Hot Topics in Pharmacology

Coronavrius Information

We are currently collating information related to SARS-CoV-2 and COVID-19 at a dedicated coronavirus information page. This contains details of ligands and targets relevant to COVID-19 and links to useful resources and publications.

Recent publications of interest recommended by NC-IUPHAR

2023: Sep | Aug | Jul | May | Apr | Mar | Feb | Jan
2022: Dec | Nov | Oct

    September 2023


  • How many kinases are druggable? A review of our current understanding.
     Anderson B, Rosston P, Ong HW, Hossain MA, Davis-Gilbert ZW, Drewry DH. How many kinases are druggable? A review of our current understanding. (2023)  Biochem J, 480 (16): 1331-1363. [PMID:37642371]
  • AI-powered therapeutic target discovery.
     Pun FW, Ozerov IV, Zhavoronkov A. AI-powered therapeutic target discovery. (2023)  Trends Pharmacol Sci, 44 (9): 561-572. [PMID:37479540]

    • August 2023


  • What is a cell type?.
     Fleck JS, Camp JG, Treutlein B. What is a cell type?. (2023)  Science, 381 (6659): 733-734. [PMID:37590360]
  • Create a culture of experiments in environmental programs.
     Ferraro PJ, Cherry TL, Shogren JF, Vossler CA, Cason TN, Flint HB, Hochard JP, Johansson-Stenman O, Martinsson P, Murphy JJ et al.. Create a culture of experiments in environmental programs. (2023)  Science, 381 (6659): 735-737. [PMID:37590363]
  • International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily - Update 2023.
     Burris TP, de Vera IMS, Cote I, Flaveny CA, Wanninayake US, Chatterjee A, Walker JK, Steinauer N, Zhang J, Coons LA et al.. International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily - Update 2023. (2023)  Pharmacol Rev, [Epub ahead of print]. [PMID:37586884]
  • A method for structure determination of GPCRs in various states.
     Guo Q, He B, Zhong Y, Jiao H, Ren Y, Wang Q, Ge Q, Gao Y, Liu X, Du Y et al.. A method for structure determination of GPCRs in various states. (2023)  Nat Chem Biol, [Epub ahead of print]. [PMID:37580554]
  • A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.
     Sutherland JJ, Yonchev D, Fekete A, Urban L. A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs. (2023)  Nat Commun, 14 (1): 4323. [PMID:37468498]

    • July 2023


  • Metal-ion transporter SLC39A8 is required for brain manganese uptake and accumulation.
     Liu Q, Jenkitkasemwong S, Prami TA, McCabe SM, Zhao N, Hojyo S, Fukada T, Knutson MD. Metal-ion transporter SLC39A8 is required for brain manganese uptake and accumulation. (2023)  J Biol Chem,: 105078 [Epub ahead of print]. [PMID:37482277]
  • Cross-talk between zinc and calcium regulates ion transport: A role for the zinc receptor, ZnR/GPR39.
     Hershfinkel M. Cross-talk between zinc and calcium regulates ion transport: A role for the zinc receptor, ZnR/GPR39. (2023)  J Physiol, [Epub ahead of print]. DOI: 10.1113/JP283834 [PMID:37462604]
  • Identification of ligand-receptor pairs that drive human astrocyte development.
     Voss AJ, Lanjewar SN, Sampson MM, King A, Hill EJ, Sing A, Sojka C, Bhatia TN, Spangle JM, Sloan SA. Identification of ligand-receptor pairs that drive human astrocyte development. (2023)  Nat Neurosci, [Epub ahead of print]. DOI: 10.1038/s41593-023-01375-8 [PMID:37460808]
  • Jeffrey Clifton Watkins FRS - The father of the glutamate receptor.
     Collingridge GL, Evans RH, Jane DE, Lodge D. Jeffrey Clifton Watkins FRS - The father of the glutamate receptor. (2023)  Neuropharmacology,: 109650 [Epub ahead of print]. [PMID:37474350]
  • The manifold costs of being a non-native English speaker in science.
     Amano T, Ramírez-Castañeda V, Berdejo-Espinola V, Borokini I, Chowdhury S, Golivets M, González-Trujillo JD, Montaño-Centellas F, Paudel K, White RL et al.. The manifold costs of being a non-native English speaker in science. (2023)  PLoS Biol, 21 (7): e3002184. [PMID:37463136]
  • Spartin is a receptor for the autophagy of lipid droplets.
     Spartin is a receptor for the autophagy of lipid droplets. (2023)  Nat Cell Biol, [Epub ahead of print]. [PMID:37474818]
  • Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform.
     Zeghal M, Laroche G, Freitas JD, Wang R, Giguère PM. Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform. (2023)  Nat Commun, 14 (1): 3684. [PMID:37407564]
  • Mammalian type Opsin 5 preferentially activates G14 in Gq-type G proteins triggering intracellular calcium response.
     Sato K, Yamashita T, Ohuchi H. Mammalian type Opsin 5 preferentially activates G14 in Gq-type G proteins triggering intracellular calcium response. (2023)  J Biol Chem,: 105020 [Epub ahead of print]. [PMID:37423300]
  • Cryo-EM structure of GABA transporter 1 reveals substrate recognition and transport mechanism.
     Nayak SR, Joseph D, Höfner G, Dakua A, Athreya A, Wanner KT, Kanner BI, Penmatsa A. Cryo-EM structure of GABA transporter 1 reveals substrate recognition and transport mechanism. (2023)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:37400654]
  • Molecular basis for substrate recognition and transport of human GABA transporter GAT1.
     Zhu A, Huang J, Kong F, Tan J, Lei J, Yuan Y, Yan C. Molecular basis for substrate recognition and transport of human GABA transporter GAT1. (2023)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:37400655]

    • May 2023


  • Advances in Malaria Pharmacology and the online Guide to MALARIA PHARMACOLOGY: IUPHAR Review 38.
     Armstrong JF, Campo B, Alexander SPH, Arendse LB, Cheng X, Davenport AP, Faccenda E, Fidock DA, Godinez-Macias KP, Harding SD et al.. Advances in Malaria Pharmacology and the online Guide to MALARIA PHARMACOLOGY: IUPHAR Review 38. (2023)  Br J Pharmacol, [Epub ahead of print]. [PMID:37197802]
  • The VGNC: expanding standardized vertebrate gene nomenclature.
     Jones TEM, Yates B, Braschi B, Gray K, Tweedie S, Seal RL, Bruford EA. The VGNC: expanding standardized vertebrate gene nomenclature. (2023)  Genome Biol, 24 (1): 115. [PMID:37173739]
  • A small-molecule PI3Kα activator for cardioprotection and neuroregeneration.
     Gong GQ, Bilanges B, Allsop B, Masson GR, Roberton V, Askwith T, Oxenford S, Madsen RR, Conduit SE, Bellini D et al.. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. (2023)  Nature, [Epub ahead of print]. [PMID:37225977]
  • Bilirubin gates the TRPM2 channel as a direct agonist to exacerbate ischemic brain damage.
     Liu HW, Gong LN, Lai K, Yu XF, Liu ZQ, Li MX, Yin XL, Liang M, Shi HS, Jiang LH et al.. Bilirubin gates the TRPM2 channel as a direct agonist to exacerbate ischemic brain damage. (2023)  Neuron, 111 (10): 1609-1625.e6. [PMID:36921602]
  • FDA approves first-in-class NK3 receptor antagonist for hot flushes.
     Mullard A. FDA approves first-in-class NK3 receptor antagonist for hot flushes. (2023)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:37208488]
  • Identification and Classification of Papain-like Cysteine Proteinases.
     Ozhelvaci F, Steczkiewicz K. Identification and Classification of Papain-like Cysteine Proteinases. (2023)  J Biol Chem,: 104801 [Epub ahead of print]. [PMID:37164157]

    • April 2023


  • Structural basis for severe pain caused by mutations in the S4-S5 linkers of voltage-gated sodium channel NaV1.7.
     Wisedchaisri G, Gamal El-Din TM, Zheng N, Catterall WA. Structural basis for severe pain caused by mutations in the S4-S5 linkers of voltage-gated sodium channel NaV1.7. (2023)  Proc Natl Acad Sci U S A, 120 (14): e2219624120. [PMID:36996107]
  • Orphan receptor GPR158 serves as a metabotropic glycine receptor: mGlyR.
     Laboute T, Zucca S, Holcomb M, Patil DN, Garza C, Wheatley BA, Roy RN, Forli S, Martemyanov KA. Orphan receptor GPR158 serves as a metabotropic glycine receptor: mGlyR. (2023)  Science, 379 (6639): 1352-1358. [PMID:36996198]
  • ATP-releasing SWELL1 channel in spinal microglia contributes to neuropathic pain.
     Chu J, Yang J, Zhou Y, Chen J, Chen KH, Zhang C, Cheng HY, Koylass N, Liu JO, Guan Y et al.. ATP-releasing SWELL1 channel in spinal microglia contributes to neuropathic pain. (2023)  Sci Adv, 9 (13): eade9931. [PMID:36989353]
  • SVEP1 is an endogenous ligand for the orphan receptor PEAR1.
     Elenbaas JS, Pudupakkam U, Ashworth KJ, Kang CJ, Patel V, Santana K, Jung IH, Lee PC, Burks KH, Amrute JM et al.. SVEP1 is an endogenous ligand for the orphan receptor PEAR1. (2023)  Nat Commun, 14 (1): 850. [PMID:36792666]
  • Structural insights into constitutive activity of 5-HT6 receptor.
     He L, Zhao Q, Qi J, Wang Y, Han W, Chen Z, Cong Y, Wang S. Structural insights into constitutive activity of 5-HT6 receptor. (2023)  Proc Natl Acad Sci U S A, 120 (14): e2209917120. [PMID:36989299]

    • March 2023


  • The evolution of antibiotic resistance is associated with collateral drug phenotypes in Mycobacterium tuberculosis.
     Waller NJE, Cheung CY, Cook GM, McNeil MB. The evolution of antibiotic resistance is associated with collateral drug phenotypes in Mycobacterium tuberculosis. (2023)  Nat Commun, 14 (1): 1517. [PMID:36934122]
  • A broad-spectrum synthetic antibiotic that does not evoke bacterial resistance.
     Heithoff DM, Mahan SP, Barnes V L, Leyn SA, George CX, Zlamal JE, Limwongyut J, Bazan GC, Fried JC, Fitzgibbons LN et al.. A broad-spectrum synthetic antibiotic that does not evoke bacterial resistance. (2023)  EBioMedicine, 89: 104461. [PMID:36801104]
  • A reference cell tree will serve science better than a reference cell atlas
    Domcke S, Shendure J. A reference cell tree will serve science better than a reference cell atlas. (2023)  Cell, 186 (6): 1103-1114. [PMID:36931241]
    Lowe D. Organizing Our Thoughts About Cells - Finally.  In the Pipeline, https://www.science.org/content/blog-post/organizing-our-thoughts-about-cells-finally
  • A community Biased Signaling Atlas.
     Caroli J, Mamyrbekov A, Harpsøe K, Gardizi S, Dörries L, Ghosh E, Hauser AS, Kooistra AJ, Gloriam DE. A community Biased Signaling Atlas. (2023)  Nat Chem Biol, [Epub ahead of print]. [PMID:36973443]
  • Purinergic GPCR-integrin interactions drive pancreatic cancer cell invasion.
     Tomas Bort E, Joseph MD, Wang Q, Carter EP, Roth NJ, Gibson J, Samadi A, Kocher HM, Simoncelli S, McCormick PJ et al.. Purinergic GPCR-integrin interactions drive pancreatic cancer cell invasion. (2023)  Elife, 12 [Epub ahead of print]. [PMID:36942939]
  • Getting the SMILES right: identifying inconsistent chemical identities in the ECHA database, PubChem and the CompTox Chemicals Dashboard.
     Glüge J, McNeill K, Scheringer M. Getting the SMILES right: identifying inconsistent chemical identities in the ECHA database, PubChem and the CompTox Chemicals Dashboard. (2023)  Environ. Sci.: Adv.,. DOI: 10.1039/D2VA00225F
  • Autoregulation of GPCR signalling through the third intracellular loop.
     Sadler F, Ma N, Ritt M, Sharma Y, Vaidehi N, Sivaramakrishnan S. Autoregulation of GPCR signalling through the third intracellular loop. (2023)  Nature, [Epub ahead of print]. [PMID:36890236]
  • Chemistry, structure and function of approved oligonucleotide therapeutics.
     Egli M, Manoharan M. Chemistry, structure and function of approved oligonucleotide therapeutics. (2023)  Nucleic Acids Res, [Epub ahead of print]. [PMID:36881759]
  • Unsaturated bond recognition leads to biased signal in a fatty acid receptor.
     Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD et al.. Unsaturated bond recognition leads to biased signal in a fatty acid receptor. (2023)  Science,: eadd6220 [Epub ahead of print]. [PMID:36862765]
  • Amyotrophic lateral sclerosis: a neurodegenerative disorder poised for successful therapeutic translation.
     Mead RJ, Shan N, Reiser HJ, Marshall F, Shaw PJ. Amyotrophic lateral sclerosis: a neurodegenerative disorder poised for successful therapeutic translation. (2023)  Nat Rev Drug Discov, 22 (3): 185-212. [PMID:36543887]
  • Methods and applications for single-cell and spatial multi-omics.
     Vandereyken K, Sifrim A, Thienpont B, Voet T. Methods and applications for single-cell and spatial multi-omics. (2023)  Nat Rev Genet,: 1-22 [Epub ahead of print]. [PMID:36864178]

    • February 2023


  • Structural basis of efficacy-driven ligand selectivity at GPCRs.
     Powers AS, Pham V, Burger WAC, Thompson G, Laloudakis Y, Sexton PM, Paul SM, Christopoulos A, Thal DM, Felder CC et al.. Structural basis of efficacy-driven ligand selectivity at GPCRs. (2023)  Nat Chem Biol, [Epub ahead of print]. [PMID:36782010]
  • The case for standardizing gene nomenclature in vertebrates
    McCarthy FM, Jones TEM, Kwitek AE, Smith CL, Vize PD, Westerfield M, Bruford EA. The case for standardizing gene nomenclature in vertebrates. (2023)  Nature, 614 (7948): E31-E32. [PMID:36792746]
    VGNC. A Debate About Vertebrate Gene Naming.  https://blog.genenames.org, https://blog.genenames.org/vgnc/2023/2/16/A-Debate-About-Vertebrate-Gene-Naming
  • Uncovering the Heritable Components of Multimorbidities and Disease Trajectories: A Nationwide Cohort Study.
     Westergaard D, Jørgensen FH, Waaben J, Lademann M, Hansen TF, Cremers J, Ostrowsk SRi, Pedersen OBV, Danish Blood Donor Study Genomic Consortium et al.. Uncovering the Heritable Components of Multimorbidities and Disease Trajectories: A Nationwide Cohort Study. (2023)  medRxiv, Preprint. DOI: 10.1101/2023.02.08.23285642
  • Investigating the potential of GalR2 as a drug target for neuropathic pain.
     Rich K, Rehman S, Jerman J, Wilkinson G. Investigating the potential of GalR2 as a drug target for neuropathic pain. (2022)  Neuropeptides, 98: 102311 [Epub ahead of print]. [PMID:36580831]
  • The evolving role of investigative toxicology in the pharmaceutical industry.
     Pognan F, Beilmann M, Boonen HCM, Czich A, Dear G, Hewitt P, Mow T, Oinonen T, Roth A, Steger-Hartmann T et al.. The evolving role of investigative toxicology in the pharmaceutical industry. (2023)  Nat Rev Drug Discov,: 1-19 [Epub ahead of print]. [PMID:36781957]
  • Lies and Liabilities: Computational Assessment of High-Throughput Screening Hits to Identify Artifact Compounds.
     Alves V, Yasgar A, Wellnitz J, Bantukallu G, Rath M, Insilicall RB, Capuzzi S, Simeonov A, Muratov E, Zakharov A, Tropsha A. Lies and Liabilities: Computational Assessment of High-Throughput Screening Hits to Identify Artifact Compounds. (2023)  ChemRxiv, Preprint. DOI: 10.26434/chemrxiv-2023-r78sj
  • AI-enhanced protein design makes proteins that have never existed.
     Eisenstein M. AI-enhanced protein design makes proteins that have never existed. (2023)  Nat Biotechnol,: 1-3 [Epub ahead of print]. [PMID:36823357]
  • Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139.
     Pallareti L, Rath TF, Trapkov B, Tsonkov T, Nielsen AT, Harpsøe K, Gentry PR, Bräuner-Osborne H, Gloriam DE, Foster SR. Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139. (2023)  Eur J Pharmacol, 943: 175553 [Epub ahead of print]. [PMID:36736525]
  • Pharmacogenomics: current status and future perspectives.
     Pirmohamed M. Pharmacogenomics: current status and future perspectives. (2023)  Nat Rev Genet, [Epub ahead of print]. [PMID:36707729]
  • A 12-gene pharmacogenetic panel to prevent adverse drug reactions: an open-label, multicentre, controlled, cluster-randomised crossover implementation study.
     Swen JJ, van der Wouden CH, Manson LE, Abdullah-Koolmees H, Blagec K, Blagus T, Böhringer S, Cambon-Thomsen A, Cecchin E, Cheung KC et al.. A 12-gene pharmacogenetic panel to prevent adverse drug reactions: an open-label, multicentre, controlled, cluster-randomised crossover implementation study. (2023)  Lancet, 401 (10374): 347-356. [PMID:36739136]

    • January 2023


  • Degrader-Antibody Conjugates: Emerging New Modality.
     Hong KB, An H. Degrader-Antibody Conjugates: Emerging New Modality. (2023)  J Med Chem, 66 (1): 140-148. [PMID:36580273]
  • Metabolites as signalling molecules.
     Baker SA, Rutter J. Metabolites as signalling molecules. (2023)  Nat Rev Mol Cell Biol, [Epub ahead of print]. [PMID:36635456]
  • Structures of the entire human opioid receptor family.
     Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y et al.. Structures of the entire human opioid receptor family. (2023)  Cell, 186 (2): 413-427.e17. [PMID:36638794]
  • Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
     Londregan AT, Aitmakhanova K, Bennett J, Byrnes LJ, Canterbury DP, Cheng X, Christott T, Clemens J, Coffey SB, Dias JM et al.. Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4. (2023)  J Med Chem, 66 (1): 460-472. [PMID:36562986]
  • Structural basis of odorant recognition by a human odorant receptor.
     Billesbølle CB, de March CA, van der Velden WJC, Ma N, Tewari, del Torrent JCL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A. Structural basis of odorant recognition by a human odorant receptor. (2023)  bioRxiv, Preprint. DOI: 10.1101/2022.12.20.520951
  • A proteome-wide atlas of drug mechanism of action.
     Mitchell DC, Kuljanin M, Li J, Van Vranken JG, Bulloch N, Schweppe DK, Huttlin EL, Gygi SP. A proteome-wide atlas of drug mechanism of action. (2023)  Nat Biotechnol, [Epub ahead of print]. [PMID:36593396]

    • December 2022


  • Pharos 2023: an integrated resource for the understudied human proteome.
     Kelleher KJ, Sheils TK, Mathias SL, Yang JJ, Metzger VT, Siramshetty VB, Nguyen DT, Jensen LJ, Vidović D, Schürer SC et al.. Pharos 2023: an integrated resource for the understudied human proteome. (2022)  Nucleic Acids Res, [Epub ahead of print]. DOI: 10.1093/nar/gkac1033
  • DrugCentral 2023 extends human clinical data and integrates veterinary drugs.
     Avram S, Wilson TB, Curpan R, Halip L, Borota A, Bora A, Bologa CG, Holmes J, Knockel J, Yang JJ et al.. DrugCentral 2023 extends human clinical data and integrates veterinary drugs. (2022)  Nucleic Acids Res, [Epub ahead of print]. [PMID:36484092]
  • Hot Topics: FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2

    Comments by the Guide to Pharmacology Curation Team, University of Edinburgh

    This manuscript reports on comprehensive and compelling experimental evidence and translational data from a retrospective review of clinical registries, which show that pharmacological inhibition of the farnesoid X receptor (FXR; using the FXR antagonist ursodeoxycholic acid/UDCA) could be a novel intervention for the prevention or treatment of COVID-19. The in vitro and in vivo studies show that FXR antagonism reduces ACE2 expression, which subsequently reduces SARS-CoV-2's ability to infect tissues including lung, liver and gastrointestinal tract.. Read the full article on our blog

    • November 2022


  • GPCRdb in 2023: state-specific structure models using AlphaFold2 and new ligand resources.
     Pándy-Szekeres G, Caroli J, Mamyrbekov A, Kermani AA, Keserű GM, Kooistra AJ, Gloriam DE. GPCRdb in 2023: state-specific structure models using AlphaFold2 and new ligand resources. (2022)  Nucleic Acids Res, [Epub ahead of print]. [PMID:36395823]
  • Colon tumour cell death causes mTOR dependence by paracrine P2X4 stimulation.
     Schmitt M, Ceteci F, Gupta J, Pesic M, Böttger TW, Nicolas AM, Kennel KB, Engel E, Schewe M, Callak Kirisözü A et al.. Colon tumour cell death causes mTOR dependence by paracrine P2X4 stimulation. (2022)  Nature, [Epub ahead of print]. [PMID:36385525]
  • Beyond PI3Ks: targeting phosphoinositide kinases in disease.
     Burke JE, Triscott J, Emerling BM, Hammond GRV. Beyond PI3Ks: targeting phosphoinositide kinases in disease. (2022)  Nat Rev Drug Discov,: 1-30 [Epub ahead of print]. [PMID:36376561]
  • Reclassifying plasmacytoid dendritic cells as innate lymphocytes.
     Ziegler-Heitbrock L, Ohteki T, Ginhoux F, Shortman K, Spits H. Reclassifying plasmacytoid dendritic cells as innate lymphocytes. (2022)  Nat Rev Immunol, [Epub ahead of print]. [PMID:36380022]
  • Structure determination of inactive-state GPCRs with a universal nanobody.
     Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G. Structure determination of inactive-state GPCRs with a universal nanobody. (2022)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:36396979]

    • October 2022


  • Genenames.org: the HGNC resources in 2023.
     Seal RL, Braschi B, Gray K, Jones TEM, Tweedie S, Haim-Vilmovsky L, Bruford EA. Genenames.org: the HGNC resources in 2023. (2022)  Nucleic Acids Res, [Epub ahead of print]. [PMID:36243972]
  • Identification of proteomic landscape of drug-binding proteins in live cells by proximity-dependent target ID.
     Kwak C, Park C, Ko M, Im CY, Moon H, Park YH, Kim SY, Lee S, Kang MG, Kwon HJ et al.. Identification of proteomic landscape of drug-binding proteins in live cells by proximity-dependent target ID. (2022)  Cell Chem Biol, [Epub ahead of print]. [PMID:36272407]