scholarly journals Update in TSH Receptor Agonists and Antagonists

2012 ◽  
Vol 97 (12) ◽  
pp. 4287-4292 ◽  
Author(s):  
Marvin C. Gershengorn ◽  
Susanne Neumann
Keyword(s):  
Thyroid Function ◽  
Small Molecule ◽  
Physiological Role ◽  
Tsh Receptor ◽  
Thyroid Tumors ◽  
Inverse Agonists ◽  
Small Molecule Drug ◽  
Pathological Conditions ◽  
Receptor Agonists And Antagonists

The physiological role of the TSH receptor (TSHR) as a major regulator of thyroid function is well understood, but TSHRs are also expressed in multiple normal extrathyroidal tissues, and the physiological roles of TSHRs in these tissues are unclear. Moreover, TSHRs play a major role in several pathological conditions including hyperthyroidism, hypothyroidism, and thyroid tumors. Small molecule, “drug-like” TSHR agonists, neutral antagonists, and inverse agonists may be useful as probes of TSHR function in extrathyroidal tissues and as leads to develop drugs for several diseases of the thyroid. In this Update, we review the most recent findings regarding the development and use of these small molecule TSHR ligands.

scholarly journals Towards Academic Drug Development Guidelines

2019 ◽  
Author(s):  
Christopher Southan
Keyword(s):  
Drug Development ◽  
Success Rate ◽  
Case Studies ◽  
Small Molecule ◽  
Research Productivity ◽  
Medicinal Chemistry ◽  
Academic Development ◽  
Commercial Development ◽  
Small Molecule Drug

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.

scholarly journals Towards Academic Drug Development Guidelines

2019 ◽  
Author(s):  
Christopher Southan
Keyword(s):  
Drug Development ◽  
Success Rate ◽  
Case Studies ◽  
Small Molecule ◽  
Research Productivity ◽  
Medicinal Chemistry ◽  
Academic Development ◽  
Commercial Development ◽  
Small Molecule Drug

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.

MYOSTATIN - A MODERN UNDERSTANDING OF THE PHYSIOLOGICAL ROLE AND SIGNIFICANCE IN THE DEVELOPMENT OF AGE-ASSOCIATED DISEASES

2021 ◽  
pp. 701-706
Author(s):  
А.А. Газданова ◽  
В.Г. Кукес ◽  
О.К. Парфенова ◽  
Н.Г. Сидоров ◽  
А.В. Перков ◽  
...  
Keyword(s):  
Muscle Growth ◽  
Physiological Role ◽  
Review Article ◽  
Negative Regulator ◽  
Transforming Growth Factors ◽  
Endogenous Factors ◽  
Pathological Conditions ◽  
Physiological Properties ◽  
The Family

Миостатин - белок, принадлежащий к классу миокинов, семейству трансформирующих факторов роста β (TGF-β). В обзорной статье, анализирующей данные литературы, показана ключевая роль миостатина в развитии старческой саркопении и кахексии при различных патологических состояниях, таких как рак, ХСН, ХБП, ХОБЛ и др. В статье рассматривается структура миостатина, подробная схема синтеза и его активации, механизм действия как негативного регулятора роста и дифференцировки мышц при этих патологических состояниях. Выделены основные физиологические свойства и клиническое значение. Рассмотрены экзогенные и эндогенные факторы, регулирующие экспрессию миостатина, и возможные механизмы их действия. Myostatin is a protein belonging to the myokine class, the family of transforming growth factors β (TGF-β). The review article, based on the analysis of literature data, shows the key role of myostatin in the development of senile sarcopenia and cachexia in various pathological conditions, such as cancer, chronic heart failure, chronic renal failure, COPD, etc. The article discusses the structure of myostatin, provides a detailed diagram of the synthesis and activation of myostatin, the ways of implementing the mechanism of action as a negative regulator of muscle growth and differentiation in these pathological conditions. The main physiological properties and clinical significance are highlighted. Exogenous and endogenous factors regulating myostatin expression and possible mechanisms of their action are considered.

Quantitative analysis of aldosterone's role in potassium regulation

1988 ◽  
Vol 255 (5) ◽  
pp. F811-F822 ◽  
Author(s):  
D. B. Young
Keyword(s):  
Quantitative Analysis ◽  
Renal Excretion ◽  
Potassium Concentration ◽  
Physiological Role ◽  
Plasma Potassium ◽  
The Body ◽  
Pharmacological Interventions ◽  
Pathological Conditions ◽  
Potassium Regulation

Aldosterone is part of a complex system that regulates plasma potassium concentration by affecting the renal excretion of the ion as well as its distribution within the body. Because there are other components of the system, it has been difficult to determine the physiological significance of aldosterone in potassium regulation by attempting to study the hormone's effects in isolation. In this presentation a quantitative analysis of the potassium control system is used to provide information concerning the physiological role of aldosterone in potassium regulation under normal and pathological conditions, as well as during pharmacological interventions.

Pharmacology of Small- and Intermediate-Conductance Calcium-Activated Potassium Channels

2020 ◽  
Vol 60 (1) ◽  
pp. 219-240 ◽  
Author(s):  
Brandon M. Brown ◽  
Heesung Shim ◽  
Palle Christophersen ◽  
Heike Wulff
Keyword(s):  
Small Molecule ◽  
Binding Sites ◽  
Physiological Role ◽  
Membrane Hyperpolarization ◽  
Multiple Binding Sites ◽  
Multiple Binding ◽  
Calcium Activated Potassium Channels ◽  
Small Conductance ◽  
Made In

The three small-conductance calcium-activated potassium (KCa2) channels and the related intermediate-conductance KCa3.1 channel are voltage-independent K+ channels that mediate calcium-induced membrane hyperpolarization. When intracellular calcium increases in the channel vicinity, it calcifies the flexible N lobe of the channel-bound calmodulin, which then swings over to the S4-S5 linker and opens the channel. KCa2 and KCa3.1 channels are highly druggable and offer multiple binding sites for venom peptides and small-molecule blockers as well as for positive- and negative-gating modulators. In this review, we briefly summarize the physiological role of KCa channels and then discuss the pharmacophores and the mechanism of action of the most commonly used peptidic and small-molecule KCa2 and KCa3.1 modulators. Finally, we describe the progress that has been made in advancing KCa3.1 blockers and KCa2.2 negative- and positive-gating modulators toward the clinic for neurological and cardiovascular diseases and discuss the remaining challenges.

scholarly journals Towards Academic Drug Development Guidelines

2019 ◽  
Author(s):  
Christopher Southan
Keyword(s):  
Drug Development ◽  
Success Rate ◽  
Case Studies ◽  
Small Molecule ◽  
Research Productivity ◽  
Medicinal Chemistry ◽  
Academic Development ◽  
Commercial Development ◽  
Small Molecule Drug

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.

scholarly journals Mitochondrial Ferritin: Its Role in Physiological and Pathological Conditions

Cells ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1969
Author(s):  
Sonia Levi ◽  
Maddalena Ripamonti ◽  
Marko Dardi ◽  
Anna Cozzi ◽  
Paolo Santambrogio
Keyword(s):  
Physiological Condition ◽  
Physiological Role ◽  
Biochemical Properties ◽  
Cross Reactivity ◽  
Pathological Conditions ◽  
Human Ferritin ◽  
Ferritin Gene ◽  
New Type ◽  
Very High

In 2001, a new type of human ferritin was identified by searching for homologous sequences to H-ferritin in the human genome. After the demonstration that this ferritin is located specifically in the mitochondrion, it was called mitochondrial ferritin. Studies on the properties of this new type of ferritin have been limited by its very high homology with the cytosolic H-ferritin, which is expressed at higher levels in cells. This great similarity made it difficult to obtain specific antibodies against the mitochondrial ferritin devoid of cross-reactivity with cytosolic ferritin. Thus, the knowledge of the physiological role of mitochondrial ferritin is still incomplete despite 20 years of research. In this review, we summarize the literature on mitochondrial ferritin expression regulation and its physical and biochemical properties, with particular attention paid to the differences with cytosolic ferritin and its role in physiological condition. Until now, there has been no evidence that the alteration of the mitochondrial ferritin gene is causative of any disorder; however, the identified association of the mitochondrial ferritin with some disorders is discussed.

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