last years, mapping the profile and determining the casuistry of the diseases. Studies of hospital veterinary casuistry are rare, mainly involving ruminants. At the end, it is concluded that studies referring to casuistry are important to know the predominant diseases in a specific area and its risk factors considering differential diagnosis and future prevention programs.

scholarly journals Effects of Cocoa Polyphenols and Dark Chocolate on Obese Adults: A Scoping Review

Nutrients ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 3695
Author(s):  
Hasmiza Halib ◽  
Amin Ismail ◽  
Barakatun-Nisak Mohd Yusof ◽  
Naomi Osakabe ◽  
Zulfitri Azuan Mat Daud
Keyword(s):  
Scoping Review ◽  
Weight Control ◽  
Metabolic Diseases ◽  
Public Health Problem ◽  
Dark Chocolate ◽  
Major Public Health Problem ◽  
Obese Adults ◽  
Cocoa Products ◽  
Different Populations

Obesity remains a major public health problem due to its increasing prevalence. Natural products have become common as adjunct therapeutic agents for treating obesity and preventing metabolic diseases. Cocoa and its products are commonly consumed worldwide. Dark chocolate, a rich source of polyphenols, has received attention lately for its beneficial role in the management of obesity; however, conflicting results are still being reported. This scoping review aims to provide a comprehensive understanding of the existing literature on the relationship and effects of cocoa and dark chocolate intake among obese adults. We searched multiple databases for research investigating the consumption of cocoa and/or dark chocolate in managing obesity among adults. This review includes epidemiological and human studies that were published in English over the last 10 years. Our review of the current literature indicates that epidemiological and human trials with obese adults have shown inconsistent results, which may be due to the different populations of subjects, and different types of cocoa products and doses used for intervention. Studies among obese adults are mainly focusing on obese individuals with comorbidities, as such more studies are needed to elucidate the role of cocoa polyphenols in weight control and preventing the risk of chronic diseases among obese individuals without comorbidities as well as healthy individuals. Careful adjustment of confounding factors would be required. The effects of cocoa and dark chocolate intake on obese adults were discussed, and further research is warranted to identify the gaps.

scholarly journals Identification of key candidate genes and molecular pathways in white fat browning: an anti-obesity drug discovery based on computational biology

2019 ◽  
Vol 13 (1) ◽  
Author(s):  
Yuyan Pan ◽  
Jiaqi Liu ◽  
Fazhi Qi
Keyword(s):  
Adipose Tissue ◽  
Drug Discovery ◽  
Text Mining ◽  
Protein Interaction ◽  
Metabolic Diseases ◽  
Interaction Analysis ◽  
Brown Fat ◽  
Molecular Pathways ◽  
Protein Protein Interaction ◽  
White Fat

Abstract Background Obesity—with its increased risk of obesity-associated metabolic diseases—has become one of the greatest public health epidemics of the twenty-first century in affluent countries. To date, there are no ideal drugs for treating obesity. Studies have shown that activation of brown adipose tissue (BAT) can promote energy consumption and inhibit obesity, which makes browning of white adipose tissue (WAT) a potential therapeutic target for obesity. Our objective was to identify genes and molecular pathways associated with WAT and the activation of BAT to WAT browning, by using publicly available data and computational tools; this knowledge might help in targeting relevant signaling pathways for treating obesity and other related metabolic diseases. Results In this study, we used text mining to find out genes related to brown fat and white fat browning. Combined with biological process and pathway analysis in GeneCodis and protein-protein interaction analysis by using STRING and Cytoscape, a list of high priority target genes was developed. The Human Protein Atlas was used to analyze protein expression. Candidate drugs were derived on the basis of the drug-gene interaction analysis of the final genes. Our study identified 18 genes representing 6 different pathways, targetable by a total of 33 drugs as possible drug treatments. The final list included 18 peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists, 4 beta 3 adrenoceptor (β3-AR) agonists, 1 insulin sensitizer, 3 insulins, 6 lipase clearing factor stimulants and other drugs. Conclusions Drug discovery using in silico text mining, pathway, and protein-protein interaction analysis tools may be a method of exploring drugs targeting the activation of brown fat or white fat browning, which provides a basis for the development of novel targeted therapies as potential treatments for obesity and related metabolic diseases.

scholarly journals Zebrafish-Based Screening Models for the Identification of Anti-Metastatic Drugs

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2407
Author(s):  
Joji Nakayama ◽  
Hideki Makinoshima
Keyword(s):  
Animal Model ◽  
Drug Discovery ◽  
Cancer Cells ◽  
High Throughput Screening ◽  
Metastatic Tumor ◽  
Tumor Formation ◽  
Zebrafish Model ◽  
Step Process ◽  
Physiological Relevance

Metastasis, a leading contributor to the morbidity of cancer patients, occurs through a multi-step process: invasion, intravasation, extravasation, colonization, and metastatic tumor formation. Each process is not only promoted by cancer cells themselves but is also affected by their microenvironment. Given this complexity, drug discovery for anti-metastatic drugs must consider the interaction between cancer cells and their microenvironments. The zebrafish is a suitable vertebrate animal model for in vivo high-throughput screening studies with physiological relevance to humans. This review covers the zebrafish model used to identify anti-metastatic drugs.

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