Review
Biology
Terry W. Moody, Irene Ramos-Alvarez, Robert T. Jensen
Summary: Cancer growth is regulated by receptor tyrosine kinases (RTKs) and G-protein-coupled receptors (GPCRs). Different mutations in EGFR and NTSR1 can lead to abnormal cancer proliferation. The use of tyrosine kinase inhibitors and SR48692 as antagonists can impair the transactivation process and inhibit cancer growth.
Article
Neurosciences
Mariela Mitre, Khalil Saadipour, Kevin Williams, Latika Khatri, Robert C. Froemke, Moses V. Chao
Summary: The study shows that oxytocin can enhance the activity of BDNF in neurons by transactivating the TrkB receptor. This finding is important for understanding the mechanism of oxytocin and its relationship with neural development and social behaviors.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2022)
Article
Developmental Biology
Farah Saad, David R. Hipfner
Summary: The Hedgehog (Hh) pathway is regulated by G protein-coupled receptors (GPCRs) in Drosophila, with Mthl5 identified as a modulator of this pathway. This suggests potential crosstalk between GPCRs and the Hh pathway in mammals as well.
Article
Cell Biology
Xiang Tao, Can Chen, Yingxiang Chen, Luoying Zhang, Jiong Hu, Hongjun Yu, Minglu Liang, Qin Fu, Kai Huang
Summary: This study reveals that beta(2)-adrenergic receptor (beta(2)AR) plays a critical role in liver regeneration by interacting with c-met and activating ERK signaling, leading to increased hepatocyte proliferation.
CELL DEATH & DISEASE
(2022)
Review
Cell Biology
Haoran Jiang, Daniella Galtes, Jialu Wang, Howard A. Rockman
Summary: This review explores the signaling pathways, dynamic structures, and physiological relevance of the three most important GPCR signaling effectors in the cardiovascular system: heterotrimeric G proteins, GPCR kinases (GRKs), and 8-arrestins. It summarizes their prominent roles in GPCR pharmacology before transitioning into less well-explored areas. The application of new technologies has contributed to an increasing understanding of GPCR structure and downstream effectors.
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
(2022)
Article
Medicine, General & Internal
Gerd Wallukat, Stephan Mattecka, Katrin Wenzel, Wieland Schroedl, Birgit Vogt, Patrizia Brunner, Ahmed Sheriff, Rudolf Kunze
Summary: This study found that C-reactive protein (CRP) affects intracellular calcium signaling and blood pressure. When CRP is combined with GPCR agonists in cardiomyocytes, it can interfere with the desensitization of GPCRs, regardless of the type of GPCR, but dependent on the concentration of CRP.
JOURNAL OF CLINICAL MEDICINE
(2022)
Article
Biology
Carolina Franco Nitta, Ellen W. Green, Elton D. Jhamba, Justine M. Keth, Irais Ortiz-Caraveo, Rachel M. Grattan, David J. Schodt, Aubrey C. Gibson, Ashwani Rajput, Keith A. Lidke, Bridget S. Wilson, Mara P. Steinkamp, Diane S. Lidke
Summary: Crosstalk between EGFR and RON is unidirectional, with EGFR phosphorylating RON to activate RON-directed signaling, which requires the formation of a signaling competent EGFR dimer. Nanoscale imaging reveals association of EGFR and RON in common plasma membrane microdomains, while two-color single particle tracking captures the formation of complexes between RON and EGF-bound EGFR.
Review
Biochemistry & Molecular Biology
Irene Lee-Rivera, Edith Lopez, Ana Maria Lopez-Colome
Summary: This review discusses the interactions of protease activated receptors (PARs) with their own family members as well as with other types of receptors. The authors point out that the cross-talk between receptors and signaling pathways is a novel mechanism providing diversity to receptor function and playing important roles in physiology and disease.
CELLULAR & MOLECULAR BIOLOGY LETTERS
(2022)
Article
Medicine, Research & Experimental
Cancan Lyu, Yuanchao Ye, Maddison M. Lensing, Kay-Uwe Wagner, Ronald J. Weigel, Songhai Chen
Summary: In HER2(+) breast cancer, overactivation of HER2 leads to aberrant G(i/o)-GPCR signaling, promoting cancer progression and resistance to HER2-targeted therapy. Pharmacologically deactivating GPCR signaling can block tumor growth and enhance therapeutic efficacy.
Review
Immunology
Nan Li, Shan Shan, Xiu-Qin Li, Ting-Ting Chen, Meng Qi, Sheng-Nan Zhang, Zi-Ying Wang, Ling-Ling Zhang, Wei Wei, Wu-Yi Sun
Summary: G protein-coupled receptor kinase 2 (GRK2) plays important roles in regulating signaling pathways associated with fibrotic diseases. Recent research suggests that GRK2 could be a potential therapeutic target for fibrotic diseases.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Sandra Berndt, Ines Liebscher
Summary: SFKs are crucial regulators of cell proliferation, differentiation, and survival, with their expression strongly linked to cancer development and tumor progression. The regulation of SFKs through GPCR-mediated pathways is complex and may involve direct protein interactions or allosteric regulation by arrestins and G proteins. The potential direct interaction between GPCRs and SFKs could lead to a novel mechanism of SFK signaling and identification of new GPCR-SFK interactions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Kinjal Patel, Nicola J. Smith
Summary: Primary cilia are important for sensing environmental changes in mammalian cells through the Sonic Hedgehog pathway. GPR161 is a significant player in primary cilia and its unique features may affect receptor function and cAMP compartmentalisation. The recent potential pairing of GPR161 and spexin-1 requires further investigation before GPR161 is considered 'deorphanised'. The constitutive activity and unconventional regulation of GPR161 suggest that it may not require an endogenous ligand.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Tasuku Nishino, Tsuyoshi Oshika, Moriatsu Kyan, Hiroaki Konishi
Summary: The study investigated the subcellular localization of GAREM1 and GAREM2 in response to cell growth stimulus. It was found that GAREM2 specifically formed granules in response to NGF and EGF stimulation, and a glycine-rich region in GAREM2 was required for this granule formation. This aggregation of GAREM2 may be linked to neurodegenerative diseases.
CELLULAR & MOLECULAR BIOLOGY LETTERS
(2021)
Article
Multidisciplinary Sciences
Maike Stegen, Andrea Engler, Crista Ochsenfarth, Iris Manthey, Jurgen Peters, Winfried Siffert, Ulrich H. Frey
Summary: The study characterized the human GRK6 promoter and found that the CREB binding site influenced promoter activity. Stimulation with a PKC activator led to decreased GRK6 expression at mRNA and protein levels, suggesting PKC might play a role in regulating GRK6 expression.
Review
Chemistry, Medicinal
Ningning Sun, Kyeong-Man Kim
Summary: The desensitization of G protein-coupled receptors can occur through various mechanisms including phosphorylation-dependent desensitization at the receptor level and downstream mechanisms involving the sequestration of G proteins. These mechanisms involve GRKs, arrestins, and deubiquitinated arrestins to regulate GPCR signaling and prevent G-protein activation. Further studies are needed on the interesting mechanism of arrestin deubiquitination in GPCR desensitization.
ARCHIVES OF PHARMACAL RESEARCH
(2021)
Article
Pharmacology & Pharmacy
Carla Sosa-Alvarado, Aurelio Hernandez-Mendez, M. Teresa Romero-Avila, Omar B. Sanchez-Reyes, Yoshinori Takei, Gozoh Tsujimoto, Akira Hirasawa, J. Adolfo Garcia-Sainz
EUROPEAN JOURNAL OF PHARMACOLOGY
(2015)
Correction
Biotechnology & Applied Microbiology
Mitra Khumbatta, Bahrom Firozgary, David John Tweardy, Joel Weinstock, Gohar Firozgary, Zal Bhatena, Tushar Bulsara, Ricardo Siller, Prema Robinson
BIOMED RESEARCH INTERNATIONAL
(2015)
Article
Pharmacology & Pharmacy
Marco A. Alfonzo-Mendez, Jean A. Castillo-Badillo, M. Teresa Romero-Avila, Richard Rivera, Jerold Chun, J. Adolfo Garcia-Sainz
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2016)
Article
Pharmacology & Pharmacy
Marco A. Alfonzo-Mendez, David A. Hernandez-Espinosa, Gabriel Carmona-Rosas, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
MOLECULAR PHARMACOLOGY
(2017)
Article
Biochemistry & Molecular Biology
S. Villegas-Comonfort, Y. Takei, G. Tsujimoto, A. Hirasawa, J. A. Garcia-Sainz
PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS
(2017)
Article
Multidisciplinary Sciences
Jean A. Castillo-Badillo, Omar B. Sanchez-Reyes, Marco A. Alfonzo-Mendez, Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
Article
Biochemistry & Molecular Biology
Juan Carlos Martinez-Morales, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
BIOSCIENCE REPORTS
(2018)
Article
Cell Biology
Gabriel Carmona-Rosas, David A. Hernandez-Espinosa, Rod Alcantara-Hernandez, Marco A. Alfonzo-Mendez, J. Adolfo Garcia-Sainz
CELLULAR SIGNALLING
(2019)
Review
Biochemistry & Molecular Biology
Karina Helivier Solis, M. Teresa Romero-Avila, Alejandro Guzman-Silva, J. Adolfo Garcia-Sainz
Summary: This review provides a comprehensive overview of the function regulation, signaling pathways activation, and structural characteristics of the LPA(3) receptor, highlighting the current knowledge gap in its functional regulation to stimulate further experimental work.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Juan Carlos Martinez-Morales, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, Jesus Adolfo Garcia-Sainz
Summary: The phosphorylation and endosomal traffic of G protein-coupled receptors play a significant role in receptor responsiveness, cellular localization, and fate, with important implications in pharmacology and therapy.
MOLECULAR PHARMACOLOGY
(2022)
Article
Cell Biology
Alejandro Guzman-Silva, Juan Carlos Martinez-Morales, Luz del Carmen Medina, M. Teresa Romero-Avila, Socrates Villegas-Comonfort, Karina Helivier Solis, J. Adolfo Garcia-Sainz
Summary: The phosphorylation sites of Free fatty acid receptor 1 were studied using mutants. The identified sites were found to play important roles in receptor phosphorylation, signaling, and internalization.
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2022)
Review
Medicine, Research & Experimental
Juan Carlos Martinez-Morales, K. Helivier Solis, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
Summary: G protein-coupled receptors (GPCRs) are membrane proteins that function as sensors and play significant roles in various physiological and pathological processes. This review provides an overview of the current understanding of the structure, signaling, internalization, and recycling of GPCRs.
ARCHIVES OF MEDICAL RESEARCH
(2022)
Article
Cell Biology
Juan Carlos Martinez-Morales, Karla D. Gonzalez-Ruiz, M. Teresa Romero-Avila, Ruth Rincon-Heredia, Guadalupe Reyes-Cruz, Jesus Adolfo Garcia-Sainz
Summary: LPA1 receptor internalization was studied using FRET to analyze the interaction between LPA1 and Rab proteins under different stimuli. The results showed that LPA-induced internalization was rapid and transient, while PMA-induced internalization was slower but sustained. LPA stimulated the interaction between LPA1 and Rab5 rapidly but transiently, while PMA showed a rapid but sustained interaction. LPA1-Rab9 interaction was only observed at 60 min, and LPA1-Rab7 interaction was observed after 5 min with LPA and after 60 min with PMA. LPA triggered immediate but transient rapid recycling, while PMA showed slower but sustained recycling. Our findings suggest that LPA1 receptor internalization varies depending on the stimuli.
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Marco A. Alfonzo-Mendez, Rocio Alcantara-Hernandez, J. Adolfo Garcia-Sainz
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2017)
Article
Pharmacology & Pharmacy
Jessica B. Nascimento-Viana, Aline R. Carvalho, Luiz Eurico Nasciutti, Rocio Alcantara-Hernandez, Fernanda Chagas-Silva, Pedro A. R. Souza, Luiz Antonio S. Romeiro, J. Adolfo Garcia-Sainz, Francois Noel, Claudia Lucia Martins Silva
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2016)