Current Molecular Pharmacology - Volume 14, Issue 4, 2021

Background: Allosteric modulators of G-protein coupled receptors regulate receptor activity by binding to sites other than the active site and have emerged as a new and highly desirable class of drugs. PAOPA (3(R)-[(2(S)-pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide), a peptidomimetic analog of L-prolyl-L-leucyl-glycinamide, is a potent dopamine D2 receptor allosteric modulator. PAOPA has shown therap Read More

Background: Piperine is a key bioactive alkaloid found in plants of piperaceae family. The compound possesses various medicinal and pharmacological activities (cholesterol-lowering, anti-cancer, Alzheimer’s disease etc.). Owing to its various target receptors (TRPV1, P-gp, CYP3A4 etc.) and several mechanisms, piperine has been studied as bio-enhancer for other drugs and its role has been evidenced in the literatu Read More

A chronic metabolic disease, diabetes mellitus (DM), is associated with various comorbidities that considerably decrease the quality of life. Sodium glucose linked transporter 2 (SGLT2) receptors are mainly situated in the proximal tubule of nephron. About 90% of glucose concentration is reabsorbed by these receptors in the nephron. The advanced remedy for the management of DM is sodium glucose co-transporter 2 in Read More

Understanding organogenesis, disorders, and repairing processes is particularly important for understanding the disease occurrence and developing treatment approaches. At present, liver- related studies are mainly conducted using in vivo models and cell lines, making it difficult to generalize the full picture of the structural characteristics and functions of human organs. Organoid is a three-dimensional (3D) culture Read More

Coronavirus disease 2019 (COVID-19) is caused by Severe Acute Respiratory Syndrome Coronaviruses 2 (SARS-CoV-2). At present, it is a potentially fatal disease and is of great global public health concern. The pathophysiological understanding of the mode of transmission of COVID-9 and the possible molecular targets are exploring successively to fight against this contagious disease. In this pandemic situation, a large number Read More

Renal Carcinoma (RC) is the ninth most prevalent cancer in men. Advancements in high- throughput technology have begun to scratch the surface of the complex landscape of renal cancer. Development, progression, invasion and metastasis are the key mechanism modulated by the microRNAs (miRNAs). Recent pieces of evidence have delineated the role of these micro steering wheels in the regulation of vital proces Read More

Protein kinase B (AKT) PI3K / AKT / mTOR signaling pathways play a crucial role in modulating cell survival, proliferation, metastasis, metabolism, angiogenesis, and apoptosis. The AKT family consists of three isoforms: AKT1, AKT2, and AKT3. Moreover, it has high sequence homology in the kinase domain and has similar substrate specificity to other members of AGC protein kinase. Recent studies have shown that AKT signals Read More

Ischemia/reperfusion (I/R) injury is a serious pathologic event that occurs due to restriction in blood supply to an organ, followed by hypoxia. This condition leads to enhanced levels of pro-inflammatory cytokines such as IL-6 and TNF-α, and stimulation of oxidative stress via enhancing reactive oxygen species (ROS) levels. Upon reperfusion, blood supply incz reases, but it deteriorates condition and leads to the generation of RO Read More

Prostate cancer (PCa) is the second most prevalent cancer and the fifth leading cause of cancer-related deaths among men. Androgen deprivation therapy (ADT) is the most frequently used therapeutic strategy in PCa; however, the development of resistance to ADT, known as castration- resistant prostate cancer (CRPC), continues to be a major obstacle against the successful treatment of PCa. The abnormal activation of Read More

Background: Valproic acid (VPA) is an HDAC inhibitor (HDACI) with an anticancer activity, but is hepatotoxic. N-(2-hydroxyphenyl)-2-propylpentanamide (o-OH-VPA) is a VPA aryl derivative designed in silico as a selective inhibitor of HDAC8 with biological properties against HeLa, rhabdomyosarcoma and breast cancer cell cultures. Objective: We studied the epigenetic mechanism of o-OH-VPA as an HDACI and eva Read More

Background: While our previous research has demonstrated that the NLRP3 inflammasome is involved in epilepsy progression, the effects of the specific NLRP3 inhibitor CY-09 remain poorly understood. Therefore, the aim of the present study was to investigate the efficacy of CY-09 against pentylenetetrazole (PTZ)-induced neuronal loss in mice. Methods: The expressions of the proinflammatory factors interleukin-1β and int Read More

Objective: The study aimed to investigate the effects of quercetin on Aquaporin 1 (AQP1) translocation in high glucose condition and made an attempt to clarify the underlying mechanisms and provide new ideas for the treatment of diabetic cataract (DC). Methods: The human lens epithelial line SRA01/04 cells were divided into groups mentioned below: normal glucose, high glucose with a specific time (0 h, 2 h, 4 h, Read More

Background: Buprenorphine (BUP), a “synthetic derivative of the opioid alkaloid thebaine”, may be associated with cellular damage in the central nervous system. Aims: This study was designed to investigate the effects of low and high doses of BUP on oxidative and inflammatory indices in the hippocampus and learning and memory behavior in an animal model. Objective: The association between BUP administration and oxidat Read More

Background: Earlier diagnosis and advances in treatment strategies have increased the average survival of cancer patients over the last decades. Despite the increased number of new anti- neoplastic agents, there has been no adequate therapy for intricate malignancies, such as pancreatic cancer. Cancer metabolism is the main building block standing behind cancer promotion and progression, even in the presence of a har Read More

Background: Anti-cancer effect of lapachol contained in Tabebuia avellandae has been poorly understood until now. Objective: The aim of this study was to investigate the inhibitory effect of lapachol on MMPs related to cell invasion. Its action mechanism was elucidated by analyzing the activity and the expression of MMPs and the proteins involved in the signaling pathway of cell invasion. Methods: The cytotoxicity of lapachol wa Read More

Background: Crocin is a known compound with the antioxidant and anti-inflammatory properties which may help to reduce the progression of neurological disorders. In this study, we aimed to investigate the protective effects of crocin on beta-amyloid peptide Aβ (1-40) and hydrogen peroxide (H2O2) induced neurotoxicity in PC12 cells. Methods: PC12 cells were pretreated with crocin and donepezil (5 and 10 μM) for 2 Read More

Background and Aim: Cisplatin (cis-diamminedichloroplatinum [II]; CDDP) is the most widely used drug in cancer chemotherapy. The nephrotoxicity of CDDP is one of its major side effects. Vorinostat (VST) has been reported to have antioxidant and anti-inflammatory effects in bothin-vitro and in vivo models. The present study aimed to explore the potential protective effects of VST against CDDP-induced nephrotoxicity in rats. Ma Read More

Background: Spinal cord injury (SCI), often characterized by sensory-motor dysfunction, is a major debilitating disorder of the central nervous system. As no useful treatment for post- SCI complications has been approved thus far, finding novel treatments is of great importance. Objective: Considering the promising effects of melatonin (MEL) against destructive mechanisms in other models of brain damage, in the current st Read More

Background: Rhinitis medicamentosa, also known as ‘rebound congestion,’ is inflammation of the nasal mucosa caused by the overuse of topical nasal decongestants. Although local decongestants resolve the initial nasal obstruction, the overuse causes rebound obstruction. However, how the overuse of the decongestant causes rhinitis medicamentosa is not known. Objectives: Here, we show the intracellular effects of oxymet Read More

Background: Cell adhesion, as dynamic interactions between cell-cell and cell-matrix, has an essential role in cancer cell migration. Integrins as cell membrane receptors are involved in cell adhesion and signal transduction. Aberrant expression of integrins is associated with the cancer cell adhesion. Objective: Targeting the process of cell adhesion and migration could be helpful to prevent cancer cell metastasis. Amygdalin i Read More