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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)

  • Review
  • Open Access
4 Citations
3,165 Views
19 Pages

Metal complexes feature a wide range of available geometries, diversified lability, controllable hydrolytic stability, and easily available rich redox activity. These characteristics, combined with the specific properties of coordinated organic molec...

  • Article
  • Open Access
25 Citations
3,417 Views
17 Pages

Alkaloid from Geissospermum sericeum Benth. & Hook.f. ex Miers (Apocynaceae) Induce Apoptosis by Caspase Pathway in Human Gastric Cancer Cells

  • Mirian Letícia Carmo Bastos,
  • João Victor Silva-Silva,
  • Jorddy Neves Cruz,
  • Amanda Roberta Palheta da Silva,
  • Alexandre Augusto Bentaberry-Rosa,
  • Gisele da Costa Ramos,
  • José Edson de Sousa Siqueira,
  • Márlia Regina Coelho-Ferreira,
  • Sandro Percário and
  • Patrícia Santana Barbosa Marinho
  • + 3 authors

Gastric cancer is among the major causes of death from neoplasia leading causes of death worldwide, with high incidence rates and problems related to its treatment. Here, we outline how Geissospermum sericeum exerts antitumor activity on the ACP02 ce...

  • Article
  • Open Access
2 Citations
2,849 Views
16 Pages

Identification of the Hepatic Metabolites of Flumazenil and their Kinetic Application in Neuroimaging

  • Wei-Hsi Chen,
  • Chuang-Hsin Chiu,
  • Shiou-Shiow Farn,
  • Kai-Hung Cheng,
  • Yuan-Ruei Huang,
  • Shih-Ying Lee,
  • Yao-Ching Fang,
  • Yu-Hua Lin and
  • Kang-Wei Chang

Studies of the neurobiological causes of anxiety disorders have suggested that the γ-aminobutyric acid (GABA) system increases synaptic concentrations and enhances the affinity of GABAA (type A) receptors for benzodiazepine ligands. Flumazenil...

  • Article
  • Open Access
2 Citations
2,858 Views
12 Pages

Triple-Therapy of Peritoneal Metastasis—Partial-Dehydration under Hyperthermic Condition Combined with Chemotherapy: The First Preliminary In-Vitro Results

  • Carolina Khosrawipour,
  • Agata Diakun,
  • Shiri Li,
  • Hien Lau,
  • Joanna Kulas,
  • Veria Khosrawipour,
  • Wojciech Kielan and
  • Agata Mikolajczyk-Martinez

A newly introduced combination of intraperitoneal dehydration and hyperthermia has recently been shown to be feasible and cytotoxic for colon cancer cells in vivo. For the first time, our study now aims to evaluate dehydration under hyperthermic cond...

  • Article
  • Open Access
1 Citations
2,869 Views
12 Pages

SIRT1 Signaling Is Involved in the Vascular Improvement Induced by Moringa Oleifera Seeds during Aging

  • Valeria Conti,
  • Joseph Iharinjaka Randriamboavonjy,
  • Herintsoa Rafatro,
  • Valentina Manzo,
  • Jessica Dal Col,
  • Amelia Filippelli,
  • Graziamaria Corbi and
  • Angela Tesse

Vascular aging is linked to reduce NO bioavailability, endothelial dysfunction, oxidative stress, and inflammation. We previously showed that a 4-week treatment of middle-aged Wistar rats (MAWRs, 46 weeks old) with Moringa oleifera seed powder (MOI,...

  • Review
  • Open Access
8 Citations
7,127 Views
13 Pages

Honey-Related Treatment Strategies in Dry Eye Disease

  • Julia Prinz,
  • Nicola Maffulli,
  • Matthias Fuest,
  • Peter Walter,
  • Frank Hildebrand and
  • Filippo Migliorini

This systematic review and meta-analysis investigated whether honey-related treatment strategies improve the signs and symptoms of patients with dry eye disease (DED). In March 2023, the following databases were accessed for clinical trials investiga...

  • Review
  • Open Access
4 Citations
7,042 Views
10 Pages

Objective. The aim of this review is to explore the role of IGF-1 and IGF-1R inhibitors in pain-related conditions and assess the effectiveness of IGF-1-related drugs in pain management. Specifically, this paper investigates the potential involvement...

  • Article
  • Open Access
2 Citations
2,234 Views
13 Pages

To elucidate the potential roles of serotonergic activity in human character traits (i.e., self-directedness, cooperativeness, and self-transcendence), we investigated the relationship between these character traits and serotonin transporter (5-HTT)...

  • Article
  • Open Access
5 Citations
2,960 Views
26 Pages

Structure Optimization of 12β-O-γ-Glutamyl Oleanolic Acid Derivatives Resulting in Potent FXR Antagonist/Modulator for NASH Therapy

  • Hao Ma,
  • Yunyang Bao,
  • Shuaishuai Niu,
  • Shaorong Wang,
  • Yiming Li,
  • Hongwei He,
  • Na Zhang and
  • Weishuo Fang

The farnesoid X receptor (FXR) plays a crucial role in regulating the metabolism of bile acids, lipids, and sugars. Consequently, it is implicated in the treatment of various diseases, including cholestasis, diabetes, hyperlipidemia, and cancer. The...

  • Article
  • Open Access
2 Citations
2,904 Views
16 Pages

MKX-AS1 Gene Expression Associated with Variation in Drug Response to Oxaliplatin and Clinical Outcomes in Colorectal Cancer Patients

  • Ricardo D. Gonzalez,
  • George W. Small,
  • Adrian J. Green,
  • Farida S. Akhtari,
  • Alison A. Motsinger-Reif,
  • Julia C. F. Quintanilha,
  • Tammy M. Havener,
  • David M. Reif,
  • Howard L. McLeod and
  • Tim Wiltshire

Oxaliplatin (OXAL) is a commonly used chemotherapy for treating colorectal cancer (CRC). A recent genome wide association study (GWAS) showed that a genetic variant (rs11006706) in the lncRNA gene MKX-AS1 and partnered sense gene MKX could impact the...

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Pharmaceuticals - ISSN 1424-8247