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Pharmaceuticals, Volume 13, Issue 2

February 2020 - 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)

  • Article
  • Open Access
16 Citations
5,024 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...

  • Feature Paper
  • Review
  • Open Access
73 Citations
10,001 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...

  • Article
  • Open Access
11 Citations
5,876 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
10 Citations
4,979 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...

  • Feature Paper
  • Article
  • Open Access
6 Citations
3,392 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...

  • Technical Note
  • Open Access
7 Citations
4,571 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...

  • Article
  • Open Access
1 Citations
3,495 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...

  • Article
  • Open Access
15 Citations
4,969 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
  • Conor R. Caffrey
  • + 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
17 Citations
4,362 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...

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Pharmaceuticals - ISSN 1424-8247