Expression and Function of Transient Receptor Potential Ankyrin 1 Ion Channels in the Caudal Nucleus of the Solitary Tract (open access)

Expression and Function of Transient Receptor Potential Ankyrin 1 Ion Channels in the Caudal Nucleus of the Solitary Tract

The article describes a study that tested and confirmed the hypothesis that TRPA1 expressed in the primary sensory afferents may modulate the function of second order NTS neurons. The expression of TRPA1 was detected in presynaptic locations, but not the somata of caudal NTS neurons that did not express TRPA1 mRNA or proteins. Moreover, caudal NTS neurons did not show somatodendritic responsiveness to TRPA1 agonists, while TRPA1 immunostaining was detected only in the afferent fibers.
Date: April 26, 2019
Creator: Feng, Lin; Uteshev, Victor V. & Premkumar, Louis S.
System: The UNT Digital Library
A Novel Prodrug Approach for Central Nervous System-Selective Estrogen Therapy (open access)

A Novel Prodrug Approach for Central Nervous System-Selective Estrogen Therapy

This article gives an overview of the discovery of small-molecule bioprecursor prodrugs carrying the para-quinol scaffold on the steroidal A-ring that are preferentially metabolized in the CNS to the corresponding estrogens. Selected examples are shown to illustrate that, independently of the route of administrations and duration of treatments, these agents produce high concentration of estrogens only in the CNS without peripheral hormonal liability. 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED) has been the best-studied representative of this novel type of prodrugs for brain and retina health. Specific applications in preclinical animal models of centrally-regulated and estrogen-responsive human diseases, including neurodegeneration, menopausal symptoms, cognitive decline and depression, are discussed to demonstrate the translational potential of their prodrug approach for CNS-selective and gender-independent estrogen therapy with inherent therapeutic safety.
Date: November 19, 2019
Creator: Prokai-Tatrai, Katalin & Prókai, László, 1958-
System: The UNT Digital Library
Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach (open access)

Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach

Using thyrotropin-releasing hormone (TRH) as a model, paper explores whether synergistic combination of lipoamino acid(s) and a linker cleaved by prolyl oligopeptidase (POP) can be used as a promoiety for prodrug design for the preferential brain delivery of the peptide.
Date: July 18, 2019
Creator: Prokai-Tatrai, Katalin; De La Cruz, Daniel L.; Nguyen, Vien; Ross, Benjamin P.; Toth, Istvan & Prókai, László, 1958-
System: The UNT Digital Library
HIV-1 Impairment via UBE3A and HIV-1 Nef Interactions Utilizing the Ubiquitin Proteasome System (open access)

HIV-1 Impairment via UBE3A and HIV-1 Nef Interactions Utilizing the Ubiquitin Proteasome System

Study examines the interaction between a key pathogenic HIV-1 viral protein, Nef, and ubiquitin (Ub)-protein ligase E3A (UBE3A).
Date: November 27, 2019
Creator: Pyeon, Dohun; Rojas, Vivian K.; Price, Lenore; Kim, Seongcheol; Singh, Meharvan & Park, In-Woo
System: The UNT Digital Library
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5 (open access)

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5

The article is part of a series of Editorials published biannually that highlights a number of recently published articles that describe crucial findings.
Date: June 30, 2019
Creator: Mangoni, Arduino A; Vanden Eynde, Jean Jacques; Jampilek, Josef; Hadjipavlou-Litina, Dimitra; Liu, Hong; Reynisson, Jóhannes et al.
System: The UNT Digital Library