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Pharmaceuticals, Volume 13, Issue 2

2020 February - 15 articles

Cover Story: Targeting deregulation within cancer cell metabolism appears to be promising strategy for the development of more efficient cancer treatments. Recent reports highlight the crucial role of the serine synthetic pathway, and particularly of its first enzyme, the phosphoglycerate dehydrogenase (PHGDH), in sustaining cancer progression. Yet, due to the usually too weak potencies in cell-based settings, the inhibitors reported so far failed to identify the potential of this approach. In this paper, we report the structure-activity relationships of a series of α-ketothioamides that we recently identified. The activity of the more potent compounds was confirmed by cellular thermal shift assays and cell-based experiments. The findings provide a deeper understanding of this series and to the identification of new PHGDH inhibitors. View this paper.
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Articles (15)

  • Review
  • Open Access
39 Citations
10,145 Views
15 Pages

21 February 2020

CXC chemokine receptor 7 (CXCR7) is a G-protein-coupled receptor that signals through the β-arrestin pathway. Its ligands include interferon-inducible T cell α chemoattractant (CXCL11) and stromal cell-derived factor-1 (CXCL12). It interac...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
18 Citations
5,562 Views
15 Pages

Binding Constants of Substituted Benzoic Acids with Bovine Serum Albumin

  • Diliara Khaibrakhmanova,
  • Alena Nikiforova and
  • Igor Sedov

20 February 2020

Experimental data on the affinity of various substances to albumin are essential for the development of empirical models to predict plasma binding of drug candidates. Binding of 24 substituted benzoic acid anions to bovine serum albumin was studied u...

(This article belongs to the Section Medicinal Chemistry)
  • Feature Paper
  • Review
  • Open Access
85 Citations
11,446 Views
18 Pages

Cell Secretome: Basic Insights and Therapeutic Opportunities for CNS Disorders

  • Andreia G. Pinho,
  • Jorge R. Cibrão,
  • Nuno A. Silva,
  • Susana Monteiro and
  • António J. Salgado

20 February 2020

Transplantation of stem cells, in particular mesenchymal stem cells (MSCs), stands as a promising therapy for trauma, stroke or neurodegenerative conditions such as spinal cord or traumatic brain injuries (SCI or TBI), ischemic stroke (IS), or Parkin...

(This article belongs to the Special Issue Therapeutics Agents for Neural Repair)
  • Article
  • Open Access
12 Citations
6,254 Views
15 Pages

Grаdiеnt HPLC Mеthоd fоr Simultаnеоus Dеtеrminаtiоn оf Еight Sаrtаn аnd Stаtin Drugs in Thеir Purе аnd Dоsаgе Fоrms

  • Mоhsеn M. Zаrеh,
  • Mоnir Z. Sааd,
  • Wаfаа S. Hаssаn,
  • Mоstаfа Е. Еlhеnnаwу,
  • Moustafa K. Soltan and
  • Mаhmоud M. Sеbаiу

20 February 2020

А grаdiеnt HPLC mеthоd was dеvеlоpеd аnd vаlidаtеd fоr rаpid simultаnеоus sеpаrаtiоn аnd dеtеrminаtiоn оf the following eight drugs оf sаrtаn аnd stаtin clаssеs in thеir purе аnd dоsаgе fоrms within 15 minutes: irbеsаrtаn (IRB), lоsаrtаn (LОS), vаlsа...

  • Review
  • Open Access
11 Citations
5,719 Views
11 Pages

12 February 2020

Background: Reducing the burden of beta-amyloid accumulation and toxic autoimmunity-related proteins, one of the recognized pathophysiological markers of chronic and common neurological disorders such as Alzheimer’s disease (AD) and multiple sc...

(This article belongs to the Special Issue Therapeutics Agents for Neural Repair)
  • Feature Paper
  • Article
  • Open Access
6 Citations
3,743 Views
12 Pages

Metabolic Stability of New Mito-Protective Short-Chain Naphthoquinones

  • Zikai Feng,
  • Jason A. Smith,
  • Nuri Gueven and
  • Joselito P. Quirino

12 February 2020

Short-chain quinones (SCQs) have been identified as potential drug candidates against mitochondrial dysfunction, which is largely dependent on their reversible redox characteristics of the active quinone core. We recently synthesized a SCQ library of...

(This article belongs to the Section Pharmacology)
  • Technical Note
  • Open Access
8 Citations
5,617 Views
9 Pages

11 February 2020

A simple color spot test for determining the presence of residual tetrabutylammonium (TBA) in various 18F-radiopharmaceuticals is described. The test can be performed in less than five minutes. Iodoplatinate-saturated TLC plates are initially spotted...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
1 Citations
3,758 Views
14 Pages

5 February 2020

Pancreatic cancer, hepatocellular carcinoma (HCC), and mesothelioma are treatment-refractory cancers, and patients afflicted with these cancers generally have a very poor prognosis. The genomics of these tumors were analyzed as part of The Cancer Gen...

(This article belongs to the Special Issue Protein Kinases and Cancer)
  • Article
  • Open Access
16 Citations
5,430 Views
20 Pages

Synthesis and Bioactivity of Phthalimide Analogs as Potential Drugs to Treat Schistosomiasis, a Neglected Disease of Poverty

  • Snigdha Singh,
  • Nelly El-Sakkary,
  • Danielle E. Skinner,
  • Prem Prakash Sharma,
  • Sabine Ottilie,
  • Yevgeniya Antonova-Koch,
  • Prashant Kumar,
  • Elizabeth Winzeler,
  • Poonam and
  • Brijesh Rathi
  • + 1 author

3 February 2020

The neglected tropical disease, schistosomiasis, is caused by trematode blood flukes of the Schistosoma genus and infects approximately 200 million people worldwide. With just one partially effective drug available for disease treatment, new drugs ar...

  • Article
  • Open Access
18 Citations
4,882 Views
20 Pages

Hormetic-Like Effects of L-Homocysteine on Synaptic Structure, Function, and Aβ Aggregation

  • Carla Montecinos-Oliva,
  • Macarena S. Arrázola,
  • Claudia Jara,
  • Cheril Tapia-Rojas and
  • Nibaldo C. Inestrosa

2 February 2020

Alzheimer’s Disease (AD) is the primary cause of dementia among the elderly population. Elevated plasma levels of homocysteine (HCy), an amino acid derived from methionine metabolism, are considered a risk factor and biomarker of AD and other t...

(This article belongs to the Special Issue Therapeutics Agents for Neural Repair)
  • Review
  • Open Access
81 Citations
12,101 Views
35 Pages

Ultrasound for Drug Synthesis: A Green Approach

  • Micheline Draye,
  • Gregory Chatel and
  • Romain Duwald

31 January 2020

This last century, the development of new medicinal molecules represents a real breakthrough in terms of humans and animal life expectancy and quality of life. However, this success is tainted by negative environmental consequences. Indeed, the synth...

(This article belongs to the Special Issue New Tools for Medicinal Chemists)
  • Review
  • Open Access
44 Citations
8,224 Views
38 Pages

30 January 2020

This review deals with the development of peptide-based radiopharmaceuticals for the use with positron emission tomography and peptide receptor radiotherapy. It discusses the pros and cons of this class of radiopharmaceuticals as well as the differen...

(This article belongs to the Special Issue The Future Direction of Radiopharmaceutical Development for Cancer Theranostics)
  • Article
  • Open Access
16 Citations
5,341 Views
14 Pages

Development and Validation of Liquid Chromatography-Tandem Mass Spectrometry Method for Simple Analysis of Sumatriptan and its Application in Bioequivalence Study

  • Wisut Wichitnithad,
  • Siriwan Nantaphol,
  • Petploy Vicheantawatchai,
  • Thanyaporn Kiatkumjorn,
  • Wachirasak Wangkangwan and
  • Pornchai Rojsitthisak

24 January 2020

This work demonstrated a sensitive, selective, and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantitation of sumatriptan in human plasma samples. Terazosin was used as an internal standard to minimize the variability...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
26 Citations
7,061 Views
22 Pages

Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH)

  • Quentin Spillier,
  • Séverine Ravez,
  • Judith Unterlass,
  • Cyril Corbet,
  • Charline Degavre,
  • Olivier Feron and
  • Raphaël Frédérick

22 January 2020

For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the...

(This article belongs to the Special Issue Recent Contributions in Medicinal Chemistry Within European GP2A Network)
  • Article
  • Open Access
43 Citations
6,441 Views
15 Pages

Peptide-Based Soft Hydrogels Modified with Gadolinium Complexes as MRI Contrast Agents

  • Enrico Gallo,
  • Carlo Diaferia,
  • Enza Di Gregorio,
  • Giancarlo Morelli,
  • Eliana Gianolio and
  • Antonella Accardo

21 January 2020

Poly-aromatic peptide sequences are able to self-assemble into a variety of supramolecular aggregates such as fibers, hydrogels, and tree-like multi-branched nanostructures. Due to their biocompatible nature, these peptide nanostructures have been pr...

(This article belongs to the Special Issue Metal-Based Drugs: Updates and Perspectives)
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Pharmaceuticals - ISSN 1424-8247