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Pharmaceuticals, Volume 16, Issue 5

May 2023 - 142 articles

Cover Story: G-protein-coupled receptors (GPCRs) represent valid molecular targets for directing peptide radioligands to malignant lesions. Diagnosis (γ-emitters: SPECT, β+-emitters: PET) and therapy (α, β-, Auger e- emitters: PRRT) are combined in a new promising “radiotheranostics” approach. Radiolabeled somatostatin analogs are widely used in neuroendocrine tumor patients, whereas peptide radioligands targeting other GPCRs in different tumors include bombesin, gastrin and exendin analogs. A recent switch from internalizing GPCR agonists to antagonists led to better pharmacokinetics and higher biosafety. GPCR antagonists do not activate their target receptor and do not elicit acute adverse effects when injected into patients. We herein discuss the challenges and opportunities of modern peptide radiotheranostics, focusing on GPCR antagonists. View this paper
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Articles (142)

  • Article
  • Open Access
7 Citations
2,748 Views
20 Pages

Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam

  • Van Bon Nguyen,
  • San-Lang Wang,
  • Tu Quy Phan,
  • Thi Huyen Thoa Pham,
  • Hung-Tse Huang,
  • Chia-Ching Liaw and
  • Anh Dzung Nguyen

Among ten extracts of indigenous medicinal plants, the MeOH extract of Terminalia triptera Stapf. (TTS) showed the most efficient mammalian α-glucosidase inhibition for the first time. The data of screening bioactive parts used indicated that t...

  • Article
  • Open Access
19 Citations
4,006 Views
18 Pages

Resveratrol Enhances Cytotoxic Effects of Cisplatin by Inducing Cell Cycle Arrest and Apoptosis in Ovarian Adenocarcinoma SKOV-3 Cells through Activating the p38 MAPK and Suppressing AKT

  • Phateep Hankittichai,
  • Phatarawat Thaklaewphan,
  • Nitwara Wikan,
  • Jirapak Ruttanapattanakul,
  • Saranyapin Potikanond,
  • Duncan R. Smith and
  • Wutigri Nimlamool

In the current study, we identified a mechanism of resveratrol (RES) underlying its anti-cancer properties against human ovarian adenocarcinoma SKOV-3 cells. We investigated its anti-proliferative and apoptosis-inducing effects in combination with ci...

  • Review
  • Open Access
7 Citations
3,405 Views
12 Pages

RadioLigand Therapy with [177Lu]Lu-PSMA-617 for Salivary Gland Cancers: Literature Review and First Compassionate Use in France

  • Marie Terroir,
  • Chloé Lamesa,
  • Mehdi Krim,
  • Lavinia Vija,
  • Jean-Sébastien Texier,
  • Thibaut Cassou-Mounat,
  • Jean-Pierre Delord,
  • Delphine Vallot and
  • Frédéric Courbon

Salivary gland cancers are rare tumors comprising a large group of heterogeneous tumors with variable prognosis. Their therapeutic management at a metastatic stage is challenging due to the lack of therapeutic lines and the toxicity of treatments. [1...

  • Article
  • Open Access
31 Citations
5,674 Views
21 Pages

Alzheimer’s disease (AD) is a progressive neurological illness characterized by memory loss and cognitive deterioration. Dapagliflozin was suggested to attenuate the memory impairment associated with AD; however, its mechanisms were not fully e...

  • Article
  • Open Access
4 Citations
3,583 Views
14 Pages

Network Biology-Inspired Machine Learning Features Predict Cancer Gene Targets and Reveal Target Coordinating Mechanisms

  • Taylor M. Weiskittel,
  • Andrew Cao,
  • Kevin Meng-Lin,
  • Zachary Lehmann,
  • Benjamin Feng,
  • Cristina Correia,
  • Cheng Zhang,
  • Philip Wisniewski,
  • Shizhen Zhu and
  • Choong Yong Ung
  • + 1 author

Anticipating and understanding cancers’ need for specific gene activities is key for novel therapeutic development. Here we utilized DepMap, a cancer gene dependency screen, to demonstrate that machine learning combined with network biology can...

  • Article
  • Open Access
5 Citations
3,518 Views
19 Pages

Assessment of Aptamer as a Potential Drug Targeted Delivery for Retinal Angiogenesis Inhibition

  • David Moreira,
  • Jéssica Lopes-Nunes,
  • Fátima Milhano Santos,
  • Maria Paula Cabral Campello,
  • Maria Cristina Oliveira,
  • António Paulo,
  • Cândida Tomaz and
  • Carla Cruz

AT11-L0 is an aptamer derivative of AS1411 composed of G-rich sequences that can adopt a G-quadruplex (G4) structure and target nucleolin (NCL), a protein that acts as a co-receptor for several growth factors. Hence, this study aimed to characterize...

  • Review
  • Open Access
17 Citations
8,716 Views
16 Pages

Effects of Lipid-Modifying and Other Drugs on Lipoprotein(a) Levels—Potent Clinical Implications

  • Amalia Despoina Koutsogianni,
  • George Liamis,
  • Evangelos Liberopoulos,
  • Petros Spyridonas Adamidis and
  • Matilda Florentin

The past few years have shown an ongoing interest in lipoprotein(a) (Lp(a)), a lipid molecule that has been proven to have atherogenic, thrombogenic, and inflammatory properties. Several lines of evidence, indeed, have demonstrated an increased risk...

  • Article
  • Open Access
4 Citations
3,728 Views
21 Pages

S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer

  • Zhenyan Hou,
  • Songwen Lin,
  • Tingting Du,
  • Mingjin Wang,
  • Weida Wang,
  • Shen You,
  • Nina Xue,
  • Yichen Liu,
  • Ming Ji and
  • Heng Xu
  • + 1 author

Microtubule-targeting agents are widely used as active anticancer drugs. However, drug resistance always emerges after their long-term use, especially in the case of paclitaxel, which is the cornerstone of all subtypes of breast cancer treatment. Hen...

  • Review
  • Open Access
18 Citations
4,928 Views
25 Pages

Neuropharmacological Potential of Diterpenoid Alkaloids

  • Arash Salehi,
  • Mustafa Ghanadian,
  • Behzad Zolfaghari,
  • Amir Reza Jassbi,
  • Maryam Fattahian,
  • Parham Reisi,
  • Dezső Csupor,
  • Ikhlas A. Khan and
  • Zulfiqar Ali

This study provides a narrative review of diterpenoid alkaloids (DAs), a family of extremely important natural products found predominantly in some species of Aconitum and Delphinium (Ranunculaceae). DAs have long been a focus of research attention d...

  • Article
  • Open Access
7 Citations
5,140 Views
14 Pages

The Potential of Epigallocatechin-3-gallate (EGCG) as Complementary Medicine for the Treatment of Inflammatory Bowel Disease

  • Sabrina Schnur,
  • Fabian Hans,
  • Annika Dehne,
  • Janina Osti,
  • Malte-Ole Schneemann,
  • Marc Schneider and
  • Marius Hittinger

Complementary and alternative medicine has the potential to enrich conventional therapy to improve the treatment of various diseases. Patients that suffer from inflammatory bowel disease, which requires a constant need for medication, have to deal wi...

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Pharmaceuticals - ISSN 1424-8247