Explanipedia

Class A Orphans in GtoPdb v.2025.3 Open

S P H Alexander, Amy E. Monaghan, Chido Mpamhanga, Richard R. Neubig, Adam J Pawson , et al. · 2025

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [206], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Angiotensin receptors in GtoPdb v.2025.3 Open

Wayne Alexander, Sadashiva S. Karnik, Jacqueline Kemp, Luxmichan Laishram, Walter G. Thomas , et al. · 2025

The actions of angiotensin II (Ang II) are mediated by AT1 and AT2 receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Angiotensin receptors [63, 155]), which have around 30% sequence similarity. The octapeptide angiotensin …

Class A Orphans in GtoPdb v.2025.2 Open

S P H Alexander, Amy E. Monaghan, Chido Mpamhanga, Richard R. Neubig, Adam J Pawson , et al. · 2025

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [197], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Class A Orphans in GtoPdb v.2025.1 Open

S P H Alexander, Chido Mpamhanga, Richard R. Neubig, Adam J Pawson, Jean‐Philippe Pin , et al. · 2025

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [164], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Gut microbe-generated phenylacetylglutamine is an endogenous allosteric modulator of β2-adrenergic receptors Open

Prasenjit Prasad Saha, Valentin Gogonea, Wendy E. Sweet, Maradumane L. Mohan, Khuraijam Dhanachandra Singh , et al. · 2024

Ammonia transporter RhBG initiates downstream signaling and functional responses by activating NFκB Open

Saurabh Mishra, Nicole Welch, Shashi Shekhar Singh, Khuraijam Dhanachandra Singh, Annette Bellar , et al. · 2024

Transceptors, solute transporters that facilitate intracellular entry of molecules and also initiate intracellular signaling events, have been primarily studied in lower-order species. Ammonia, a cytotoxic endogenous metabolite, is convert…

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors Open

S P H Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie , et al. · 2023

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 600…

Angiotensin receptors in GtoPdb v.2023.1 Open

Wayne Alexander, Kenneth E. Bernstein, Kevin Catt, Marc de Gasparo, Khuraijam Dhanachandra Singh , et al. · 2023

The actions of angiotensin II (Ang II) are mediated by AT1 and AT2 receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Angiotensin receptors [63, 155]), which have around 30% sequence similarity. The decapeptide angiotensin …

Class A Orphans in GtoPdb v.2023.1 Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2023

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [161], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Distinct Mechanisms of β-Arrestin–Biased Agonist and Blocker of AT1R in Preventing Aortic Aneurysm and Associated Mortality Open

Zaira Palomino Jara, Terri J. Harford, Khuraijam Dhanachandra Singh, Russell Desnoyer, Avinash Kumar , et al. · 2022

Background: Aortic aneurysm (AA) is a “silent killer” human disease with no effective treatment. Although the therapeutic potential of various pharmacological agents have been evaluated, there are no reports of β-arrestin–biased AT1R (angi…

Class A Orphans in GtoPdb v.2022.3 Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2022

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [161], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Hydrazone bimetallic complex: synthesis, characterization, in silico and biological evaluation targeting breast and lung cancer cells’ G-quadruplex DNA Open

Mayada S. Ali, Dhanachandra Kuraijam, Sadashiva S. Karnik, Laila A. Jaragh-Alhadad · 2022

Manganese complex of (N'1E,N'3E)-N'1,N'3-bis(2-hydroxybenzylidene)isophthalo-hydrazide [H4L] was designed, spectroscopically analyzed, and confirmed via GC-MS, FTIR, CHNS, UV-VIS, magnetic susceptibility measurements, and molar electric co…

Cancer targeted drug delivery using active low-density lipoprotein nanoparticles encapsulated pyrimidines heterocyclic anticancer agents as microtubule inhibitors Open

Laila A. Jaragh-Alhadad, Haider Behbehani, Sadashiva S. Karnik · 2022

Recently, nanomedicine had the potential to increase the delivery of active compounds to specific cell sites. Nano-LDL particles are recognized as an excellent active nano-platform for cancer-targeted delivery. Loading of therapeutic agent…

Sulfonamide derivatives mediate breast and lung cancer cell line killing through tubulin inhibition Open

Laila A. Jaragh-Alhadad, Mayada S. Ali, Moustafa S. Moustafa, Gamaleldin I. Harisa, Fars K. Alanazi , et al. · 2022

Tubulin plays essential roles in cell signaling, division, proliferation, and other cellular functions. Tubulin is a potential target for anticancer agents. The classical tubulin inhibitors have a low therapeutic index, multi-drug resistan…

Low-density lipoprotein encapsulated thiosemicarbazone metal complexes is active targeting vehicle for breast, lung, and prostate cancers Open

Laila A. Jaragh-Alhadad, Mayada S. Ali, Terri J. Harford, Sadashiva S. Karnik · 2022

Cancer is a leading cause of death worldwide and affects society in terms of the number of lives lost. Current cancer treatments are based on conventional chemotherapy which is nonspecific in targeting cancer. Therefore, intensive efforts …

Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin receptors: IUPHAR Review 34 Open

Khuraijam Dhanachandra Singh, Sadashiva S. Karnik · 2022

Functional advances have guided our knowledge of physiological and fatal pathological mechanisms of the hormone angiotensin II (AngII) and its antagonists. Such studies revealed that tissue response to a given dose of the hormone or its an…

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors Open

S P H Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie , et al. · 2021

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasi…

Class A Orphans in GtoPdb v.2021.3 Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2021

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [161], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Novel allosteric ligands of the angiotensin receptor AT1R as autoantibody blockers Open

Khuraijam Dhanachandra Singh, Zaira Palomino Jara, Terri J. Harford, Prasenjit Prasad Saha, Triveni R. Pardhi , et al. · 2021

Significance High-resolution structural knowledge is a key driver for discovering small molecules to target functional motifs in G protein-coupled receptors (GPCRs). Reports of autoantibodies targeting extracellular motifs of GPCRs are inc…

Integrated multiomics analysis identifies molecular landscape perturbations during hyperammonemia in skeletal muscle and myotubes Open

Nicole Welch, Shashi Shekhar Singh, Avinash Kumar, Saugato Rahman Dhruba, Saurabh Mishra , et al. · 2021

Novel AT1R-Allosteric Ligands Mask the Preeclampsia Auto-antibody Epitope and Decrease Angiotensin-induced Vasoconstriction Open

Khuraijam Dhanachandra Singh, Zaira Palomino Jara, Terri J. Harford, Prasenjit Prasad Saha, Triveni R. Pardhi , et al. · 2021

Summary Maternal blood pressure regulation by the hormone angiotensin II (AngII) sustains fetal growth through feto-placental circulation. AngII binding to orthosteric pocket in the angiotensin type 1 receptor (AT1R) induces G protein and …

β-Arrestin–Biased Agonist Targeting the Brain AT <sub>1</sub> R (Angiotensin II Type 1 Receptor) Increases Aversion to Saline and Lowers Blood Pressure in Deoxycorticosterone Acetate–Salt Hypertension Open

Mario Zanaty, Fernando A. C. Seara, Pablo Nakagawa, Guorui Deng, Natalia M. Mathieu , et al. · 2020

Activation of central AT 1 Rs (angiotensin type 1 receptors) is required for the increased blood pressure, polydipsia, and salt intake in deoxycorticosterone acetate (DOCA)–salt hypertension. TRV120027 (TRV027) is an AT 1 R-biased agonist …

Receptors | Angiotensin Receptors Open

Triveni R. Pardhi, Sadashiva S. Karnik · 2020

Class A Orphans (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2020

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [194], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

Angiotensin-Converting Enzyme Inhibitors Versus Angiotensin II Receptor Blockers Open

Ankur Kalra, Edward S. Hawkins, Amy S. Nowacki, Vardhmaan Jain, Alex Milinovich , et al. · 2020

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) utilizes membrane-bound ACE2 (angiotensin-converting enzyme 2) as a functional receptor to gain entry into host cells.An early finding of the coronavirus disease 2019 (COVID-19) …

SARS-CoV-2 and ACE2: The biology and clinical data settling the ARB and ACEI controversy Open

Mina K. Chung, Sadashiva S. Karnik, Joshua Saef, Cornelia C. Bergmann, John Barnard , et al. · 2020

BACKGROUND: SARS-CoV-2 enters cells by binding of its spike protein to angiotensin-converting enzyme 2 (ACE2). Angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin II receptor blockers (ARBs) have been reported to increase ACE2 …

Editorial: Proceedings of KININ2018CLE, Cleveland, Ohio, June 18-20, 2018: A Compendium of the Presentations Open

Alvin H. Schmaier, Marvin T. Nieman, Keith R. McCrae, Sadashiva S. Karnik, João Bosco Pesquero · 2019

EDITORIAL article Front. Med., 22 November 2019Sec. Hematology Volume 6 - 2019 | https://doi.org/10.3389/fmed.2019.00272

Class A Orphans (version 2019.5) in the IUPHAR/BPS Guide to Pharmacology Database Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2019

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [194], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors Open

S P H Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie , et al. · 2019

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacolog…

Class A Orphans (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Open

S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner , et al. · 2019

Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [191], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have rece…

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