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Pharmaceuticals, Volume 14, Issue 7

July 2021 - 105 articles

Cover Story: Cell-Penetrating Peptides (CPPs) and nanobodies could combine into powerful targeting tools, if we optimize their synergy. Nanobodies are low molecular weight antigen-specific binders that show good tissue penetration. However, their fast clearance narrows the time window in which nanobodies distribute into the target tissue. CPPs could increase tissue accumulation of nanobodies, by enhancing their cellular uptake. Several CPPs enhance the uptake of the epidermal growth factor receptor-targeting nanobody 7D12 in monolayer cultures and cell spheroids. The physicochemical properties of each CPP influence those of the whole conjugate. Differences between CPPs suggest that future research should focus on understanding which and how physicochemical properties of CPP conjugates drive optimal biodistribution. View this paper
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Articles (105)

  • Article
  • Open Access
5 Citations
4,414 Views
15 Pages

Functional Characterization of the Oxantel-Sensitive Acetylcholine Receptor from Trichuris muris

  • Tina V. A. Hansen,
  • Richard K. Grencis,
  • Mohamed Issouf,
  • Cédric Neveu and
  • Claude L. Charvet

The human whipworm, Trichuris trichiura, is estimated to infect 289.6 million people globally. Control of human trichuriasis is a particular challenge, as most anthelmintics have a limited single-dose efficacy, with the striking exception of the narr...

  • Article
  • Open Access
5 Citations
4,973 Views
16 Pages

Development of Machine Learning Models for Accurately Predicting and Ranking the Activity of Lead Molecules to Inhibit PRC2 Dependent Cancer

  • Danishuddin,
  • Vikas Kumar,
  • Shraddha Parate,
  • Ashutosh Bahuguna,
  • Gihwan Lee,
  • Myeong Ok Kim and
  • Keun Woo Lee

Disruption of epigenetic processes to eradicate tumor cells is among the most promising interventions for cancer control. EZH2 (Enhancer of zeste homolog 2), a catalytic component of polycomb repressive complex 2 (PRC2), methylates lysine 27 of histo...

  • Review
  • Open Access
26 Citations
12,090 Views
13 Pages

Monoclonal Antibodies Targeting CGRP: From Clinical Studies to Real-World Evidence—What Do We Know So Far?

  • Theodoros Mavridis,
  • Christina I. Deligianni,
  • Georgios Karagiorgis,
  • Ariadne Daponte,
  • Marianthi Breza and
  • Dimos D. Mitsikostas

Now more than ever is the time of monoclonal antibody use in neurology. In headaches, disease-specific and mechanism-based treatments existed only for symptomatic management of migraines (i.e., triptans), while the standard prophylactic anti-migraine...

  • Review
  • Open Access
23 Citations
6,009 Views
19 Pages

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

  • Lexi Gower-Fry,
  • Travis Kronemann,
  • Andreas Dorian,
  • Yinglan Pu,
  • Carolin Jaworski,
  • Carmen Wängler,
  • Peter Bartenstein,
  • Leonie Beyer,
  • Simon Lindner and
  • Klaus Jurkschat
  • + 3 authors

The incorporation of silicon fluoride acceptor (SiFA) moieties into a variety of molecules, such as peptides, proteins and biologically relevant small molecules, has improved the generation of 18F-radiopharmaceuticals for medical imaging. The efficie...

  • Article
  • Open Access
9 Citations
4,594 Views
18 Pages

Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties

  • Kalyan K. Sethi,
  • KM Abha Mishra,
  • Saurabh M. Verma,
  • Daniela Vullo,
  • Fabrizio Carta and
  • Claudiu T. Supuran

New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hC...

  • Review
  • Open Access
90 Citations
9,939 Views
16 Pages

Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

  • Ryldene Marques Duarte da Cruz,
  • Francisco Jaime Bezerra Mendonça-Junior,
  • Natália Barbosa de Mélo,
  • Luciana Scotti,
  • Rodrigo Santos Aquino de Araújo,
  • Reinaldo Nóbrega de Almeida and
  • Ricardo Olímpio de Moura

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, des...

  • Feature Paper
  • Article
  • Open Access
36 Citations
4,697 Views
8 Pages

Soluble Angiotensin Converting Enzyme 2 (ACE2) Is Upregulated and Soluble Endothelial Nitric Oxide Synthase (eNOS) Is Downregulated in COVID-19-induced Acute Respiratory Distress Syndrome (ARDS)

  • Alice G. Vassiliou,
  • Alexandros Zacharis,
  • Chrysi Keskinidou,
  • Edison Jahaj,
  • Maria Pratikaki,
  • Parisis Gallos,
  • Ioanna Dimopoulou,
  • Anastasia Kotanidou and
  • Stylianos E. Orfanos

A damaged endothelium is an underlying condition of the many complications of COVID-19 patients. The increased mortality risk associated with diseases that have underlying endothelial dysfunction, such as acute respiratory distress syndrome (ARDS), s...

  • Article
  • Open Access
5 Citations
4,818 Views
14 Pages

The present study aimed to evaluate the effects of NK-4 on the apoptosis of photoreceptors in a rat model of retinitis pigmentosa and explore the mechanism underlying anti-apoptosis activity. The Royal College of Surgeons (RCS) rats received an intra...

  • Article
  • Open Access
24 Citations
4,587 Views
21 Pages

The objective of the present study was to develop n-propyl gallate-loaded solid lipid nanoparticles (PG-SLNs) in a hydrogel (HG) formulation using Transcutol-P (TC-P) as a permeation enhancer. Modified solvent injection technique was applied to produ...

  • Article
  • Open Access
12 Citations
4,797 Views
20 Pages

Albumin Nanoparticle Formulation for Heart-Targeted Drug Delivery: In Vivo Assessment of Congestive Heart Failure

  • Nikita Lomis,
  • Ziyab K. Sarfaraz,
  • Aiman Alruwaih,
  • Susan Westfall,
  • Dominique Shum-Tim and
  • Satya Prakash

Congestive heart failure is a fatal cardiovascular disease resulting in tissue necrosis and loss of cardiac contractile function. Inotropic drugs such as milrinone are commonly used to improve the myocardial contractility and heart function. However,...

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Pharmaceuticals - ISSN 1424-8247