scholarly journals Discovery of Oxazolidinone-Based Heterocycles as Subtype Selective Sigma-2 Ligands

2021 ◽  
Author(s):  
Benjamin E Blass ◽  
Richie Rashmin Bhandare ◽  
Daniel J. Canney
Keyword(s):  
Therapeutic Target ◽  
Amyloid Plaques ◽  
Therapeutic Options ◽  
Potential Therapeutic Target ◽  
Root Cause ◽  
Amyloid Hypothesis ◽  
Medical Need ◽  
The Us ◽  
Subtype Selective ◽  
The Brain

Abstract Alzheimer’s disease is a major, unmet medical need that impacts 6 million people in the US alone. Therapeutic options are limited, and the root cause of this condition remains unclear. The Amyloid Hypothesis has been proposed as a means of explaining the formation of amyloid plaques in the brain of patient. The sigma-2 receptor was recently identified as a potential therapeutic target capable of arresting the formation of amyloid plaques. Herein, we report the identification of a series of novel, functionalized oxazolidin-2-ones sigma-2 ligands.

SET Protein in Cancer: A Potential Therapeutic Target

2021 ◽  
Vol 21 ◽  
Author(s):  
Xinjie Liang ◽  
Xuefei Bao ◽  
Guoliang Chen
Keyword(s):  
Drug Resistance ◽  
Clinical Trials ◽  
Cancer Therapy ◽  
Tumor Cells ◽  
Strong Correlation ◽  
Therapeutic Target ◽  
Poor Prognosis ◽  
Therapeutic Options ◽  
Potential Therapeutic Target ◽  
Bona Fide

: SET protein is a multi-functional oncoprotein that is ubiquitously expressed in most tumor cells. Dysregulation of SET has been associated with many types of cancer. Due to ever-accumulating evidence of its strong correlation with both poor prognosis and drug resistance, the targeting of SET is starting to be explored. SET is currently regarded as a potential target for cancer therapy, and several inhibitors are being developed for clinical trials. In this review, the physiological and pathological functions of SET, as well as its antagonists, will be discussed along with the prospects and challenges involved with translating SET inhibitors into bona fide therapeutic options.

Role of spinal neurons in the maintenance of elevated sympathetic activity: a novel therapeutic target?

2020 ◽  
Vol 319 (3) ◽  
pp. R282-R287
Author(s):  
Maycon I. O. Milanez ◽  
Erika E. Nishi ◽  
Cássia T. Bergamaschi ◽  
Ruy R. Campos
Keyword(s):  
Cardiovascular Diseases ◽  
Therapeutic Target ◽  
Sympathetic Activity ◽  
Spinal Neurons ◽  
Potential Therapeutic Target ◽  
Present Evidence ◽  
Extensive Range ◽  
Vasomotor Activity ◽  
The Brain

The control of sympathetic vasomotor activity involves a complex network within the brain and spinal circuits. An extensive range of studies has indicated that sympathoexcitation is a common feature in several cardiovascular diseases and that strategies to reduce sympathetic vasomotor overactivity in such conditions can be beneficial. In the present mini-review, we present evidence supporting the spinal cord as a potential therapeutic target to mitigate sympathetic vasomotor overactivity in cardiovascular diseases, focusing mainly on the actions of spinal angiotensin II on the control of sympathetic preganglionic neuronal activity.

Changes in the Brain Extracellular Matrix Composition in schizophrenia: A Pathophysiological Dysregulation and a Potential Therapeutic Target

2021 ◽  
Author(s):  
Daniela Rodrigues-Amorim ◽  
Tania Rivera-Baltanás ◽  
Patricia Fernández-Palleiro ◽  
Marta Iglesias-Martínez-Almeida ◽  
Luis Freiría-Martínez ◽  
...  
Keyword(s):  
Extracellular Matrix ◽  
Therapeutic Target ◽  
Matrix Composition ◽  
Potential Therapeutic Target ◽  
The Brain ◽  
Brain Extracellular Matrix

scholarly journals ABCC9/SUR2 in the brain: Implications for hippocampal sclerosis of aging and a potential therapeutic target

2015 ◽  
Vol 24 ◽  
pp. 111-125 ◽  
Author(s):  
Peter T. Nelson ◽  
Gregory A. Jicha ◽  
Wang-Xia Wang ◽  
Eseosa Ighodaro ◽  
Sergey Artiushin ◽  
...  
Keyword(s):  
Therapeutic Target ◽  
Hippocampal Sclerosis ◽  
Potential Therapeutic Target ◽  
The Brain

scholarly journals RALGPS1 is over-expressed in brain metastatic breast cancer.

2020 ◽  
Author(s):  
Shahan Mamoor
Keyword(s):  
Breast Cancer ◽  
Metastatic Breast Cancer ◽  
Brain Metastasis ◽  
Brain Metastases ◽  
Microarray Data ◽  
Therapeutic Target ◽  
Metastatic Breast ◽  
Clinical Problem ◽  
Potential Therapeutic Target ◽  
The Brain

Brain metastases are a clinical problem in patients with breast cancer (1-3). We mined published microarray data (4, 5) to discover genes associated with brain metastasis in patients with brain metastatic breast cancer. We found that RALGPS1 was among the genes most differentially expressed in the brain metastases of patients with brain metastatic breast cancer. RALGPS1 may be of relevance to the biology underlying metastasis to the brain, and it may be of relevance as a potential therapeutic target in patients with intractable disease.

The US Expert Panel on the Appropriate Use Recommendations of Aducanumab in Clinical Practice

2021 ◽  
pp. 1-1
Author(s):  
S. Gauthier ◽  
P. Rosa-Neto
Keyword(s):  
Clinical Practice ◽  
Expert Panel ◽  
Amyloid Plaques ◽  
Public Domain ◽  
Phase Iii ◽  
Appropriate Use ◽  
The Public ◽  
New Class ◽  
The Us ◽  
The Brain

The authors of these recommendations must be congratulated on rapidly putting together a workable set of guidelines on the best use in clinical practice of the first drug approved (1) in a new class of medications acting on the excessive deposition of amyloid plaques in the brain of persons with early symptoms of Alzheimer’s disease (AD). These guidelines have been written despite the current lack of peer-reviewed publications about the Phase III pivotal studies so changes may be required once all the data is available in the public domain (2, 3, 4).

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