Current Medicinal Chemistry - Volume 28, Issue 42, 2021

This review summarizes key literature defining the phenotypes of individual class IIa HDAC proteins and compounds that selectively target their enzymatic catalytic domain (CD). The focus is on the effects of class IIa HDACs in physiological and pathological conditions, both in vitro and in vivo, and on their mode of action in regulating genes, upstream proteins and signaling pathways. Phenotype studies further demonstrate eith Read More

Nonactic acid, which is a macrocyclic nonactin subunit, contains four asymmetric centers and has the molecular formula of C10H18O3. Due to their various biological activities and challenging structural characteristics, nonactic acid and its derivatives have attracted much attention from scientists since 1955. These compounds possess significant antibacterial, insecticidal and acaricidal activities, as well as a promoting eff Read More

Hydrogels are hydrophilic but water-soluble polymer systems with a three-dimensional network structure. They can absorb large amounts of water and maintain their shape and remain soft. The high-moisturizing properties, good biocompatibility, and controlled biodegradability of hydrogels have allowed them to be widely used in wound dressing, tissue engineering, controlled drug delivery systems, and other fields. This articl Read More

Lipid-based formulations have recently been investigated as a promising approach to enhance the bioavailability of drugs, especially poorly water-soluble drugs. The encapsulation of lipid-based formulations in porous materials can result in a transformation of liquids or semisolid forms to solid dosage forms. Moreover, the specific structure of porous carriers could offer an enhanced ability to load and control active pharmaceuti Read More

Background: Growing evidence indicates that miRs have critical activities in adjusting cellular processes, e.g., cell death, proliferation, and cell-cycle. Introduction: This study aimed to provide a concise review of the recent findings regarding tumoral miRs and the cross-talk between miRs and epigenetic factors. Results: Like the protein-coding genes, the expression levels of miRs are mediated by various transcriptional net Read More

An important group of antiemetic drugs used in the treatment of nausea and vomiting after chemotherapy containing an indole moiety in their structures, working as 5- hydroxytryptamine type 3 serotonin receptor antagonist (5-HT3). This study focuses on compounds bearing an indole core that present a 5-HT3 receptor antagonist activity, which have been successfully used as antiemetic drugs for reducing chemotherapy ad Read More

Background: Endometrial cancer is the fourth most common malignancy in female population worldwide. It was estimated that 65,620 new cases and 12.590 subsequent deaths occurred in 2020 in the United States. Patients with type II and advanced endometrial cancer do not respond well to the current treatments. Therefore, endometrial cancer should be better understood in order to develop more effective treatments. Obje Read More

As cancer continues to be one of the leading causes of death, various cancer treatments are being developed from traditional surgery to the more recent emergence of target therapy. However, therapy resistance is a restricting problem that needs to be overcome. Henceforth, the field of research shifts to new plausible drug targets, among which is the ubiquitin-proteasome system. This review is focused on the ubiquitin c Read More

Background: Experimental evidence has shown that lncRNA MALAT1 is related to proliferation ability, invasion and migration ability, autophagy ability, and chemoresistance in gastric cancer. Moreover, MALAT1 is related to metastasis and patient prognosis in gastric cancer. This review aims to reveal the biological functions and specific mechanisms of MALAT1 in gastric cancer. Methods: After a comprehensive and systematic Read More

Diabetic nephropathy (DN) is one of the most common complications of diabetes and the main cause of end-stage renal disease (ESRD). The inflammatory response plays a key role in the pathological process of DN. As the most deeply studied inflammasome, NLRP3 should not be overlooked in DN. Its abnormal activation accelerates DN progression. In this review, we summarize our understanding of the structural Read More