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Topic Review
FAAH, MAGL, and DAGL in Obesity Treatment
The endocannabinoid system (ECS) plays an integral role in maintaining metabolic homeostasis and may affect hunger, caloric intake, and nutrient absorption. Obesity has been associated with higher levels of the endogenous cannabinoid transmitters (endocannabinoids). Therefore, the ECS is an important target in obesity treatment. Modulating the enzymes that synthesize and degrade endocannabinoids, namely fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and diacylglycerol lipase (DAGL), may be a promising strategy to treat obesity.
  • 1.1K
  • 18 Jan 2022
Topic Review
Nanomaterials Aiming to Tackle Antibiotic-Resistant Bacteria
The most important current issue related to human health is bacterial resistance against antibiotics. Prolonged treatment using antibiotics is required in multidrug-resistant conditions, along with debridement of tissue, but in a small number of cases, the high costs of healthcare and low patient compliance prevent this treatment from succeeding. The identical features of nanomaterials make them unique candidates and boost the efficacy against multi-drug-resistant bacterial infection. Nanomaterials execute different bactericidal actions, and therefore bacteria face difficulty against therapeutics due to nanomaterial morphology such as size, shape, and surface chemistry. Nanomaterials can penetrate the bacterial membrane with unique drug cargo. Therefore, nanomaterials may be helpful for treatment by improving the therapeutic efficacy through their interaction with the bacterial cell system.
  • 1.1K
  • 30 Mar 2022
Topic Review
NF-κB Pathway Inhibitors in Alzheimer’s Disease Treatment
The NF-κB family is a group of transcription factors that play a pivotal role in regulating various biological processes, including immune responses, inflammation, cell survival, and cellular differentiation. The involvement of the NF-κB pathway in immune system responses, inflammation, oxidative stress, and neuronal survival highlights its significance in Alzheimer’s disease (AD) progression.
  • 1.1K
  • 25 Sep 2023
Topic Review
Grimelysin and Protealysin
The entry reviews the discovery, properties, and functional activities of new bacterial enzymes, proteases grimelysin (ECP 32) of Serratia grimesii and protealysin of Serratia proteamaculans, characterized by both a highly specific “actinase” activity and their ability to stimulate bacterial invasion. Grimelysin cleaves the only one polypeptide bond Gly42-Val43 in actin. This bond is not cleaved by any other proteases and leads to a reversible loss of actin polymerization. Similar properties were characteristic for another bacterial protease, protealysin. These properties made grimelysin and protealysin a unique tool to study the functional properties of actin. Furthermore, bacteria Serratia spp. producing grimelysin/protealysin invade eukaryotic cells, and the recombinant Escherichia coli expressing the grimelysin or protealysins gene become invasive. Being an intracellular enzyme, grimelysin/protealysin can be delivered by bacteria to eukaryotic cells. These data indicate that the protease is a virulence factor, and actin can be a target for the protease upon its translocation into the host cell.
  • 1.1K
  • 27 Oct 2020
Topic Review
Ferulic Acid in Animal Models of Alzheimer’s Disease
Alzheimer’s disease (AD) is a neurodegenerative disease with a high incidence in the elderly. Many preclinical studies show that a natural product, ferulic acid (FA), displays neuroprotective effects in AD models. 
  • 1.1K
  • 27 Oct 2021
Topic Review
Aripiprazole Lauroxil
Aripiprazole lauroxil is a prodrug of aripiprazole and is administered as an intramuscular injection. Once administered, aripiprazole lauroxil is first converted to N-hydroxymethyl aripiprazole by enzyme-mediated hydrolysis and is hydrolyzed again to aripiprazole. Aripiprazole was originally reported to be a partial agonist at D2and 5HT1Areceptors, with a combination of antagonistic activity at 5HT2Areceptors.
  • 1.1K
  • 18 Jul 2021
Topic Review
In Silico Models to Predict Drug-Induced Liver Injury
Drug-induced liver injury (DILI) is a major cause of the withdrawal of pre-marketed drugs, typically attributed to oxidative stress, mitochondrial damage, disrupted bile acid homeostasis, and innate immune-related inflammation. DILI can be divided into intrinsic and idiosyncratic DILI with cholestatic liver injury as an important manifestation. The diagnosis of DILI remains a challenge today and relies on clinical judgment and knowledge of the insulting agent. Early prediction of hepatotoxicity is an important but still unfulfilled component of drug development. In response, in silico modeling has shown good potential to fill the missing puzzle. Computer algorithms, with machine learning and artificial intelligence as a representative, can be established to initiate a reaction on the given condition to predict DILI. 
  • 1.1K
  • 29 Dec 2022
Topic Review
Target antigens for Approved ADCs
Biologically-based therapies increasingly rely on the endocytic cycle of internalization and exocytosis of target receptors for cancer therapies. However, receptor trafficking pathways (endosomal sorting (recycling, lysosome localization) and lateral membrane movement) are often dysfunctional in cancer. Antibody-drug conjugates (ADCs) have revitalized the concept of targeted chemotherapy by coupling inhibitory antibodies to cytotoxic payloads. Significant advances in ADC technology and format, and target biology have hastened the FDA approval of nine ADCs (four since 2019). Although the links between aberrant endocytic machinery and cancer are emerging, the impact of dysregulated internalization processes of ADC targets and response rates or resistance have not been well studied. This is despite the reliance on ADC uptake and trafficking to lysosomes for linker cleavage and payload release. 
  • 1.1K
  • 21 Jul 2021
Topic Review
Cenobamate and Drug-Resistant Epilepsy
Cenobamate (CNB), ([(R)-1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl], is a novel tetrazole alkyl carbamate derivative. In November 2019, the Food and Drug Administration approved Xcopri®, marketed by SK Life Science Inc., (Paramus, NJ, USA) for adult focal seizures. The European Medicines Agency approved Ontozry® by Arvelle Therapeutics Netherlands B.V.(Amsterdam, The Neatherlands) in March 2021. Cenobamate is a medication that could potentially change the perspectives regarding the management and prognosis of refractory epilepsy.
  • 1.1K
  • 02 Aug 2023
Topic Review
1-C Metabolism in AML
One-carbon (1-C) metabolism is essential for numerous cancer cell functions, including protein and nucleic acid synthesis and maintaining cellular redox balance, and inhibition of the 1-C pathway has yielded several highly active drugs, such as methotrexate and 5-FU. 
  • 1.1K
  • 07 Jul 2021
Topic Review
COVID 19 BIBILOGRAPHIC DRUG DISCUSSIONS
In this type of note some Probable synthetic drugs both the Non Antiviral as well as Antiviral synthetic drugs servingagainst Covid19 commonly used under trial basis are taken into discussion .Starting from Hydroxy- Chloroquine sulphateto Remdesivir just some points are discussed only but the in detail study regarding Structure , SAR , Q –SAR ,Formulations Pharmacology / Bio-logical activities are available in the following BIBILOGRAPHIC discussions
  • 1.1K
  • 05 Nov 2020
Topic Review
Sustained Antiviral Ocular Drug Delivery
The eyes are the window to the world and the key to communication, but they are vulnerable to multitudes of ailments. More serious than is thought, corneal infection by herpes simplex viruses (HSVs) is a prevalent yet silent cause of blindness in both the paediatric and adult population, especially if immunodeficient. Globally, there are 1.5 million new cases and forty thousand visual impairment cases reported yearly. The Herpetic Eye Disease Study recommends topical antiviral as the front-line therapy for HSV keratitis. Ironically, topical eye solutions undergo rapid nasolacrimal clearance, which necessitates oral drugs but there is a catch of systemic toxicity. The hurdle of antiviral penetration to reach an effective concentration is further complicated by drugs’ poor permeability and complex layers of ocular barriers.
  • 1.1K
  • 02 Feb 2021
Topic Review
Treatment Advances in Sepsis and Septic Shock
Sepsis is defined as a life-threatening organ dysfunction caused by a dysregulated host response to infection, and it affects over 25 million people every year. Even more severe, septic shock is a subset of sepsis defined by persistent hypotension, and hospital mortality rates are higher than 40%. As new pathophysiological mechanisms have been uncovered, immunostimulatory therapy has emerged as a promising path forward. Highly investigated treatment strategies include cytokines and growth factors, immune checkpoint inhibitors, and even cellular therapies.
  • 1.1K
  • 04 May 2023
Topic Review
Diabetic Retinopathy Treatment
Diabetic retinopathy (DR) is one of the leading matters of vision-loss globally. Even though there have been extensive efforts to reduce vision loss, the prevalence of DR is still uprising. There are several pharmacological and surgical therapies currently used in clinics, but none of them has not been used as effective therapies at the early stage of DR.
  • 1.1K
  • 01 Nov 2021
Topic Review
Magnetic Molecularly Imprinted Polymers
The combination of molecular imprinting technology with magnetic nanoparticles provides a new class of smart hybrids, i.e., magnetic molecularly imprinted polymers (MMIPs) to overcome limitations in current cancer therapy. The application of these complexes is gaining more interest in therapy, due to their favorable properties, namely, the ability to be guided and to generate slight hyperthermia with an appropriate external magnetic field, alongside the high selectivity and loading capacity of imprinted polymers toward a template molecule. In cancer therapy, using the MMIPs as smart-drug-delivery robots can be a promising alternative to conventional direct administered chemotherapy, aiming to enhance drug accumulation/penetration into the tumors while fewer side effects on the other organs. 
  • 1.1K
  • 23 Sep 2020
Topic Review
Dabigatran in Alzheimer’s Disease
Alzheimer’s disease (AD) is caused by neurodegenerative, but also vascular and hemostatic changes in the brain. The oral thrombin inhibitor dabigatran, which has been used for over a decade in preventing thromboembolism and has a well-known pharmacokinetic, safety and antidote profile, can be an option to treat vascular dysfunction in early AD, a condition known as cerebral amyloid angiopathy (CAA). Dabigatran blocks soluble thrombin, thrombin-mediated formation of fibrin and amyloid-ß protein (Aβ)-containing fibrin clots. These clots are deposited in brain parenchyma and blood vessels in areas of CAA, leading to vascular and blood-brain barrier dysfunction, hypoperfusion and chronically reduced oxygen (hypoxia) and nutrient supply, mainly in hippocampal and neocortical brain areas. Dabigatran has the potential to preserve perfusion and oxygen delivery to the brain, and to prevent parenchymal Aß-, thrombin- and fibrin-triggered inflammatory and neurodegenerative processes, leading to synapse and neuron death, and cognitive decline. 
  • 1.1K
  • 06 Jul 2021
Topic Review
Unconventional Treatment of Biofilm Infection
Today, researchers are looking at new ways to treat severe infections caused by resistance to standard antibiotic therapy. This is quite challenging due to the complex and interdependent relationships involved: the cause of infection–the patient–antimicrobial agents. The sessile biofilm form is essential in research to reduce resistance to very severe infections (such as ESKAPE pathogens: Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanni, Pseudomonas aeruginosa, and Enterobacter spp). The purpose of this study is to elucidate the mechanisms of the occurrence, maintenance, and suppression of biofilm infections. One form of biofilm suppression is the efficient action of natural antagonists of bacteria—bacteriophages. Bacteriophages effectively penetrate the biofilm’s causative cells. They infect those bacterial cells and either destroy them or prevent the infection from spreading. In this process, bacteriophages are specific, relatively easy to apply, and harmless to the patient. Antimicrobial peptides (AMPs) support the mechanisms of bacteriophages’ action. AMPs could also attack and destroy infectious agents on their own (even on biofilm). AMPs are simple, universal peptide molecules, mainly cationic peptides. Additional AMP research could help develop even more effective treatments of biofilm (bacteriophages, antibiotics, AMPs, nanoparticles). This is a review of recent unconventional agents, such as bacteriophages and AMPs, used for the eradication of biofilm, providing an overview of potentially new biofilm treatment strategies.
  • 1.1K
  • 20 Oct 2020
Topic Review
Oral siRNA Delivery for Inflammatory Bowel Disease Treatments
RNA interference (RNAi) therapies have significant potential for the treatment of inflammatory bowel diseases (IBD). Oral nanomedicines carrying small interfering RNA (siRNA) drugs include the following two: (1) Polyplex or lipoplex. (2) Polyplex or lipoplex embedded in hydrogels or polymeric materials
  • 1.1K
  • 11 Oct 2022
Topic Review
Bone Mass Loss during Menopause
Antiosteoporotic Activity of Genistein Aglycone in Postmenopausal Women: Evidence from a Post-Hoc Analysis of a Multicenter Randomized Controlled Trial. Genistein has a preventive role against bone mass loss during menopause. However, experimental data in animal models of osteoporosis suggest an anti-osteoporotic potential for this isoflavone. We performed a post-hoc analysis of a previously published trial investigating the effects of genistein in postmenopausal women with low bone mineral density. The parent study was a randomized, double-blind, placebo-controlled trial involving postmenopausal women with a femoral neck (FN) density <0.795 g/cm². A cohort of the enrolled women was, in fact, identified at the baseline as osteoporotic (n = 121) on the basis of their T-score and analyzed thereafter for the 24 months' treatment with either 1000 mg of calcium and 800 IU vitamin D3 (placebo; n = 59); or calcium, vitamin D3, and Genistein aglycone (54 mg/day; genistein; n = 62). According to the femoral neck T-scores, 31.3% of the genistein and 30.9% of the placebo recipients were osteoporotic at baseline. In the placebo and genistein groups, the 10-year hip fracture probability risk assessed by Fracture Risk Assessment tool (FRAX) was 4.1 ± 1.9 (SD) and 4.2 ± 2.1 (SD), respectively. Mean bone mineral density (BMD) at the femoral neck increased from 0.62 g/cm² at baseline to 0.68 g/cm² at 1 year and 0.70 g/cm² at 2 years in genistein recipients, and decreased from 0.61 g/cm² at baseline to 0.60 g/cm² at 1 year and 0.57 g/cm² at 2 years in placebo recipients. At the end of the study only 18 postmenopausal women had osteoporosis in the genistein group with a prevalence of 12%, whereas in the placebo group the number of postmenopausal women with osteoporosis was unchanged, after 24 months. This post-hoc analysis is a proof-of concept study suggesting that genistein may be useful not only in postmenopausal osteopenia but also in osteoporosis. However, this proof-of concept study needs to be confirmed by a large, well designed, and appropriately focused randomized clinical trial in a population at high risk of fractures.
  • 1.1K
  • 01 Nov 2020
Topic Review
Endocannabinoid Signaling Pathways
Endocannabinoids play an important role as powerful regulators of synaptic function in the central nervous system where they regulate neural functions and behaviors. As fundamental modulators of synaptic function, endocannabinoids can regulate neural functions such as cognition, motor control, pain, and feeding behavior. The interaction between endogenous or exogenous ligands and endocannabinoid receptors initiates signaling pathways.
  • 1.1K
  • 24 Apr 2023
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