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We collate information related to SARS-CoV-2 and COVID-19 on 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

2025: May | Apr | Mar | Feb | Jan
2024: Dec | Nov | Oct | Sep | Aug | Jul | Jun | May

    May 2025


  • Preclinical pharmacokinetics, metabolism, and disposition of NXE0041178, a novel orally bioavailable agonist of the GPR52 receptor with potential for treatment of schizophrenia and related psychiatric disorders.
     Poulter S, Austin N, Watson SP, Bucknell SJ, O'Brien MA, Tolonen A, Lassila T, Stott LA, Mead A, MacSweeney C. Preclinical pharmacokinetics, metabolism, and disposition of NXE0041178, a novel orally bioavailable agonist of the GPR52 receptor with potential for treatment of schizophrenia and related psychiatric disorders. (2025)  Xenobiotica,: 1-24 [Epub ahead of print]. [PMID:40367121]
  • The genetic interaction map of the human solute carrier superfamily.
     Wolf G, Leippe P, Onstein S, Goldmann U, Frommelt F, Teoh ST, Girardi E, Wiedmer T, Superti-Furga G. The genetic interaction map of the human solute carrier superfamily. (2025)  Mol Syst Biol, [Epub ahead of print]. [PMID:40355755]
  • Data- and knowledge-derived functional landscape of human solute carriers.
     Goldmann U, Wiedmer T, Garofoli A, Sedlyarov V, Bichler M, Haladik B, Wolf G, Christodoulaki E, Ingles-Prieto A, Ferrada E et al.. Data- and knowledge-derived functional landscape of human solute carriers. (2025)  Mol Syst Biol, [Epub ahead of print]. [PMID:40355757]
  • The solute carrier superfamily interactome.
     Frommelt F, Ladurner R, Goldmann U, Wolf G, Ingles-Prieto A, Lineiro-Retes E, Gelová Z, Hopp AK, Christodoulaki E, Teoh ST et al.. The solute carrier superfamily interactome. (2025)  Mol Syst Biol, [Epub ahead of print]. [PMID:40355756]
  • PLA2G15 is a BMP hydrolase and its targeting ameliorates lysosomal disease.
     Nyame K, Xiong J, Alsohybe HN, de Jong APH, Peña IV, de Miguel R, Brummelkamp TR, Hartmann G, Nijman SMB, Raaben M et al.. PLA2G15 is a BMP hydrolase and its targeting ameliorates lysosomal disease. (2025)  Nature, [Epub ahead of print]. [PMID:40335701]
  • Activation of lysosomal iron triggers ferroptosis in cancer.
     Cañeque T, Baron L, Müller S, Carmona A, Colombeau L, Versini A, Solier S, Gaillet C, Sindikubwabo F, Sampaio JL et al.. Activation of lysosomal iron triggers ferroptosis in cancer. (2025)  Nature, [Epub ahead of print]. [PMID:40335696]
  • At The Interface: Small-Molecule Inhibitors of Soluble Cytokines.
     Raavi, Koehler AN, Vegas AJ. At The Interface: Small-Molecule Inhibitors of Soluble Cytokines. (2025)  Chem Rev, 125 (9): 4528-4568. [PMID:40233276]
  • The structure of human sweetness
    Juen Z, Lu Z, Yu R, Chang AN, Wang B, Fitzpatrick AWP, Zuker CS. The structure of human sweetness. (2025)  Cell, [Epub ahead of print]. [PMID:40339580]
    Dolgin E. How we taste sweetness: long-sought structure of human receptor mapped at last. (2025)  Nature, [Epub ahead of print]. [PMID:40335811]

    • April 2025


  • Chemistry Meets Biology: Cross-Disciplinary Evaluation of Drug Discovery Databases.
     Kyrsanov AV, Tkachenko IV, Shtil NA, Gavrilenko KS, Pashenko OY, Judd DB, Ryabukhin SV, Volochnyuk DM. Chemistry Meets Biology: Cross-Disciplinary Evaluation of Drug Discovery Databases. (2025)  J Chem Inf Model, 65 (8): 4057-4066. [PMID:40197979]
  • Cryoelectron microscopy as a tool for illuminating activation mechanisms of human class A orphan G protein-coupled receptors.
     Russell IC, Lee D, Wootten D, Sexton PM, Bumbak F. Cryoelectron microscopy as a tool for illuminating activation mechanisms of human class A orphan G protein-coupled receptors. (2025)  Pharmacol Rev, 77 (3): 100056 [Epub ahead of print]. [PMID:40286430]
  • The aryl hydrocarbon receptor: a rehabilitated target for therapeutic immune modulation.
     Polonio CM, McHale KA, Sherr DH, Rubenstein D, Quintana FJ. The aryl hydrocarbon receptor: a rehabilitated target for therapeutic immune modulation. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:40247142]
  • Enzymes in secondary pharmacology screening panels: is there room for improvement?.
     Maciag M, Karamyan VT. Enzymes in secondary pharmacology screening panels: is there room for improvement?. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:40263626]
  • Huge reproducibility project fails to validate dozens of biomedical studies.
     de Oliveira Andrade R. Huge reproducibility project fails to validate dozens of biomedical studies. (2025)  Nature, [Epub ahead of print]. [PMID:40281293]
  • Structural basis for the activation of proteinase-activated receptors PAR1 and PAR2.
     Lyu Z, Lyu X, Malyutin AG, Xia G, Carney D, Alves VM, Falk M, Arora N, Zou H, McGrath AP et al.. Structural basis for the activation of proteinase-activated receptors PAR1 and PAR2. (2025)  Nat Commun, 16 (1): 3931. [PMID:40287415]
  • Structure-based discovery of novel non-covalent small molecule inhibitors of USP30.
     Anbazhagan P, Anantharajan J, Fulwood J, Low CH, Baburajendran N, Foo K, Xu W. Structure-based discovery of novel non-covalent small molecule inhibitors of USP30. (2025)  J Comput Aided Mol Des, 39 (1): 19. [PMID:40274689]
  • Understanding peptide hormones: from precursor proteins to bioactive molecules.
     Coassolo L, Wiggenhorn A, Svensson KJ. Understanding peptide hormones: from precursor proteins to bioactive molecules. (2025)  Trends Biochem Sci, [Epub ahead of print]. [PMID:40234176]
  • Vascular motion in the dorsal root ganglion sensed by Piezo2 in sensory neurons triggers episodic neuropathic pain.
     Xie W, Lückemeyer DD, Qualls KA, Prudente AS, Berta T, Gu M, Strong JA, Dong X, Zhang JM. Vascular motion in the dorsal root ganglion sensed by Piezo2 in sensory neurons triggers episodic neuropathic pain. (2025)  Neuron, [Epub ahead of print]. [PMID:40154477]
  • Enteric neuronal Piezo1 maintains mechanical and immunological homeostasis by sensing force.
     Xie Z, Rose L, Feng J, Zhao Y, Lu Y, Kane H, Hibberd TJ, Hu X, Wang Z, Zang K et al.. Enteric neuronal Piezo1 maintains mechanical and immunological homeostasis by sensing force. (2025)  Cell, [Epub ahead of print]. [PMID:40132579]

    • March 2025


  • Immune regulation by the SUMO family.
     Tharuka MDN, Courelli AS, Chen Y. Immune regulation by the SUMO family. (2025)  Nat Rev Immunol, [Epub ahead of print]. [PMID:40108400]
  • Molecular glues that inhibit deubiquitylase activity and inflammatory signaling.
     Chandler F, Reddy PAN, Bhutda S, Ross RL, Datta A, Walden M, Walker K, Di Donato S, Cassel JA, Prakesch MA et al.. Molecular glues that inhibit deubiquitylase activity and inflammatory signaling. (2025)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:40097626]
  • Complex G-protein signaling of the adhesion GPCR, ADGRA3.
     Bagger SM, Schihada H, Walser ALS, Drzazga AK, Grätz L, Palmisano T, Kuhn CK, Mavri M, Mølleskov-Jensen AS, Tall GG et al.. Complex G-protein signaling of the adhesion GPCR, ADGRA3. (2025)  J Biol Chem,: 108441 [Epub ahead of print]. [PMID:40127866]
  • The structural diversity of psychedelic drug actions revealed.
     Gumpper RH, Jain MK, Kim K, Sun R, Sun N, Xu Z, DiBerto JF, Krumm BE, Kapolka NJ, Kaniskan HÜ et al.. The structural diversity of psychedelic drug actions revealed. (2025)  Nat Commun, 16 (1): 2734. [PMID:40108183]
  • Computational drug repurposing: approaches, evaluation of in silico resources and case studies.
     Tanoli Z, Fernández-Torras A, Özcan UO, Kushnir A, Nader KM, Gadiya Y, Fiorenza L, Ianevski A, Vähä-Koskela M, Miihkinen M et al.. Computational drug repurposing: approaches, evaluation of in silico resources and case studies. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:40102635]
  • Genetic causes of obesity: mapping a path forward.
     Loos RJF. Genetic causes of obesity: mapping a path forward. (2025)  Trends Mol Med, [Epub ahead of print]. [PMID:40089418]
  • Sensing ceramides by CYSLTR2 and P2RY6 to aggravate atherosclerosis.
     Zhang S, Lin H, Wang J, Rui J, Wang T, Cai Z, Huang S, Gao Y, Ma T, Fan R et al.. Sensing ceramides by CYSLTR2 and P2RY6 to aggravate atherosclerosis. (2025)  Nature, [Epub ahead of print]. [PMID:40049228]
  • Metabolic signaling of ceramides through the FPR2 receptor inhibits adipocyte thermogenesis.
     Lin H, Ma C, Cai K, Guo L, Wang X, Lv L, Zhang C, Lin J, Zhang D, Ye C et al.. Metabolic signaling of ceramides through the FPR2 receptor inhibits adipocyte thermogenesis. (2025)  Science,: eado4188 [Epub ahead of print]. [PMID:40080544]
  • Post-translational modifications orchestrate the intrinsic signaling bias of GPR52.
     Zhang B, Ge W, Ma M, Li S, Yu J, Yang G, Wang H, Li J, Li Q, Zeng R et al.. Post-translational modifications orchestrate the intrinsic signaling bias of GPR52. (2025)  Nat Chem Biol, [Epub ahead of print]. [PMID:40087539]
  • Regulation of mammalian cellular metabolism by endogenous cyanide production.
     Zuhra K, Petrosino M, Janickova L, Petric J, Ascenção K, Vignane T, Khalaf M, Philipp TM, Ravani S, Anand A et al.. Regulation of mammalian cellular metabolism by endogenous cyanide production. (2025)  Nat Metab, 7 (3): 531-555. [PMID:40033006]
  • Fifteen years of ChEMBL and its role in cheminformatics and drug discovery.
     Zdrazil B. Fifteen years of ChEMBL and its role in cheminformatics and drug discovery. (2025)  J Cheminform, 17 (1): 32. [PMID:40065463]
  • GPCR drug discovery: new agents, targets and indications.
     Lorente JS, Sokolov AV, Ferguson G, Schiöth HB, Hauser AS, Gloriam DE. GPCR drug discovery: new agents, targets and indications. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:40033110]
  • International Union of Basic and Clinical Pharmacology. CXIX. Fundamental insights and clinical relevance regarding the carnitine palmitoyltransferase family of enzymes.
     Rodríguez-Rodríguez R, Baena M, Zagmutt S, Paraiso WK, Reguera AC, Fadó R, Casals N. International Union of Basic and Clinical Pharmacology. CXIX. Fundamental insights and clinical relevance regarding the carnitine palmitoyltransferase family of enzymes. (2025)  Pharmacol Rev, 77 (3): 100051 [Epub ahead of print]. [PMID:40106976]

    • February 2025


  • A five-drug class model using routinely available clinical features to optimise prescribing in type 2 diabetes: a prediction model development and validation study.
     Dennis JM, Young KG, Cardoso P, Güdemann LM, McGovern AP, Farmer A, Holman RR, Sattar N, McKinley TJ, Pearson ER et al.. A five-drug class model using routinely available clinical features to optimise prescribing in type 2 diabetes: a prediction model development and validation study. (2025)  Lancet, 405 (10480): 701-714. [PMID:40020703]
  • NAPE-PLD is target of thiazide diuretics
    Chiarugi S, Margheriti F, De Lorenzi V, Martino E, Margheritis EG, Moscardini A, Marotta R, Chaves-Sanjuan A, Del Seppia C, Federighi G et al.. NAPE-PLD is target of thiazide diuretics. (2025)  Cell Chem Biol, [Epub ahead of print]. [PMID:39999832]
    Lowe D. The Thiazide Target, At Last.  In the Pipeline, https://www.science.org/content/blog-post/thiazide-target-last
  • Dozens of new obesity drugs are coming: these are the ones to watch.
     Dolgin E. Dozens of new obesity drugs are coming: these are the ones to watch. (2025)  Nature, 638 (8050): 308-310. [PMID:39939789]
  • Structural insights into TRPV2 modulation by probenecid.
     Rocereta JA, Sturhahn T, Pumroy RA, Fricke TC, Herzog C, Leffler A, Moiseenkova-Bell V. Structural insights into TRPV2 modulation by probenecid. (2025)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:39972168]
  • Snapshots of acyl carrier protein shuttling in human fatty acid synthase.
     Schultz K, Costa-Pinheiro P, Gardner L, Pinheiro LV, Ramirez-Solis J, Gardner SM, Wellen KE, Marmorstein R. Snapshots of acyl carrier protein shuttling in human fatty acid synthase. (2025)  Nature, [Epub ahead of print]. [PMID:39979457]
  • Structural basis for channel gating and blockade in tri-heteromeric GluN1-2B-2D NMDA receptor.
     Kang H, Epstein M, Banke TG, Perszyk R, Simorowski N, Paladugu S, Liotta DC, Traynelis SF, Furukawa H. Structural basis for channel gating and blockade in tri-heteromeric GluN1-2B-2D NMDA receptor. (2025)  Neuron, [Epub ahead of print]. [PMID:39954679]
  • Thalamic opioids from POMC satiety neurons switch on sugar appetite.
     Minère M, Wilhelms H, Kuzmanovic B, Lundh S, Fusca D, Claßen A, Shtiglitz S, Prilutski Y, Talpir I, Tian L et al.. Thalamic opioids from POMC satiety neurons switch on sugar appetite. (2025)  Science, 387 (6735): 750-758. [PMID:39946455]
  • Deep-tissue transcriptomics and subcellular imaging at high spatial resolution.
     Gandin V, Kim J, Yang LZ, Lian Y, Kawase T, Hu A, Rokicki K, Fleishman G, Tillberg P, Castrejon AA et al.. Deep-tissue transcriptomics and subcellular imaging at high spatial resolution. (2025)  Science,: eadq2084 [Epub ahead of print]. [PMID:39977545]
  • Disease diagnostics using machine learning of B cell and T cell receptor sequences.
     Zaslavsky ME, Craig E, Michuda JK, Sehgal N, Ram-Mohan N, Lee JY, Nguyen KD, Hoh RA, Pham TD, Röltgen K et al.. Disease diagnostics using machine learning of B cell and T cell receptor sequences. (2025)  Science, 387 (6736): eadp2407. [PMID:39977494]

    • January 2025


  • Identification of a binding site for small molecule inhibitors targeting human TRPM4.
     Ekundayo B, Arullampalam P, Gerber CE, Hämmerli AF, Guichard S, Boukenna M, Ross-Kaschitza D, Lochner M, Rougier JS, Stahlberg H et al.. Identification of a binding site for small molecule inhibitors targeting human TRPM4. (2025)  Nat Commun, 16 (1): 833. [PMID:39828793]
  • Cryo-EM structure of an activated GPR4-Gs signaling complex.
     Ma Y, Wang Y, Tang M, Weng Y, Chen Y, Xu Y, An S, Wu Y, Zhao S, Xu H et al.. Cryo-EM structure of an activated GPR4-Gs signaling complex. (2025)  Nat Commun, 16 (1): 605. [PMID:39799123]
  • Structures of ATP-binding cassette transporter ABCC1 reveal the molecular basis of cyclic dinucleotide cGAMP export.
     Shinde O, Boyer JA, Cambier S, VanPortfliet JJ, Sui X, Yadav GP, Viverette EG, Borgnia MJ, West AP, Zhang Q et al.. Structures of ATP-binding cassette transporter ABCC1 reveal the molecular basis of cyclic dinucleotide cGAMP export. (2025)  Immunity, 58 (1): 59-73.e5. [PMID:39765229]
  • Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes.
     Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, Styrpejko D, Ramos-Gonzalez N, Woo S, Villers K et al.. Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes. (2025)  Nat Chem Biol, [Epub ahead of print]. [PMID:39775170]
  • Cryo-EM reveals cholesterol binding in the lysosomal GPCR-like protein LYCHOS.
     Zhao J, Shen Q, Yong X, Li X, Tian X, Sun S, Xu Z, Zhang X, Zhang L, Yang H et al.. Cryo-EM reveals cholesterol binding in the lysosomal GPCR-like protein LYCHOS. (2025)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:39824976]
  • 2024 FDA approvals exceed average number but have lower sales projections.
     Baedeker M, Ringel MS, Möller CC. 2024 FDA approvals exceed average number but have lower sales projections. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:39824959]
  • Molecular architecture of human LYCHOS involved in lysosomal cholesterol signaling.
     Xiong Q, Zhu Z, Li T, Li X, Zhou Z, Chao Y, Yang C, Feng S, Qu Q, Li D. Molecular architecture of human LYCHOS involved in lysosomal cholesterol signaling. (2025)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:39824977]
  • PlexinD1 is a driver and a therapeutic target in advanced prostate cancer.
     Wei J, Wang J, Guan W, Li J, Pu T, Corey E, Lin TP, Gao AC, Wu BJ. PlexinD1 is a driver and a therapeutic target in advanced prostate cancer. (2025)  EMBO Mol Med, 17 (2): 336-364. [PMID:39748059]
  • Wide-ranging cellular functions of ion channels and lipid scramblases in the structurally related TMC, TMEM16 and TMEM63 families.
     Jan LY, Jan YN. Wide-ranging cellular functions of ion channels and lipid scramblases in the structurally related TMC, TMEM16 and TMEM63 families. (2025)  Nat Struct Mol Biol, 32 (2): 222-236. [PMID:39715905]
  • A propofol binding site in the voltage sensor domain mediates inhibition of HCN1 channel activity.
     Burtscher V, Wang L, Cowgill J, Chen ZW, Edge C, Smith E, Chang Y, Delemotte L, Evers AS, Chanda B. A propofol binding site in the voltage sensor domain mediates inhibition of HCN1 channel activity. (2025)  Sci Adv, 11 (1): eadr7427. [PMID:39752505]
  • Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery.
     Conflitti P, Lyman E, Sansom MSP, Hildebrand PW, Gutiérrez-de-Terán H, Carloni P, Ansell TB, Yuan S, Barth P, Robinson AS et al.. Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:39747671]
  • 2024 FDA approvals.
     Mullard A. 2024 FDA approvals. (2025)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:39747473]
  • Insights into phosphate homeostasis regulation by XPR1.
     Bondeson DP. Insights into phosphate homeostasis regulation by XPR1. (2025)  Nat Struct Mol Biol, 32 (1): 5-7. [PMID:39738853]
  • Lipidomic profiling of mouse brain and human neuron cultures reveals a role for Mboat7 in mTOR-dependent neuronal migration.
     Tang I, Nisal A, Reed A, Ware TB, Johansen A, Zaki MS, Cravatt BF, Gleeson JG. Lipidomic profiling of mouse brain and human neuron cultures reveals a role for Mboat7 in mTOR-dependent neuronal migration. (2025)  Sci Transl Med, 17 (779): eadp5247. [PMID:39742503]

    • December 2024


  • DEP-1 is a brain insulin receptor phosphatase that prevents the simultaneous activation of counteracting metabolic pathways.
     Chopra S, Kadiri OL, Ulke J, Hauffe R, Jonas W, Cheshmeh S, Schmidt L, Bishop CA, Yagoub S, Schell M et al.. DEP-1 is a brain insulin receptor phosphatase that prevents the simultaneous activation of counteracting metabolic pathways. (2024)  Cell Rep, 43 (12): 114984 [Epub ahead of print]. [PMID:39589923]
  • Structural insights into endogenous ligand selectivity and activation mechanisms of FFAR1 and FFAR2.
     Ke Y, Huang Y, Yi C, Ma L, Chu X, Wu B, Zhao Q, Han S. Structural insights into endogenous ligand selectivity and activation mechanisms of FFAR1 and FFAR2. (2024)  Cell Rep, 43 (12): 115024. [PMID:39616615]
  • Mutant-selective AKT inhibition through lysine targeting and neo-zinc chelation.
     Craven GB, Chu H, Sun JD, Carelli JD, Coyne B, Chen H, Chen Y, Ma X, Das S, Kong W et al.. Mutant-selective AKT inhibition through lysine targeting and neo-zinc chelation. (2024)  Nature, [Epub ahead of print]. [PMID:39506119]
  • Adipokines: masterminds of metabolic inflammation.
     Tilg H, Ianiro G, Gasbarrini A, Adolph TE. Adipokines: masterminds of metabolic inflammation. (2024)  Nat Rev Immunol, [Epub ahead of print]. [PMID:39511425]
  • A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells.
     Talele S, Gonzalez S, Trudeau J, Junaid A, Loy CA, Altman RA, Sjögren B. A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells. (2024)  J Med Chem, 67 (22): 20343-20352. [PMID:39547663]
  • Liver X receptor unlinks intestinal regeneration and tumorigenesis.
     Das S, Parigi SM, Luo X, Fransson J, Kern BC, Okhovat A, Diaz OE, Sorini C, Czarnewski P, Webb AT et al.. Liver X receptor unlinks intestinal regeneration and tumorigenesis. (2025)  Nature, 637 (8048): 1198-1206. [PMID:39567700]
  • Schwann cell C5aR1 co-opts inflammasome NLRP1 to sustain pain in a mouse model of endometriosis.
     Titiz M, Landini L, Souza Monteiro de Araujo D, Marini M, Seravalli V, Chieca M, Pensieri P, Montini M, De Siena G, Pasquini B et al.. Schwann cell C5aR1 co-opts inflammasome NLRP1 to sustain pain in a mouse model of endometriosis. (2024)  Nat Commun, 15 (1): 10142. [PMID:39587068]
  • Structural basis for the reaction cycle and transport mechanism of human Na+-sulfate cotransporter NaS1 (SLC13A1).
     Chen X, Zhang Y, Yin J, Liu C, Xie M, Wang Y, Chen M, Zhang R, Yuan X, Li D et al.. Structural basis for the reaction cycle and transport mechanism of human Na+-sulfate cotransporter NaS1 (SLC13A1). (2024)  Sci Adv, 10 (47): eado6778. [PMID:39576865]
  • Structural basis for inositol pyrophosphate gating of the phosphate channel XPR1.
     Lu Y, Yue CX, Zhang L, Yao D, Xia Y, Zhang Q, Zhang X, Li S, Shen Y, Cao M et al.. Structural basis for inositol pyrophosphate gating of the phosphate channel XPR1. (2024)  Science, 386 (6723): eadp3252. [PMID:39325866]
  • Tlr7 drives sex differences in age- and Alzheimer's disease-related demyelination.
     Lopez-Lee C, Kodama L, Fan L, Zhu D, Zhu J, Wong MY, Ye P, Norman K, Foxe NR, Ijaz L et al.. Tlr7 drives sex differences in age- and Alzheimer's disease-related demyelination. (2024)  Science, 386 (6725): eadk7844. [PMID:39607927]

    • November 2024


  • Cryo-EM structure of the heteromeric TRPC1/TRPC4 channel.
     Won J, Kim J, Kim J, Ko J, Park CH, Jeong B, Lee SE, Jeong H, Kim SH, Park H et al.. Cryo-EM structure of the heteromeric TRPC1/TRPC4 channel. (2025)  Nat Struct Mol Biol, 32 (2): 326-338. [PMID:39478185]
  • Pharmacological restoration of GTP hydrolysis by mutant RAS.
     Cuevas-Navarro A, Pourfarjam Y, Hu F, Rodriguez DJ, Vides A, Sang B, Fan S, Goldgur Y, de Stanchina E, Lito P. Pharmacological restoration of GTP hydrolysis by mutant RAS. (2025)  Nature, 637 (8044): 224-229. [PMID:39476862]
  • Structure of G protein-coupled receptor GPR1 bound to full-length chemerin adipokine reveals a chemokine-like reverse binding mode.
     Liu A, Liu Y, Chen G, Lyu W, Ye F, Wang J, Liao Q, Zhu L, Du Y, Ye RD. Structure of G protein-coupled receptor GPR1 bound to full-length chemerin adipokine reveals a chemokine-like reverse binding mode. (2024)  PLoS Biol, 22 (10): e3002838. [PMID:39466725]
  • Membrane potential stimulates ADP import and ATP export by the mitochondrial ADP/ATP carrier due to its positively charged binding site.
     Mavridou V, King MS, Bazzone A, Springett R, Kunji ERS. Membrane potential stimulates ADP import and ATP export by the mitochondrial ADP/ATP carrier due to its positively charged binding site. (2024)  Sci Adv, 10 (44): eadp7725. [PMID:39485853]
  • Exposure to sugar rationing in the first 1000 days of life protected against chronic disease.
     Gracner T, Boone C, Gertler PJ. Exposure to sugar rationing in the first 1000 days of life protected against chronic disease. (2024)  Science, 386 (6725): 1043-1048. [PMID:39480913]
  • The translational value of ligand-receptor binding kinetics in drug discovery.
     Liu H, Zhang H, IJzerman AP, Guo D. The translational value of ligand-receptor binding kinetics in drug discovery. (2024)  Br J Pharmacol, 181 (21): 4117-4129. [PMID:37705429]
  • Alzheimer Disease as a Clinical-Biological Construct-An International Working Group Recommendation.
     Dubois B, Villain N, Schneider L, Fox N, Campbell N, Galasko D, Kivipelto M, Jessen F, Hanseeuw B, Boada M et al.. Alzheimer Disease as a Clinical-Biological Construct-An International Working Group Recommendation. (2024)  JAMA Neurol, 81 (12): 1304-1311. [PMID:39483064]
  • Spatial proteomics identifies JAKi as treatment for a lethal skin disease.
     Nordmann TM, Anderton H, Hasegawa A, Schweizer L, Zhang P, Stadler PC, Sinha A, Metousis A, Rosenberger FA, Zwiebel M et al.. Spatial proteomics identifies JAKi as treatment for a lethal skin disease. (2024)  Nature, 635 (8040): 1001-1009. [PMID:39415009]

    • October 2024


  • Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41.
     Tsutsumi N, Kildedal DF, Hansen OK, Kong Q, Schols D, Van Loy T, Rosenkilde MM. Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41. (2025)  Br J Pharmacol, 182 (1): 26-51. [PMID:39443818]
  • Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential.
     Peter S, Siragusa L, Thomas M, Palomba T, Cross S, O'Boyle NM, Bajusz D, Ferenczy GG, Keserű GM, Bottegoni G et al.. Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential. (2024)  J Chem Inf Model, 64 (21): 8176-8192. [PMID:39441864]
  • Multiscale drug screening for cardiac fibrosis identifies MD2 as a therapeutic target.
     Zhang H, Thai PN, Shivnaraine RV, Ren L, Wu X, Siepe DH, Liu Y, Tu C, Shin HS, Caudal A et al.. Multiscale drug screening for cardiac fibrosis identifies MD2 as a therapeutic target. (2024)  Cell, [Epub ahead of print]. [PMID:39413786]
  • PLD3 and PLD4 synthesize S,S-BMP, a key phospholipid enabling lipid degradation in lysosomes.
     Singh S, Dransfeld UE, Ambaw YA, Lopez-Scarim J, Farese Jr RV, Walther TC. PLD3 and PLD4 synthesize S,S-BMP, a key phospholipid enabling lipid degradation in lysosomes. (2024)  Cell, 187 (24): 6820-6834.e24. [PMID:39423811]
  • Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury.
     Lin H, Ma C, Zhuang X, Liu S, Liu D, Zhang M, Lu Y, Zhou G, Zhang C, Wang T et al.. Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury. (2024)  Cell Metab, 36 (11): 2402-2418.e10. [PMID:39389061]
  • Lighting up arginine metabolism reveals its functional diversity in physiology and pathology.
     Li R, Li Y, Jiang K, Zhang L, Li T, Zhao A, Zhang Z, Xia Y, Ge K, Chen Y et al.. Lighting up arginine metabolism reveals its functional diversity in physiology and pathology. (2024)  Cell Metab, [Epub ahead of print]. [PMID:39413790]
  • GPR158 in pyramidal neurons mediates social novelty behavior via modulating synaptic transmission in male mice.
     Wei S, Jiang J, Wang D, Chang J, Tian L, Yang X, Ma XR, Zhao JW, Li Y, Chang S et al.. GPR158 in pyramidal neurons mediates social novelty behavior via modulating synaptic transmission in male mice. (2024)  Cell Rep, 43 (10): 114796. [PMID:39383040]
  • Bioassay protocol metadata annotation: Proposed standards adoption.
     Balakrishnan R, Berg EL, Butler CC, Clark AM, Denker SP, Feierberg I, Harris J, Ikeda TP, Jeschonek S, Makarov VA et al.. Bioassay protocol metadata annotation: Proposed standards adoption. (2024)  SLAS Discov, 29 (8): 100188. [PMID:39427714]
  • Pervasive sublethal effects of agrochemicals on insects at environmentally relevant concentrations.
     Gandara L, Jacoby R, Laurent F, Spatuzzi M, Vlachopoulos N, Borst NO, Ekmen G, Potel CM, Garrido-Rodriguez M, Böhmert AL et al.. Pervasive sublethal effects of agrochemicals on insects at environmentally relevant concentrations. (2024)  Science, 386 (6720): 446-453. [PMID:39446951]
  • P2X7 receptors exhibit at least three modes of allosteric antagonism.
     Oken AC, Ditter IA, Lisi NE, Krishnamurthy I, Godsey MH, Mansoor SE. P2X7 receptors exhibit at least three modes of allosteric antagonism. (2024)  Sci Adv, 10 (40): eado5084. [PMID:39365862]
  • Cryo-EM investigation of ryanodine receptor type 3.
     Chen YS, Garcia-Castañeda M, Charalambous M, Rossi D, Sorrentino V, Van Petegem F. Cryo-EM investigation of ryanodine receptor type 3. (2024)  Nat Commun, 15 (1): 8630. [PMID:39366997]
  • The synaptic vesicle cluster as a controller of pre- and postsynaptic structure and function.
     Reshetniak S, Bogaciu CA, Bonn S, Brose N, Cooper BH, D'Este E, Fauth M, Fernández-Busnadiego R, Fiosins M, Fischer A et al.. The synaptic vesicle cluster as a controller of pre- and postsynaptic structure and function. (2024)  J Physiol, [Epub ahead of print]. [PMID:39367860]

    • September 2024


  • Ketamine and Major Ketamine Metabolites Function as Allosteric Modulators of Opioid Receptors.
     Gomes I, Gupta A, Margolis EB, Fricker LD, Devi LA. Ketamine and Major Ketamine Metabolites Function as Allosteric Modulators of Opioid Receptors. (2024)  Mol Pharmacol, 106 (5): 240-252. [PMID:39187388]
  • Assessing Darkness of the Human Kinome from a Medicinal Chemistry Perspective.
     Voßen S, Xerxa E, Bajorath J. Assessing Darkness of the Human Kinome from a Medicinal Chemistry Perspective. (2024)  J Med Chem, 67 (19): 17919-17928. [PMID:39320975]
  • Cryo-EM structure of human class C orphan GPCR GPR179 involved in visual processing.
     Yun Y, Jeong H, Laboute T, Martemyanov KA, Lee HH. Cryo-EM structure of human class C orphan GPCR GPR179 involved in visual processing. (2024)  Nat Commun, 15 (1): 8299. [PMID:39333506]
  • Targeting RNA with small molecules, from RNA structures to precision medicines: IUPHAR review: 40.
     Tong Y, Childs-Disney JL, Disney MD. Targeting RNA with small molecules, from RNA structures to precision medicines: IUPHAR review: 40. (2024)  Br J Pharmacol, 181 (21): 4152-4173. [PMID:39224931]

    • August 2024


  • A neurodevelopmental disorder mutation locks G proteins in the transitory pre-activated state.
     Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W et al.. A neurodevelopmental disorder mutation locks G proteins in the transitory pre-activated state. (2024)  Nat Commun, 15 (1): 6643. [PMID:39103320]

    • July 2024


  • Glutathione-Based Photoaffinity Probe Identifies Caffeine as a Positive Allosteric Modulator of the Calcium-Sensing Receptor.
     Matarage Don NNJ, Padmavathi R, Khasro TD, Zaman MRU, Ji HF, Ram JL, Ahn YH. Glutathione-Based Photoaffinity Probe Identifies Caffeine as a Positive Allosteric Modulator of the Calcium-Sensing Receptor. (2024)  ACS Chem Biol, 19 (7): 1661-1670. [PMID:38975966]
  • Cryo-EM Structure and Biochemical Analysis of the Human Chemokine Receptor CCR8.
     Peng Q, Jiang H, Cheng X, Wang N, Zhou S, Zhang Y, Yang T, Chen Y, Zhang W, Lv S et al.. Cryo-EM Structure and Biochemical Analysis of the Human Chemokine Receptor CCR8. (2024)  Biochemistry, 63 (15): 1892-1900. [PMID:38985857]
  • ChemFREE: a one-stop comprehensive platform for ecological and environmental risk evaluation of chemicals in one health world.
     Chen D, Liu Y, Liu Y, Zhao K, Zhang T, Gao Y, Wang Q, Song B, Hao G. ChemFREE: a one-stop comprehensive platform for ecological and environmental risk evaluation of chemicals in one health world. (2024)  Nucleic Acids Res, 52 (W1): W450-W460. [PMID:38832633]
  • The cerebellum modulates thirst.
     Mishra I, Feng B, Basu B, Brown AM, Kim LH, Lin T, Raza MA, Moore A, Hahn A, Bailey S et al.. The cerebellum modulates thirst. (2024)  Nat Neurosci, 27 (9): 1745-1757. [PMID:38987435]
  • The sphingosine-1-phosphate receptor 1 mediates the atheroprotective effect of eicosapentaenoic acid.
     Zhou T, Cheng J, He S, Zhang C, Gao MX, Zhang LJ, Sun JP, Zhu Y, Ai D. The sphingosine-1-phosphate receptor 1 mediates the atheroprotective effect of eicosapentaenoic acid. (2024)  Nat Metab, 6 (8): 1566-1583. [PMID:38907081]
  • Coordinated action of a gut-liver pathway drives alcohol detoxification and consumption.
     Fu Y, Mackowiak B, Lin YH, Maccioni L, Lehner T, Pan H, Guan Y, Godlewski G, Lu H, Chen C et al.. Coordinated action of a gut-liver pathway drives alcohol detoxification and consumption. (2024)  Nat Metab, 6 (7): 1380-1396. [PMID:38902331]
  • Inhibition of OSBP blocks retrograde trafficking by inducing partial Golgi degradation.
     He N, Depta L, Rossetti C, Caramelle L, Cigler M, Bryce-Rogers HP, Michon M, Rafn Dan O, Hoock J, Barbier J et al.. Inhibition of OSBP blocks retrograde trafficking by inducing partial Golgi degradation. (2025)  Nat Chem Biol, 21 (2): 203-214. [PMID:38907112]
  • Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting OSBP.
     Cigler M, Imrichova H, Frommelt F, Caramelle L, Depta L, Rukavina A, Kagiou C, Hannich JT, Mayor-Ruiz C, Superti-Furga G et al.. Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting OSBP. (2025)  Nat Chem Biol, 21 (2): 193-202. [PMID:38907113]
  • 3-Hydroxykynurenine targets kainate receptors to promote defense against infection.
     Parada-Kusz M, Clatworthy AE, Goering ER, Blackwood SM, Shigeta JY, Mashin E, Salm EJ, Choi C, Combs S, Lee JSW et al.. 3-Hydroxykynurenine targets kainate receptors to promote defense against infection. (2024)  Nat Chem Biol, 20 (12): 1586-1596. [PMID:38898166]
  • A molecular glue degrader of the WIZ transcription factor for fetal hemoglobin induction.
     Ting PY, Borikar S, Kerrigan JR, Thomsen NM, Aghania E, Hinman AE, Reyes A, Pizzato N, Fodor BD, Wu F et al.. A molecular glue degrader of the WIZ transcription factor for fetal hemoglobin induction. (2024)  Science, 385 (6704): 91-99. [PMID:38963839]
  • NN1213 - A Potent, Long-Acting, and Selective Analog of Human Amylin.
     Dahl K, Raun K, Hansen JL, Poulsen C, de la Cour CD, Clausen TR, Hansen AMK, John LM, Plesner A, Sun G et al.. NN1213 - A Potent, Long-Acting, and Selective Analog of Human Amylin. (2024)  J Med Chem, 67 (14): 11688-11700. [PMID:38960379]
  • A µ-opioid receptor modulator that works cooperatively with naloxone.
     O'Brien ES, Rangari VA, El Daibani A, Eans SO, Hammond HR, White E, Wang H, Shiimura Y, Krishna Kumar K, Jiang Q et al.. A µ-opioid receptor modulator that works cooperatively with naloxone. (2024)  Nature, 631 (8021): 686-693. [PMID:38961287]

    • June 2024


  • Characterization of genetic variants of GIPR reveals a contribution of β-arrestin to metabolic phenotypes.
     Kizilkaya HS, Sørensen KV, Madsen JS, Lindquist P, Douros JD, Bork-Jensen J, Berghella A, Gerlach PA, Gasbjerg LS, Mokrosiński J et al.. Characterization of genetic variants of GIPR reveals a contribution of β-arrestin to metabolic phenotypes. (2024)  Nat Metab, 6 (7): 1268-1281. [PMID:38871982]
  • Liver ACOX1 regulates levels of circulating lipids that promote metabolic health through adipose remodeling.
     Lu D, He A, Tan M, Mrad M, El Daibani A, Hu D, Liu X, Kleiboeker B, Che T, Hsu FF et al.. Liver ACOX1 regulates levels of circulating lipids that promote metabolic health through adipose remodeling. (2024)  Nat Commun, 15 (1): 4214. [PMID:38760332]
  • The state of the art in secondary pharmacology and its impact on the safety of new medicines.
     Brennan RJ, Jenkinson S, Brown A, Delaunois A, Dumotier B, Pannirselvam M, Rao M, Ribeiro LR, Schmidt F, Sibony A et al.. The state of the art in secondary pharmacology and its impact on the safety of new medicines. (2024)  Nat Rev Drug Discov, 23 (7): 525-545. [PMID:38773351]
  • Molecular mechanism of choline and ethanolamine transport in humans.
     Ri K, Weng TH, Claveras Cabezudo A, Jösting W, Zhang Y, Bazzone A, Leong NCP, Welsch S, Doty RT, Gursu G et al.. Molecular mechanism of choline and ethanolamine transport in humans. (2024)  Nature, 630 (8016): 501-508. [PMID:38778100]
  • Kainate receptor channel opening and gating mechanism.
     Gangwar SP, Yelshanskaya MV, Nadezhdin KD, Yen LY, Newton TP, Aktolun M, Kurnikova MG, Sobolevsky AI. Kainate receptor channel opening and gating mechanism. (2024)  Nature, 630 (8017): 762-768. [PMID:38778115]
  • Distinct µ-opioid ensembles trigger positive and negative fentanyl reinforcement.
     Chaudun F, Python L, Liu Y, Hiver A, Cand J, Kieffer BL, Valjent E, Lüscher C. Distinct µ-opioid ensembles trigger positive and negative fentanyl reinforcement. (2024)  Nature, 630 (8015): 141-148. [PMID:38778097]
  • Bitter taste TAS2R14 activation by intracellular tastants and cholesterol.
     Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J et al.. Bitter taste TAS2R14 activation by intracellular tastants and cholesterol. (2024)  Nature, 631 (8020): 459-466. [PMID:38776963]
  • The microbial metabolite agmatine acts as an FXR agonist to promote polycystic ovary syndrome in female mice.
     Yun C, Yan S, Liao B, Ding Y, Qi X, Zhao M, Wang K, Zhuo Y, Nie Q, Ye C et al.. The microbial metabolite agmatine acts as an FXR agonist to promote polycystic ovary syndrome in female mice. (2024)  Nat Metab, 6 (5): 947-962. [PMID:38769396]

    • May 2024


  • Structural and functional evidence that GPR30 is not a direct estrogen receptor.
     Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D et al.. Structural and functional evidence that GPR30 is not a direct estrogen receptor. (2024)  Cell Res, 34 (7): 530-533. [PMID:38744981]
  • Atypical chemokine receptors in the immune system.
     Comerford I, McColl SR. Atypical chemokine receptors in the immune system. (2024)  Nat Rev Immunol, 24 (10): 753-769. [PMID:38714818]
  • GLP-1-directed NMDA receptor antagonism for obesity treatment.
     Petersen J, Ludwig MQ, Juozaityte V, Ranea-Robles P, Svendsen C, Hwang E, Kristensen AW, Fadahunsi N, Lund J, Breum AW et al.. GLP-1-directed NMDA receptor antagonism for obesity treatment. (2024)  Nature, 629 (8014): 1133-1141. [PMID:38750368]