PubMed Journal Database | Current topics in medicinal chemistry RSS

00:04 EST 6th December 2019 | BioPortfolio

The US National Library of Medicine and National Institutes of Health manage which comprises of more than 29 million records, papers, reports for biomedical literature, including MEDLINE, life science and medical journals, articles, reviews, reports and  books.

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For example view all recent relevant publications on Epigenetics and associated publications and clincial trials.

Showing PubMed Articles 1–25 of 54 from Current topics in medicinal chemistry

The use of fibrin-based tissue adhesives for breast in reconstructive and plastic surgery.

Breast plastic surgery is a rapidly evolving field in medicine. The modern view of surgical trends reflects the desire to minimize complications and introduce advanced technologies. These always will be priorities for surgeons. Reconstructive surgery, a branch of plastic surgery focusing on restoration of lost functional and aesthetic component, seeks to enhance psychological rehabilitation and improve quality of life, as well as aesthetic recovery.

Ligand-Based Pharmacophore Modeling and Virtual Screening to discover novel CYP1A1 Inhibitors.

Cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) is an imperative enzyme due to its immersion in the biotransformation of a wide range of drugs and other xenobiotics. The involvement in drug metabolism suggests this enzyme an effective drug target for the development of novel therapeutics. The discovery of CYP1A1 specific inhibitors would be of particular relevance for the clinical pharmacology.

Search for potential Inducible Nitric Oxide Synthase inhibitors with favorable ADMET profiles for the therapy of Helicobacter pylori infections.

Helicobacter pylori is a gram-negative bacterium related to chronic gastritis, peptic ulcer and gastric carcinoma. During its infection process, promotes excessive inflammatory response, increasing the release of reactive species and inducing the production of pro-inflammatory mediators. Inducible Nitric Oxide Synthase (iNOS) plays a crucial role in the gastric carcinogenesis process and a key mediator of inflammation and host defense systems, which is expressed in macrophages induced by inflammatory stimul...

In silico insights on Disialoganglioside GD2 : A Potential target for Pediatric Neuroblastoma.

The In silico approach provides a platform for determination and establishing a potential inhibitor against GD2 in Pediatric neuroblastoma.

Herbal Medicine of the 21st Century: A Focus on the Chemistry, Pharmacokinetics and Toxicity of Five Widely Advocated Phytotherapies.

Widely advocated for their health benefits worldwide, herbal medicine (HM) has evolved into a billion dollar generating industry. Much is known on their wellness, prophylactic and therapeutic benefits for the relief of both minor to chronic ailments given their long-standing use among various cultures. On the other hand, their equally meaningful chemistry, pharmacokinetic, interaction and toxicity profile has been poorly researched and documented. Consequently, this review is an attempt to highlight the hea...

Feasibility of targeting glioblastoma stem cells: From concept to clinical trials.

Glioblastoma is a highly aggressive and invasive brain tumor. Current treatment options do not prolong overall survival significantly because the disease is highly prone to relapse. Therefore, research to find new therapies is of paramount importance. It was discovered that glioblastomas contain a population of cells with stem-like properties and that these cells are may be responsible for tumor recurrence. In this critical review, we will discuss potential treatment strategies to target cancer stem cells i...

Synthesis, biological evaluation and molecular docking studies of novel di-hydropyridine analogs as potent antioxidants.

The aim of the present study to synthesis and biological evaluation of 3-ethyl 5-methyl 2-(2-aminoethoxy)-4-(2-chlorophenyl)-1,4-dihydropyridine-3,5-dicarboxylate derivatives. Dihydropyridine (DHP) is an important class of calcium antagonist structure, the structure of the compound pyridine natured with semi-saturated with two substituents replacing one double bond. DHP inhibits the influx of extracellular Ca2+ through L-type voltage-dependent calcium channels in earlier reports.

In-silico subtractive proteomic analysis approach for therapeutic targets in MDR Salmonella enterica sub sp. Enterica serovar Typhi str. CT18.

In the present study, an attempt has been made for subtractive proteomic analysis approach for novel drug targets in Salmonella enterica subsp. Enterica serover Typhi str.CT18 using computational tools. Paralogous, redundant and less than 100 amino acid protein sequences were removed by using CD-HIT.

Cytotoxicity of Anchusa arvensis against HepG-2 cell lines: Mechanistic and computational approaches.

Liver cancer, a devastating cancer with increasing incidence and mortality rates worldwide. Plants possess numerous therapeutic properties, therefore the search for novel, naturally occurring cytotoxic compounds is urgently needed.

Spiro-Lactams as Novel Antimicrobial Agents.

To extend our previous studies on spirocyclic-β-lactams with anti-HIV and antiplasmodial properties to new spirocyclic-lactams in order to further explore structure-activity relationships.

Whether The Validation Of The Predictive Potential Of Toxicity Models Is Solved Task?

Different kinds of biological activity are defined by complex biochemical interactions, i.e. are a "mathematical function" not only of the molecular structure but also some unclear addition circumstances, such as physicochemical conditions, interactions via energy and information effects between a substance and organisms, organs, cells. These circumstances lead to great complexity of prediction for biochemical endpoints, since all "details" of corresponding phenomena are practically unavailable for the accu...

Identification of Dual negative allosteric modulators of Group I mGluR family: A shape based screening, ADME Prediction, Induced Fit Docking and Molecular Dynamics approach against Neurodegenerative Diseases.

Glutamate is principal neurotransmitter in human brain that exerts its effects through iGlu and mGlu receptors. The mGluRs are the class C GPCRs play vital role in various neurobiological functions, mGluR1 and mGluR5 are the two receptors distributed throughout the brain involved in cognition, learning, memory and other important neurological process. Dysfunction of these receptors can cause neurodegenerative diseases such as Alzheimer's disease, Parkinson Disease, X-fragile syndrome, anxiety, depression et...

Developing Insulin and BDNF Mimetics for Diabetes Therapy.

Diabetes is a global public health concern nowadays. The majority of diabetes mellitus (DM) patients belong to type 2 diabetes mellitus (T2DM), which is highly associated with obesity. The general principle of current therapeutic strategies for patients with T2DM mainly focuses on restoring cellular insulin response by potentiating the insulin-induced signaling pathway. In late-stage T2DM, impaired insulin production requires the patients to receive insulin replacement therapy for maintaining their glucose ...

Insights into the Structural Aspects of the mGlu Receptor Orthosteric Binding Site.

The amino terminal domain (ATD) of the metabotropic glutamate (mGlu) receptors contains the orthosteric glutamate recognition site, which is highly conserved across the eight mGlu receptor subtypes. In total, 29 X-ray crystal structures of the mGlu ATD proteins have been reported to date. These structures span across 3 subgroups and 6 subtypes, and include apo, agonist- and antagonist-bound structures. We will discuss the insights gained from the analysis of these structures with the focus on the interactio...

NMDAR PAMs: Multiple Chemotypes for Multiple Binding Sites.

The N-methyl-D-aspartate receptor (NMDAR) is a member of the ionotropic glutamate receptor (iGluR) family that plays a crucial role in brain signalling and development. NMDARs are nonselective cation channels that are involved with the propagation of excitatory neurotransmission signals with important effects on synaptic plasticity. NMDARs are functionally and structurally complex receptors, they exist as a family of subtypes each with its own unique pharmacological properties. Their implication in a variet...

Activation of Transient Receptor Potential Vanilloid (TRPV) 4 as a Therapeutic Strategy in Osteoarthritis.

Transient receptor potential vanilloid (TRPV) 4 belongs to the TRPV subfamily of TRP ion channels. TRPV4 channels play a critical role in chondrocytes and thus TRPV4 is an attractive target of disease-modifying osteoarthritis drugs (DMOADs). Initial investigations of small molecules by Glaxo Smith Klein (GSK) as both agonists and antagonists via oral/intravenous administration have led to the use of existing agonists as lead compounds for biological studies. Our recent results suggest that local injection o...

Identifying cancer targets based on machine learning methods via Chou's 5-steps rule and general pseudo components.

In recent years, the successful implementation of human genome project has made people realize that genetic, environmental and lifestyle factors should be combined together to study cancer due to the complexity and various forms of the disease. The increasing availability and growth rate of 'big data' derived from various omics, opens a new window for study and therapy of cancer. In this paper, we will introduce the application of machine learning methods in handling cancer big data including the use of art...

Advances in Dopamine D1 Receptor Ligands for Neurotherapeutics.

The dopamine D1 receptor (D1R) is essential for neurotransmission in various brain pathways where it modulates key functions including voluntary movement, memory, attention and reward. Not surprisingly, the D1R has been validated as a promising drug target for over 40 years and selective activation of this receptor may provide novel neurotherapeutics for neurodegenerative and neuropsychiatric disorders. Several pharmacokinetic challenges with previously identified small molecule D1R agonists have been recen...

EDITORIAL; GPCR Drug Discovery: Emerging Targets, Novel Approaches and Future Trends.

Recent Advances in Medicinal Chemistry to Treat Filariasis and Helminthiasis.

Bioactive Natural and Synthetic Peroxides for the Treatment of Helminth and Protozoan Pathogens: Synthesis and Properties.

The significant spread of helminth and protozoan infections, the uncontrolled intake of the known drugs by a large population, the emergence of resistant forms of pathogens have prompted people to search for alternative drugs. In this review, we have focused attention on structures and synthesis of peroxides active against parasites causing neglected tropical diseases and toxoplasmosis. To date, promising active natural, semi-synthetic and synthetic peroxides compounds have been found.

Advances in Dopamine D1 Receptor Ligands for Neurotherapeutics.

The dopamine D1 receptor (D1R) is essential for neurotransmission in various brain pathways where it modulates key functions including voluntary movement, memory, attention and reward. Not surprisingly, the D1R has been validated as a promising drug target for over 40 years and selective activation of this receptor may provide novel neurotherapeutics for neurodegenerative and neuropsychiatric disorders. Several pharmacokinetic challenges with previously identified small molecule D1R agonists have been recen...

Targeting Mutant KRAS for Anticancer Therapy.

Over the past decades, designing therapeutic strategies to target KRAS-mutant cancers, which is one of the most frequent mutant oncogenes among all cancer types, have proven unsuccessful regardless of many concerted attempts. There are key challenges for KRAS-mutant anticancer therapy, as the complex cellular processes involved in KRAS signaling has present. Herein we highlight the emerging therapeutic approaches for inhibiting KRAS signaling and blocking KRAS functions, in hope to serve as a more effective...

Recent Advances in Developing K-Ras Plasma Membrane Localization Inhibitors.

The Ras proteins play an important role in cell growth, differentiation, proliferation and survival by regulating diverse signaling pathways. Oncogenic mutant K-Ras is the most frequently mutated class of Ras superfamily and highly prevalent in many human cancers. Despite intensive efforts to combat various K-Ras-mutant-driven cancers, no effective K-Ras-specific inhibitors have yet been approved for clinical use to date. Since K-Ras proteins must be associated to the plasma membrane for their function, tar...

Drug Combinatorial Therapies for Treatment of KRAS Mutated Lung Cancers.

KRAS is the most common oncogene to be mutated in lung cancer, and therapeutics directly targeting KRAS has proven to be challenging. The mutations of KRAS are associated with poor prognosis, resistance to both adjuvant therapy and targeted EGFR TKI. The EGFR TKI provide significant clinical benefit for patients whose tumors bear EGFR mutations. However, tumors with KRAS mutations rarely respond to EGFR TKI therapy. Thus, the combination therapy is essential for the treatment of lung cancers with KRAS mutat...

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