scholarly journals Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Ying Chen ◽  
Ruya You ◽  
Ke Wang ◽  
Yousheng Wang

Human urate anion transporter 1 (hURAT1) is responsible for the reabsorption of uric acid in the proximal renal tubules and is a promising therapeutic target for treating hyperuricemia. To mitigate the side effects of URAT1-targeted clinical agents such as benzbromarone, there is significant interest in discovering new URAT1 inhibitors and developing technology that can evaluate URAT1 inhibition. This review summarizes the methods for assay of URAT1 inhibition and the progress on the discovery of natural and synthetic URAT1 inhibitors in the past five years.

GYNECOLOGY ◽  
2019 ◽  
Vol 21 (3) ◽  
pp. 6-8
Author(s):  
Vera N Prilepskaya

This article presents information about modern principles of diagnosis and treatment of HPV-associated diseases. Behind cervical cancer morbidity and mortality rates over the past 10 years increase significantly. Examination and observation of patients with human papillomavirus persistence of highly oncogenic types is important a link in cancer prevention. The article presents diagnostic methods, treatment of cervical diseases, as well as the possibility of pharmacotherapy in HPV-associated diseases.


Author(s):  
Valery Ray

Abstract Gas Assisted Etching (GAE) is the enabling technology for High Aspect Ratio (HAR) circuit access via milling in Focused Ion Beam (FIB) circuit modification. Metal interconnect layers of microelectronic Integrated Circuits (ICs) are separated by Inter-Layer Dielectric (ILD) materials, therefore HAR vias are typically milled in dielectrics. Most of the etching precursor gases presently available for GAE of dielectrics on commercial FIB systems, such as XeF2, Cl2, etc., are also effective etch enhancers for either Si, or/and some of the metals used in ICs. Therefore use of these precursors for via milling in dielectrics may lead to unwanted side effects, especially in a backside circuit edit approach. Making contacts to the polysilicon lines with traditional GAE precursors could also be difficult, if not impossible. Some of these precursors have a tendency to produce isotropic vias, especially in Si. It has been proposed in the past to use fluorocarbon gases as precursors for the FIB milling of dielectrics. Preliminary experimental evaluation of Trifluoroacetic (Perfluoroacetic) Acid (TFA, CF3COOH) as a possible etching precursor for the HAR via milling in the application to FIB modification of ICs demonstrated that highly enhanced anisotropic milling of SiO2 in HAR vias is possible. A via with 9:1 aspect ratio was milled with accurate endpoint on Si and without apparent damage to the underlying Si substrate.


2019 ◽  
Vol 32 (2) ◽  
pp. 108-110 ◽  
Author(s):  
E. Besserer-Offroy ◽  
P. Sarret

In the past few years, several biased ligands acting at the mu-opioid receptor were reported in the literature. These agonists are aimed at reducing pain while having fewer side effects than morphine, the gold standard of opioid analgesics. In this mini-review, we describe and discuss the recent advances in mu-biased ligands actually in preclinical and clinical development stages, including the latest U.S. Food and Drug Administration review of oliceridine, a biased mu-agonist for moderate to severe acute pain treatment developed by the company Trevena.


2019 ◽  
Author(s):  
Silvia Scaricamazza ◽  
Illari Salvatori ◽  
Giacomo Giacovazzo ◽  
Jean Philippe Loeffler ◽  
Frederique Renè ◽  
...  

2019 ◽  
Vol 20 (12) ◽  
pp. 1217-1226 ◽  
Author(s):  
Arunaksharan Narayanankutty

Background: Phosphoinositide 3-kinase (PI3Ks) is a member of intracellular lipid kinases and involved in the regulation of cellular proliferation, differentiation and survival. Overexpression of the PI3K/Akt/mTOR signalling has been reported in various forms of cancers, especially in colorectal cancers (CRC). Due to their significant roles in the initiation and progression events of colorectal cancer, they are recognized as a striking therapeutic target. Objective: The present review is aimed to provide a detailed outline on the role of PI3K/Akt/mTOR pathway in the initiation and progression events of colorectal cancers as well as its function in drug resistance. Further, the role of PI3K/Akt/mTOR inhibitors alone and in combination with other chemotherapeutic drugs, in alleviating colorectal cancer is also discussed. The review contains preclinical and clinical evidence as well as patent literature of the pathway inhibitors which are natural and synthetic in origin. Methods: The data were obtained from PubMed/Medline databases, Scopus and Google patent literature. Results: PI3K/Akt/mTOR signalling is an important event in colorectal carcinogenesis. In addition, it plays significant roles in acquiring drug resistance as well as metastatic initiation events of CRCs. Several small molecules of natural and synthetic origin have been found to be potent inhibitors of CRCs by effectively downregulating the pathway. Data from various clinical studies also support these pathway inhibitors and several among them are patented. Conclusion: Inhibitors of the PI3K/mTOR pathway have been successful for the treatment of primary and metastatic colorectal cancers, rendering the pathway as a promising clinical cancer therapeutic target.


2021 ◽  
Author(s):  
Johannes Burtscher ◽  
Muhammed Muazzam Kamil Syed ◽  
Hilal A. Lashuel ◽  
Grégoire P. Millet

1999 ◽  
Vol 5 (S2) ◽  
pp. 836-837
Author(s):  
R. Mitra ◽  
W.A. Chiou ◽  
A.Madan ◽  
R. Hoffman ◽  
J.R. Weertman

There has been a significant interest in the development of dispersion-hardened aluminum for many years for high specific strength and modulus. Such materials are usually processed by powder or ingot metallurgy routes. In this study, Al3 Ti dispersion hardened Al was obtained by annealing Al-Ti multilayers. Al-Ti multilayered films have been characterized in the past by observing the structure of the layers, as well as tensile properties and hardness. This paper reports the structure of Al-Ti multilayers and the evolution of matrix and dispersoid microstructure on annealing.The Al-Ti multilayered structures were prepared by magnetron sputtering using Al and Ti as targets and either Si (100) or NaCl as substrates. The bi-layer thickness was maintained around 16 nm with Ti constituting 12% of the total. The substrate was alternately moved below the Al and Ti targets for the purpose of deposition. The as-deposited film on the substrate and NaCl salts were annealed at 400°C for periods between 1 and 24 h in a vacuum (10−5 torr) furnace.


Author(s):  
Marco Spreafico ◽  
Alicja M. Gruszka ◽  
Debora Valli ◽  
Mara Mazzola ◽  
Gianluca Deflorian ◽  
...  

2014 ◽  
Vol 18 (4) ◽  
pp. 403-414 ◽  
Author(s):  
Shinya Matsuzaki ◽  
Satoshi Serada ◽  
Akiko Morimoto ◽  
Yutaka Ueda ◽  
Kiyoshi Yoshino ◽  
...  

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