Article
Food Science & Technology
Xavier Maia Mariano, Luana Caroline de Assis Ferreira, Camila Megale Almeida-Leite, Celio Jose de Castro Junior, Maria Elena de Lima
Summary: The synthetic peptide PnPP-15 shows promising antinociceptive effects against diabetic neuropathic pain and exhibits synergism when used in combination with pregabalin, resulting in a more efficient treatment.
Article
Food Science & Technology
Ekaterina N. N. Lyukmanova, Pavel A. A. Mironov, Dmitrii S. S. Kulbatskii, Mikhail A. A. Shulepko, Alexander S. S. Paramonov, Elizaveta M. M. Chernaya, Yulia A. A. Logashina, Yaroslav A. A. Andreev, Mikhail P. P. Kirpichnikov, Zakhar O. O. Shenkarev
Summary: This article reports on the neurotoxin Phα1β (PnTx3-6) from the venom of the spider Phoneutria nigriventer, which acts as an antagonist on two ion channels involved in nociception. The study demonstrates that Phα1β can reduce both acute and chronic pain. NMR spectroscopy was used to determine the spatial structure and dynamics of Phα1β, providing important insights into the structure and function of spider toxins.
Article
Biochemistry & Molecular Biology
F. C. Cardoso, A. A. Walker, G. F. King, M. V. Gomez
Summary: This study explored the neuroactivity and molecular diversity of Phoneutria nigriventer venom. By using proteomics and multi-pharmacology activity coupled to fractionation-guided high-throughput cellular assays, the research provides a proof-of-concept for studying spider-venom derived neuroactive peptides. The venom was found to be highly complex and contains potent modulators of voltage-gated ion channels.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2023)
Article
Endocrinology & Metabolism
Claudia Pedron, Flavia Tasmin Techera Antunes, Isadora Nunes Rebelo, Maria Martha Campos, Aurea Pandolfo Correa, Caroline Peres Klein, Iasmine Berbigier de Oliveira, Marta do Nascimento Cordeiro, Marcus Vinicius Gomez, Alessandra Hubner de Souza
Summary: In this study, mice treated with reserpine showed significant relief in pain and depressive symptoms when administered with the Tx3-3 toxin, indicating its potential for fibromyalgia treatment. Traditional analgesics also demonstrated anti-nociceptive effects in this model.
Article
Pharmacology & Pharmacy
Zachary W. Reichenbach, Kelly DiMattio, Suren Rajakaruna, David Ambrose, William D. Cornwell, Ronald J. Tallarida, Thomas Rogers, Lee-Yuan Liu-Chen, Ronald F. Tuma, Sara Jane Ward
Summary: Non-selective cannabinoid (CB) agonists can enhance the analgesic effects of morphine but inhibit its antinociceptive tolerance. Activation of CB2 receptors can reverse allodynia and hyperalgesia in chronic pain models, and co-administration of CB2 receptor selective agonists with morphine can synergistically enhance the effects. However, the interactions between CB2 receptor selective agonist O-1966 and morphine depend on the order of administration.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Yue Wang, Youwen Zhuang, Jeffrey F. DiBerto, X. Edward Zhou, Gavin P. Schmitz, Qingning Yuan, Manish K. Jain, Weiyi Liu, Karsten Melcher, Yi Jiang, Bryan L. Roth, H. Eric Xu
Summary: Opioids are powerful painkillers with serious side effects. The study examines the binding and selectivity mechanisms of endogenous opioid peptides with opioid receptors, revealing a structural framework for the design of safer pain relief drugs.
Review
Biochemistry & Molecular Biology
Katarzyna Kaczynska, Piotr Wojciechowski
Summary: Opioids, while potent analgesics, are associated with side effects like tolerance, addiction, respiratory depression, and cardiovascular events. Researchers are seeking ways to counteract these effects, with peptides and related compounds showing potential in modulating opioid actions. Various peptides, including nociceptin/orphanin, ghrelin, oxytocin, endothelin, and venom peptides, have been researched for their modulation of opioid effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Chemistry, Medicinal
Tao Zhuang, Jiaying Xiong, Shuaishuai Hao, Wei Du, Zhenming Liu, Bifeng Liu, Guisen Zhang, Yin Chen
Summary: Opioid analgesics are effective for pain management but have undesirable side effects, prompting the need for new, safer analgesics. The sigma-1 receptor plays a crucial role in pain modulation and its antagonists can reduce pain and enhance the effects of opioid analgesics.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Psychiatry
Javier Ballester, Anne K. Baker, Ilkka K. Martikainen, Vincent Koppelmans, Jon-Kar Zubieta, Tiffany M. Love
Summary: This study found that chronic pain patients at high risk for opioid misuse showed higher baseline MOR availability in the right amygdala, while patients at low risk for opioid misuse showed less pain-induced activation of MOR-mediated, endogenous opioid neurotransmission in the nucleus accumbens.
TRANSLATIONAL PSYCHIATRY
(2022)
Article
Chemistry, Medicinal
Ying-Ting Hsu, Shen-Ren Chen, Yung-Chiao Chang, Hsiao-Fu Chang, Teng-Kuang Yeh, Jian-Ying Chuang, Horace H. Loh, Hsing-Pang Hsieh, Shau-Hua Ueng, Shiu-Hwa Yeh
Summary: The demand for a non-addictive analgesic medication is increasing due to clinical misuse. Compound 14 is a dual agonist of the mu opioid receptor (MOR) and nociceptin-orphanin FQ opioid peptide (NOP) receptor, providing pain relief at very small doses and reducing unwanted side effects. Evaluating its effects in wild type and humanized mice can help develop a safer prescription analgesic drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Karan H. Muchhala, Joanna C. Jacob, William L. Dewey, Hamid Akbarali
Summary: The role of 0-arrestin-2 in opioid tolerance was investigated, showing its involvement in acute, but not chronic tolerance in dorsal root ganglia neurons and in vivo antinociception. These findings suggest that opioid-induced antinociceptive tolerance can develop even without 0-arrestin-2 activation, significantly impacting the clinical utility of biased agonists.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Alexander R. French, Richard M. van Rijn
Summary: Kappa opioid receptor (icOR) agonists are considered safer alternatives to clinically used mu opioid receptor (mu OR) analgesics with no abuse liability and respiratory depression effects. However, they have their own limiting adverse effects that hinder clinical translation. Recent studies suggest that these effects may be due to distinct intracellular signaling pathways, leading to the hypothesis that biased icOR agonists away from ll-arrestin signaling could have improved therapeutic windows. Overall, G-protein-biased icOR agonists generally have better therapeutic windows compared to unbiased agonists, although study design limits strong conclusions in this regard. The development of biased icOR agonists and new tools in the field puts icOR research in a position to advance our understanding and translation of biased icOR agonists to clinical use.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Lisa M. Eubanks, Steven Blake, Yoshihiro Natori, Beverly Ellis, Paul T. Bremer, Kim D. Janda
Summary: The opioid epidemic remains a dire public health crisis, with synthetic opioids such as fentanyl being highly potent and dangerous. Researchers have developed vaccines targeting synthetic opioids like fentanyl and carfentanil, which have shown protective effects in mice, providing new strategies for preventing drug abuse and overdose.
ACS CHEMICAL BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Flavia Tasmin Techera Antunes, Emanuelle Sistherenn Caminski, Marcus Vinicius Gomez, Alessandra Hubner de Souza
Summary: This study reviewed the pharmacological evidence of Ph alpha 1 beta and its recombinant form CTK 01512-2, and found that these peptides have potential analgesic and neuroprotective effects.
INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS
(2022)
Article
Food Science & Technology
Julieta Vasquez-Escobar, Dora Maria Benjumea-Gutierrez, Carolina Lopera, Herlinda C. Clement, Damaris I. Bolanos, Jorge Luis Higuita-Castro, Gerardo A. Corzo, Ligia Luz Corrales-Garcia
Summary: This paper reports the isolation of an insecticidal peptide from the venom gland transcriptome of the Brazilian spider, Phoneutria depilata. A synthetic gene was constructed and the recombinant peptide (rCtx-4) was expressed, purified and validated. The insecticidal activity of rCtx-4 was demonstrated in crickets, indicating its potential as a bioinsecticide for agricultural use.
Article
Pharmacology & Pharmacy
Katharina Held, Vincenzo Davide Aloi, Ana Cristina Nogueira Freitas, Annelies Janssens, Andrei Segal, Julia Przibilla, Stephan Ernst Philipp, Yu Tian Wang, Thomas Voets, Joris Vriens
Summary: This study compares the pharmacological properties of different splice variants of TRPM3, demonstrating that the length of the pore-forming loop in the alternative splicing region defines the channel's activation by specific compounds.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Dongchen An, Ernesto Lopes Pinheiro-Junior, Laszlo Beress, Irina Gladkikh, Elena Leychenko, Eivind A. B. Undheim, Steve Peigneur, Jan Tytgat
Summary: AsKC11, a Kunitz peptide found in the venom of A. sulcata, is the first peptide shown to directly activate neuronal GIRK1/2 channels independent from Gi/o protein activity, without affecting the inward-rectifier potassium channel (IRK1) and with only a minor effect on K(V)1.6 channels. Thus, AsKC11 is a novel activator of GIRK channels resulting in larger K+ currents because of an increased chord conductance.
Article
Chemistry, Medicinal
Ernesto Lopes Pinheiro-Junior, Rimma Kalina, Irina Gladkikh, Elena Leychenko, Jan Tytgat, Steve Peigneur
Summary: Hcr 1b-2, a peptide from the venom of Heteractis crispa, shows a lack of selectivity and targets multiple ion channels, making it an interesting tool for studying ion channels and developing new ion channel ligands.
Article
Biochemistry & Molecular Biology
Prapenpuksiri Rungsa, Steve Peigneur, Nisachon Jangpromma, Sompong Klaynongsruang, Jan Tytgat, Sakda Daduang
Summary: This study investigates the structure-activity relationship of antimicrobial peptides by analyzing the effect of amino acid substitutions and deletion of C-terminal residues. It is found that phenylalanine substitution increases antibacterial activity, while deletions of C-terminal residues decrease antibacterial and hemolytic activity.
Article
Biochemistry & Molecular Biology
Pornsawan Khamtorn, Steve Peigneur, Fernanda Gobbi Amorim, Loic Quinton, Jan Tytgat, Sakda Daduang
Summary: This study provides an overview of the molecular diversity of Latrodectus geometricus spider venom through transcriptomic analysis. Several important venom components were identified, and the bioactivity of the venom was investigated using an electrophysiological bioassay. The findings contribute to our understanding of spider venom and can aid in the development of insecticides targeting voltage-gated sodium channels.
Article
Endocrinology & Metabolism
Sabrina Pereira Silva, Otavio Garcia Martins, Liciane Fernandes Medeiros, Priscila Centeno Crespo, Carlus Augustu Tavares do Couto, Joice Soares de Freitas, Andressa de Souza, Amanda Morastico, Luis Augusto Xavier Cruz, Paulo Roberto Stefani Sanches, Wolnei Caumo, Giovana Duzzo Gamaro, Iraci Lucena da Silva Torres, Izabel Cristina Custodio de Souza
Summary: This study evaluated the effect of transcranial direct current stimulation (tDCS) on a chronic inflammatory pain model in rats. The results showed that tDCS treatment was able to reverse mechanical allodynia, decrease thermal hyperalgesia, and reduce local inflammation.
NEUROIMMUNOMODULATION
(2022)
Article
Polymer Science
Daniele N. Gouveia, Adriana G. Guimaraes, Marlange A. Oliveira, Thallita K. Rabelo, Licia T. S. Pina, Wagner B. R. Santos, Iggo K. S. Almeida, Tatianny A. Andrade, Mairim Russo Serafini, Bruno S. Lima, Adriano A. S. Araujo, Jose Evaldo R. Menezes-Filho, Artur Santos-Miranda, Luciana Scotti, Marcus Tullius Scotti, Henrique Douglas Melo Coutinho, Jullyana S. S. Quintans, Raffaele Capasso, Lucindo J. Quintans-Junior
Summary: Alpha-terpineol nanocapsules (TP-LNC) show potential as a candidate drug for treating chemotherapy-induced peripheral neuropathy. The study finds that TP-LNC has stability and encapsulation efficiency, and can prolong the antihyperalgesic effect when combined with free TP. Furthermore, TP has molecular interactions with different calcium channels, reducing calcium currents.
Article
Biochemistry & Molecular Biology
James P. Farmer, Shailesh N. Mistry, Charles A. Laughton, Nicholas D. Holliday
Summary: This study developed fluorescent-labeled peptides as novel binding and activation biosensors for the GPCR-IAM site, allowing the assessment of the affinity of unlabeled ligands for the receptor and providing a new method for screening IAMs. Moreover, this method can be used to investigate the efficacy of orthosteric agonists and the dynamics of receptor activation.
Article
Neurosciences
Paul Vicuna Serrano, Maxciel Zortea, Rael Lopes Alves, Gerardo Beltran, Cibely Bavaresco, Leticia Ramalho, Camila Fernanda da Silveira Alves, Liciane Medeiros, Paulo R. S. Sanches, Danton P. Silva Jr, Iraci Lucena da Silva Torres, Felipe Fregni, Wolnei Caumo
Summary: The study demonstrated that daily treatment with a home-based tDCS device improved cognitive impairment in FM over 4 weeks. The use of a-tDCS at home was well-tolerated, indicating its potential as an alternative treatment for cognitive dysfunction. Furthermore, the efficacy of a-tDCS was associated with the severity of DPMS dysfunction and changes in neuroplasticity state.
FRONTIERS IN HUMAN NEUROSCIENCE
(2022)
Article
Neurosciences
Fabricio Finamor, Vanessa Leal Scarabelot, Liciane Fernandes Medeiros, Dirson Joao Stein, Morgana Duarte da Silva, Etiane Callai, Wolnei Caumo, Andressa de Souza, Iraci L. S. Torres
Summary: This study evaluated the involvement of GABAergic, glutamatergic, opioidergic systems, and BDNF levels in trigeminal neuropathic pain (TNP) in rats. The results suggest that GABA, phenobarbital, and morphine can reverse the hyperalgesia induced by TNP. Glutamatergic antagonists can increase pain threshold, and BDNF levels are elevated in TNP and normal tissues. These findings contribute to our understanding of the neural mechanisms underlying TNP.
NEUROSCIENCE LETTERS
(2023)
Article
Biochemistry & Molecular Biology
Junyu Liu, Michael Maxwell, Thom Cuddihy, Theo Crawford, Madeline Bassetti, Cameron Hyde, Steve Peigneur, Jan Tytgat, Eivind A. B. Undheim, Mehdi Mobli
Summary: Receptor avidity through multivalency is difficult to engineer in synthetic molecules, but can be found in natural bivalent antibodies. The discovery of bivalent venom peptides with tandem repeat domains has provided insight into multivalency in biomolecules. ScrepYard, an online resource, assists in identifying SCREP sequences and characterizing this emerging class of biomolecules.
Article
Pharmacology & Pharmacy
Noemie Luyts, Jan Daniluk, Ana Cristina Nogueira Freitas, Bahar Bazeli, Annelies Janssens, Marie Mulier, Wouter Everaerts, Thomas Voets
Summary: In this study, the effect of Phenazopyridine (PAP) on pain-related Transient Receptor Potential (TRP) channels was investigated. The results showed that PAP can rapidly and reversibly inhibit the cold and menthol sensitivity of TRPM8 channels. This suggests that the inhibition of TRPM8 may be the mechanism underlying the analgesic activity of PAP.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Neurosciences
Priscila Centeno Crespo, Leo Anderson Meira Martins, Clara Camacho Dos Reis, Liciane Fernandes Medeiros, Vanessa Leal Scarabelot, Giovana Duzzo Gamaro, Mayara Sandrielly Pereira Soares, Roselia Maria Spanevello, Francieli Moro Stefanello, Izabel Cristina Custodio De Souza
Summary: This study analyzed the effects of transcranial direct current stimulation (tDCS) on biochemical parameters in rats with neuropathic pain. The results showed that tDCS increased the total sulfhydryl content in the spinal cord of rats, positively modulating neuropathic pain.
NEUROSCIENCE LETTERS
(2023)
Article
Chemistry, Medicinal
Bianca Maria Casella, James P. P. Farmer, Desislava N. N. Nesheva, Huw E. L. Williams, Steven J. J. Charlton, Nicholas D. D. Holliday, Charles A. A. Laughton, Shailesh N. N. Mistry
Summary: Inhibition of CXCR2 is a potential strategy for the treatment of pulmonary diseases and cancers. This study reports the design and synthesis of fluorescent NAMs that selectively bind to CXCR2, enabling the measurement and evaluation of their pharmacological properties. These NAMs can be used as alternative compounds for targeting these receptors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Anesthesiology
Tania Maria Hendges de Paula, Mariane Schaffer Castro, Liciane Fernandes Medeiros, Rodrigo Hernandes Paludo, Fabricia Fritz Couto, Taina Ramires da Costa, Juliana Pereira Fortes, Maiara de Oliveira Salbego, Gabriel Schardosim Behnck, Thielly Amaral Mesquita de Moura, Mariana Lenz Tarouco, Wolnei Caumo, Andressa de Souza
Summary: This study aimed to evaluate the analgesic and neuromodulatory effects of a combination of Low-Dose Naltrexone (LDN) and Transcranial Direct Current Stimulation (tDCS) in patients with fibromyalgia. The results showed that the combination of LDN and tDCS can reduce pain frequency and intensity. However, further studies are needed to analyze the possible association.
BRAZILIAN JOURNAL OF ANESTHESIOLOGY
(2023)
