scholarly journals JAK‐inhibitors in dermatology – small molecules, big impact? Overview of the mechanism of action, previous study results and potential adverse effects

2021 ◽  
Author(s):  
Benjamin Klein ◽  
Regina Treudler ◽  
Jan C. Simon
Keyword(s):  
Adverse Effects ◽  
Small Molecules ◽  
Mechanism Of Action ◽  
Jak Inhibitors ◽  
Study Results

Thrombosis in IBD in the Era of JAK Inhibition

2020 ◽  
Vol 22 (1) ◽  
pp. 126-136
Author(s):  
Virginia Solitano ◽  
Gionata Fiorino ◽  
Ferdinando D’Amico ◽  
Laurent Peyrin-Biroulet ◽  
Silvio Danese
Keyword(s):  
Small Molecules ◽  
Arterial Thrombosis ◽  
Protective Role ◽  
Jak Inhibitors ◽  
Thrombotic Risk ◽  
Increased Risk ◽  
Bowel Diseases ◽  
Thrombotic Complications ◽  
Inflammatory Bowel ◽  
Inflammatory Effect

: Patients with inflammatory bowel diseases (IBD) have an increased risk of thrombosis. The interaction between inflammation and coagulation has been extensively studied. It is well-known that some drugs can influence the haemostatic system, but several concerns on the association between therapies and increased risk of thrombosis remain open. While biologics seem to have a protective role against thrombosis via their anti-inflammatory effect, some concerns about an increased risk of thrombosis with JAK inhibitors have been raised. We conducted a literature review to assess the association between biologics/small molecules and venous/arterial thrombotic complications. An increased risk of venous and arterial thrombosis was found in patients treated with corticosteroids, whereas anti-TNF were considered protective agents. No thromboembolic adverse event was reported with vedolizumab and ustekinumab. In addition, thromboembolic events rarely occurred in patients with ulcerative colitis (UC) after therapy with tofacitinib. The overall risk of both venous and arterial thrombosis was not increased based on the available evidence. Finally, in the era of JAK inhibitors, treatment should be individualized by evaluating the pre-existing potential thrombotic risk balanced with the intrinsic risk of the medication used.

scholarly journals Techniques to Study Inflammasome Activation and Inhibition by Small Molecules

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1704
Author(s):  
Diego Angosto-Bazarra ◽  
Cristina Molina-López ◽  
Alejandro Peñín-Franch ◽  
Laura Hurtado-Navarro ◽  
Pablo Pelegrín
Keyword(s):  
Inflammatory Response ◽  
Small Molecules ◽  
Mechanism Of Action ◽  
Inflammatory Diseases ◽  
Inflammasome Activation ◽  
Chronic Inflammatory Diseases ◽  
Anti Inflammatory ◽  
Inhibitory Molecules ◽  
Inflammasome Inhibitors

Inflammasomes are immune cytosolic oligomers involved in the initiation and progression of multiple pathologies and diseases. The tight regulation of these immune sensors is necessary to control an optimal inflammatory response and recover organism homeostasis. Prolonged activation of inflammasomes result in the development of chronic inflammatory diseases, and the use of small drug-like inhibitory molecules are emerging as promising anti-inflammatory therapies. Different aspects have to be taken in consideration when designing inflammasome inhibitors. This review summarizes the different techniques that can be used to study the mechanism of action of potential inflammasome inhibitory molecules.

scholarly journals Ru(II)-Dppz Derivatives and Their Interactions with DNA: Thirty Years and Counting

2021 ◽  
Vol 11 (7) ◽  
pp. 3038
Author(s):  
Maria Letizia Di Pietro ◽  
Giuseppina La Ganga ◽  
Francesco Nastasi ◽  
Fausto Puntoriero
Keyword(s):  
Transition Metal ◽  
Metal Complexes ◽  
Small Molecules ◽  
Transition Metal Complexes ◽  
Mechanism Of Action ◽  
Spectroscopic Techniques ◽  
Biological Applications ◽  
Ancillary Ligands ◽  
Structural Modifications ◽  
Over Time

Transition metal complexes with dppz-type ligands (dppz = dipyrido[3,2-a:2′,3′-c]phenazine) are extensively studied and attract a considerable amount of attention, becoming, from the very beginning and increasingly over time, a powerful tool for investigating the structure of the DNA helix. In particular, [Ru(bpy)2(dppz)]2+ and [Ru(phen)2(dppz)]2+ and their derivatives were extensively investigated as DNA light-switches. The purpose of this mini-review, which is not and could not be exhaustive, was to first introduce DNA and its importance at a biological level and research in the field of small molecules that are capable of interacting with it, in all its forms. A brief overview is given of the results obtained on the Ru-dppz complexes that bind to DNA. The mechanism of the light-switch active in this type of species is also briefly introduced along with its effects on structural modifications on both the dppz ligand and the ancillary ligands. Finally, a brief mention is made of biological applications and the developments obtained due to new spectroscopic techniques, both for understanding the mechanism of action and for cellular imaging applications.

Application of Cis-Diamminedichloro-Platinum in Combination Antineoplastic Therapy of Testicular Cancer

1978 ◽  
Vol 12 (4) ◽  
pp. 226-229 ◽  
Author(s):  
Janice M. Williams ◽  
Nicholas G. Popovich
Keyword(s):  
Adverse Effects ◽  
Testicular Cancer ◽  
Antineoplastic Therapy ◽  
Mechanism Of Action ◽  
Combination Chemotherapy ◽  
Clinical Use ◽  
Adult Males ◽  
Testicular Carcinoma ◽  
Dosage Administration

Testicular carcinoma is a leading cause of cancer-related deaths in adult males between the ages of 20 and 35. Cis-Diamminedichloroplatinum (II) (i.e., CDDP) is currently being used investigatively in combination chemotherapy for the treatment of this disease. This article reviews the literature to date on CDDP and its application in testicular cancer. Individual CDDP parameters (e.g., chemistry, mechanism of action, effectiveness and clinical use, adverse effects, dosage, administration and distribution) are discussed.

Ecotoxicity Effects of Nanomaterials on Aquatic Organisms

2016 ◽  
pp. 330-351 ◽  
Author(s):  
César A Barbero ◽  
Edith Inés Yslas
Keyword(s):  
Adverse Effects ◽  
Surface Charge ◽  
Direct Effect ◽  
Mechanism Of Action ◽  
Aquatic Environment ◽  
Physicochemical Characteristic ◽  
Aquatic Organisms ◽  
Development Stage ◽  
Engineered Nanomaterials ◽  
Toxicity Data

The increasing production and use of engineered nanomaterials raise concerns about inadvertent exposure and the potential for adverse effects on the aquatic environment. The aim of this chapter is focused on studies of nanotoxicity in different models of aquatic organisms and their impact. Moreover, the chapter provides an overview of nanoparticles, their applications, and the potential nanoparticle-induced toxicity in aquatic organisms. The topics discussed in this chapter are the physicochemical characteristic of nanomaterials (size, aggregation, morphology, surface charge, reactivity, dissolution, etc.) and their influence on toxicity. Further, the text discusses the direct effect of nanomaterials on development stage (embryonic and adult) in aquatic organisms, the mechanism of action as well as the toxicity data of nanomaterials in different species.f action as well as the toxicity data of nanomaterials in different species.

Mineralocorticoid receptor antagonists

ESC CardioMed ◽  
2018 ◽  
pp. 167-173
Author(s):  
Faiez Zannad ◽  
João Pedro Ferreira
Keyword(s):  
Myocardial Infarction ◽  
Heart Failure ◽  
Adverse Effects ◽  
Beneficial Effect ◽  
Mechanism Of Action ◽  
Mineralocorticoid Receptor ◽  
Post Myocardial Infarction ◽  
Mineralocorticoid Receptor Antagonists ◽  
Receptor Antagonists ◽  
Clinical Syndromes

Hypertension, post-myocardial infarction, and heart failure are the cardiovascular clinical syndromes where mineralocorticoid receptor antagonists (MRAs) have shown a beneficial effect. Most guidelines while recommending a MRA do not make a clear recommendation as to which MRA should be used, how doses should be titrated, or which monitorization is indicated. This chapter provides an appraisal of the different types of MRA drugs and their pharmacological differences with respect to mechanism of action, pharmacokinetics, monitoring, adverse effects, and drug interactions.

scholarly journals Biochemical investigations of the mechanism of action of small molecules ZL006 and IC87201 as potential inhibitors of the nNOS-PDZ/PSD-95-PDZ interactions

2015 ◽  
Vol 5 (1) ◽  
Author(s):  
Anders Bach ◽  
Søren W. Pedersen ◽  
Liam A. Dorr ◽  
Gary Vallon ◽  
Isabelle Ripoche ◽  
...  
Keyword(s):  
Small Molecules ◽  
Mechanism Of Action ◽  
Potential Inhibitors

Calcineurin Inhibitors: A Novel Approach to Canine Atopic Dermatitis

2005 ◽  
Vol 41 (2) ◽  
pp. 92-97 ◽  
Author(s):  
Rosanna Marsella
Keyword(s):  
Atopic Dermatitis ◽  
Adverse Effects ◽  
Mechanism Of Action ◽  
Broad Spectrum ◽  
Skin Diseases ◽  
Calcineurin Inhibitors ◽  
Relevant Information ◽  
Novel Approach ◽  
Allergic Skin ◽  
Traditional Therapies

The introduction of calcineurin inhibitors represents a major addition to the armamentarium of drugs available to veterinary clinicians for the management of allergic skin diseases. Both cyclosporine and tacrolimus have been proven to be well tolerated and effective for the treatment of atopic dermatitis in dogs. Although broad spectrum in their mechanism of action, they lack the major adverse effects of glucocorticoids and provide an appealing alternative to traditional therapies. The purposes of this article are to review clinically relevant information regarding these agents and to provide tips for maximizing the benefit obtained from these therapies.

New Drug Review-Ezogabine (Potiga): Seizing the seizure

2011 ◽  
Vol 1 (6) ◽  
pp. 135-136
Author(s):  
Misty L. Gonzalez
Keyword(s):  
Clinical Trial ◽  
Adverse Effects ◽  
Drug Interactions ◽  
Drug Administration ◽  
Mechanism Of Action ◽  
New Drug ◽  
Clinical Trial Evidence ◽  
Clinically Significant ◽  
Trial Evidence ◽  
Drug Review

Ezogabine was approved by the Food and Drug Administration (FDA) in June of 2011. This article reviews clinically significant aspects of this new drug including: the FDA-approved indications, mechanism of action, administration, drug interactions, adverse effects, clinical trial evidence, innovative properties and place in therapy.

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