scholarly journals Piper longum: A review of its phytochemicals and their network pharmacological evaluation

2017 ◽  
Author(s):  
Neha Choudhary ◽  
Vikram Singh
Keyword(s):  
Drug Targets ◽  
Network Pharmacology ◽  
High Confidence ◽  
Protein Targets ◽  
Piper Longum ◽  
Protein Target ◽  
The Common ◽  
Novel Drug ◽  
Novel Drug Targets

AbstractPiper longum L. (P. longum, also called as long pepper) is one of the common culinary herb and has been extensively used as an important constituent of various indigenous medicines, specifically in traditional Indian medicinal system known as Ayurveda. Towards obtaining a global regulatory framework of P. longum’s constituents, in this work we first reviewed phytochemicals present in this herb and then studied their pharmacological and medicinal features using network pharmacology approach. We developed high-confidence level tripartite networks consisting of phytochemicals – protein targets – disease association and explain the role of its phytochemicals to various chronic diseases. 7 drug-like phytochemicals in this herb were found as the potential regulators of 5 FDA approved drug targets; and 28 novel drug targets were also reported. 105 phytochemicals were linked with immunomodulatory potency by pathway level mapping in human metabolic network. A sub-network of human PPI regulated by its phytochemicals was derived and various modules in this sub-network were successfully associated with specific diseases.Graphical abstractAbbreviationsP. longumPiper longum L.PCPhytochemicalPTProtein targetBPBiological pathwaysDADisease asscociationPCtNumber of protein targets corresponding to a particular phytochemicalTtTotal number of protein targets of P. longumADMETAbsorption, Distribution, Metabolism, Excretion and Toxicity.

scholarly journals A Novel FtsZ-Like Protein Is Involved in Replication of the Anthrax Toxin-Encoding pXO1 Plasmid in Bacillus anthracis

2006 ◽  
Vol 188 (8) ◽  
pp. 2829-2835 ◽  
Author(s):  
Eowyn Tinsley ◽  
Saleem A. Khan
Keyword(s):  
Bacillus Anthracis ◽  
Drug Targets ◽  
Mutational Analysis ◽  
Anthrax Toxin ◽  
Replication Proteins ◽  
Reading Frame ◽  
Virulence Plasmids ◽  
Novel Drug ◽  
Novel Drug Targets

ABSTRACTPlasmid pXO1 encodes the tripartite anthrax toxin, which is the major virulence factor ofBacillus anthracis. In spite of the important role of pXO1 in anthrax pathogenesis, very little is known about its replication and maintenance inB. anthracis. We cloned a 5-kb region of the pXO1 plasmid into anEscherichia colivector and showed that this plasmid can replicate when introduced intoB. anthracis. Mutational analysis showed that open reading frame 45 (repX) of pXO1 was required for the replication of the miniplasmid inB. anthracis. Interestingly,repXshowed limited homology to bacterial FtsZ proteins that are involved in cell division. A mutation in the predicted GTP binding domain of RepX abolished its replication activity. Genes almost identical torepXare contained on several megaplasmids in members of theBacillus cereusgroup, including aB. cereusstrain that causes an anthrax-like disease. Our results identify a novel group of FtsZ-related initiator proteins that are required for the replication of virulence plasmids inB. anthracisand possibly in related organisms. Such replication proteins may provide novel drug targets for the elimination of plasmids encoding the anthrax toxin and other virulence factors.

Receptor Mediated Uptake of Pepsin: Significance in Otolaryngology

2008 ◽  
Vol 18 (3) ◽  
pp. 134-142
Author(s):  
Nikki Johnston
Keyword(s):  
Drug Targets ◽  
Proton Pump Inhibitor Therapy ◽  
Positive Symptom ◽  
Persistent Symptoms ◽  
Laryngeal Injury ◽  
Intraluminal Impedance ◽  
Gastric Contents ◽  
Novel Drug ◽  
Novel Drug Targets

Abstract Reflux of gastric contents into the laryngopharynx contributes to voice disorders, otolaryngological inflammatory disorders, and perhaps even neoplastic diseases of the laryngopharynx. Treatment is currently focuses on increasing the pH of the refluxate because it was thought that the refluxate would not cause injury/symptoms at higher pH. However, many patients with reflux-attributed laryngeal injury/disease have persistent symptoms despite aggressive acid supression therapy. Recent studies using combined multi-channel intraluminal impedance with pH montioring have shown a positive symptom association with non- and weakly-acidic reflux and an association between non-/weakly acidic reflux and refractory symptoms on proton pump inhibitor therapy. Thus, the role of acid alone in the development of reflux related laryngeal pathology has to be questioned and studies examining the effects of the other components of the refluxate are clearly needed. Our data, described herein, supports a role for pepsin in reflux-attributed laryngeal injury/disease independent of the pH of the refluxate and highlights potential novel drug targets.

Understanding Mass Spectrometry-based Global Mycobacterial Lipidomics

2020 ◽  
Vol 20 (8) ◽  
pp. 607-623
Author(s):  
Zeeshan Fatima ◽  
Shiv Nandan ◽  
Saif Hameed
Keyword(s):  
Mass Spectrometry ◽  
Drug Targets ◽  
Infectious Agent ◽  
Dry Weight ◽  
Diagnostic Methods ◽  
Detection Methods ◽  
Novel Drug ◽  
Significant Attention ◽  
Novel Drug Targets

: Tuberculosis (TB) is the foremost cause of mortality from single infectious agent Mycobacterium tuberculosis (MTB). Current therapeutic regimes suffer from several problems, including side effects, costs and emergence of multidrug resistance (MDR). Moreover, conventional diagnostic methods are either too slow, or lack accurate and robust biomarkers. Under such circumstances, identification of rapid metabolite based biomarkers as novel drug targets could be a potential approach to circumvent MDR. In the era of “OMIC” sciences, lipidomics has gained significant attention to unravel the complexity of lipid-loaded Mycobacterium species. Lipidomics is a subbranch of metabolomics with extreme atomic diversity between the metabolites. There is no single principle on which the metabolite diversity can be defined, unlike other biomolecules viz. nucleic acid, proteins or carbohydrates. MTB encodes 10% of the genome for lipid metabolism and lipids account for 60% of its dry weight. Mycobacterium harbor a wide spectra of lipid repertoire ranging from highly apolar to highly polar lipids, adding complexity to their identification and analysis. Compared to targeted approaches, untargeted or global lipidomics of MTB is still more challenging. This review describes recent advances in lipidomics technology with regard to chromatography, detection methods and assessment on the existing mass spectrometry-based lipidomics tools to study the untargeted or global MTB lipidomics. It also identifies the limitations associated with present technologies as well as explores solutions to practical challenges concurrent with the establishment of MTB lipidome. Together we endorse that the emerging tools of lipidomics have provided a broader vision to comprehend the role of lipid molecules in MTB pathogenesis and the need for further improvements.

scholarly journals The Research Progress of Vascular Macrophages and Atherosclerosis

2020 ◽  
Vol 2020 ◽  
pp. 1-4 ◽  
Author(s):  
Yeqing Tong ◽  
Li Cai ◽  
Shiyu Yang ◽  
Shuang Liu ◽  
Zhihong Wang ◽  
...  
Keyword(s):  
Immune Regulation ◽  
Drug Targets ◽  
Scientific Evidence ◽  
Research Progress ◽  
Prevention And Treatment ◽  
Depth Study ◽  
Novel Drug ◽  
Host Genes ◽  
Novel Drug Targets

Background/Aims. Vascular macrophages may affect the immune regulation of atherosclerosis (AS). In recent years, there are lots of researches on the association of vascular macrophages and AS which has attracted increasing attention, and the in-depth study of its mechanism is gradually clear. Materials. We made a minireview on the association of vascular macrophages with AS based on recent research studies systematically, from the mechanisms of macrophages accumulating in the walls of blood vessels, and the role of macrophages in AS as well as microenvironmental determinants of macrophage function in AS. The discovery of these mechanisms could reveal the pathogenesis of AS comprehensively and is crucial to provide scientific evidence for formulating the related measures of prevention and treatment for AS. Discussion. Vascular macrophages play important roles in the development of AS, and the vascular macrophages may become new targets for the prevention and treatment of AS. Effective regulation of host genes may help prevent or even treat AS. Conclusion. This minireview focuses on the association of vascular macrophages with the development of AS, which may supply some clues for future therapies and novel drug targets for AS.

scholarly journals Molecular Mechanisms to Target Cellular Senescence in Hepatocellular Carcinoma

Cells ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 2540
Author(s):  
Constanze Mittermeier ◽  
Andreas Konopa ◽  
Susanne Muehlich
Keyword(s):  
Hepatocellular Carcinoma ◽  
Drug Targets ◽  
Molecular Mechanisms ◽  
Serum Response Factor ◽  
Pharmacological Interventions ◽  
Therapeutic Concepts ◽  
Novel Drug ◽  
Serum Response ◽  
Novel Drug Targets

Hepatocellular carcinoma (HCC) has emerged as a major cause of cancer-related death and is the most common type of liver cancer. Due to the current paucity of drugs for HCC therapy there is a pressing need to develop new therapeutic concepts. In recent years, the role of Serum Response Factor (SRF) and its coactivators, Myocardin-Related Transcription Factors A and B (MRTF-A and -B), in HCC formation and progression has received considerable attention. Targeting MRTFs results in HCC growth arrest provoked by oncogene-induced senescence. The induction of senescence acts as a tumor-suppressive mechanism and therefore gains consideration for pharmacological interventions in cancer therapy. In this article, we describe the key features and the functional role of senescence in light of the development of novel drug targets for HCC therapy with a focus on MRTFs.

scholarly journals Characterization of the erythrocyte GTPase Rac1 in relation to Plasmodium falciparum invasion

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Silvio Paone ◽  
Sarah D’Alessandro ◽  
Silvia Parapini ◽  
Francesco Celani ◽  
Valentina Tirelli ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Host Cell ◽  
Drug Targets ◽  
Parasitophorous Vacuole ◽  
Erythrocyte Invasion ◽  
Inhibitory Compounds ◽  
Novel Drug ◽  
Novel Drug Targets

AbstractMalaria is still a devastating disease with 228 million cases globally and 405,000 lethal outcomes in 2018, mainly in children under five years of age. The threat of emerging malaria strains resistant to currently available drugs has made the search for novel drug targets compelling. The process by which Plasmodium falciparum parasites invade the host cell has been widely studied, but only a few erythrocyte proteins involved in this process have been identified so far. The erythrocyte protein Rac1 is a GTPase that plays an important role in host cell invasion by many intracellular pathogens. Here we show that Rac1 is recruited in proximity to the site of parasite entry during P. falciparum invasion process and that subsequently localizes to the parasitophorous vacuole membrane. We also suggest that this GTPase may be involved in erythrocyte invasion by P. falciparum, by testing the effect of specific Rac1 inhibitory compounds. Finally, we suggest a secondary role of the erythrocyte GTPase also in parasite intracellular development. We here characterize a new erythrocyte protein potentially involved in P. falciparum invasion of the host cell and propose the human GTPase Rac1 as a novel and promising antimalarial drug target.

Novel drug targets in 2019

2020 ◽  
Vol 19 (5) ◽  
pp. 300-300 ◽  
Author(s):  
Sorin Avram ◽  
Liliana Halip ◽  
Ramona Curpan ◽  
Tudor I. Oprea
Keyword(s):  
Drug Targets ◽  
Novel Drug ◽  
Novel Drug Targets
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