Hot Topics in Pharmacology

Coronavirus Information

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

2024: Sep | Aug | Jul | Jun | May | Apr | Mar | Jan
2023: Nov | Oct

    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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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. (2024)  Nat Chem Biol, [Epub ahead of print]. [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. (2024)  Nat Chem Biol, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [PMID:38750368]
  • Differential G protein activation by the long and short isoforms of the dopamine D2 receptor.
     Reiner-Link D, Madsen JS, Gloriam DE, Bräuner-Osborne H, Hauser AS. Differential G protein activation by the long and short isoforms of the dopamine D2 receptor. (2024)  Br J Pharmacol, [Epub ahead of print]. [PMID:38725357]

    • April 2024


  • Shifting our perspective on orphan G protein-coupled receptors.
     Smith NJ, Murray F. Shifting our perspective on orphan G protein-coupled receptors. (2024)  Nat Struct Mol Biol, 31 (4): 582-583. [PMID:38565695]
  • AI is a viable alternative to high throughput screening: a 318-target study.
     Atomwise AIMS Program. AI is a viable alternative to high throughput screening: a 318-target study. (2024)  Sci Rep, 14 (1): 7526. [PMID:38565852]

    • March 2024


  • MFSD7c functions as a transporter of choline at the blood-brain barrier.
     Nguyen XTA, Le TNU, Nguyen TQ, Thi Thuy Ha H, Artati A, Leong NCP, Nguyen DT, Lim PY, Susanto AV, Huang Q et al.. MFSD7c functions as a transporter of choline at the blood-brain barrier. (2024)  Cell Res, 34 (3): 245-257. [PMID:38302740]
  • Orphan lysosomal solute carrier MFSD1 facilitates highly selective dipeptide transport.
     Boytsov D, Madej GM, Horn G, Blaha N, Köcher T, Sitte HH, Siekhaus D, Ziegler C, Sandtner W, Roblek M. Orphan lysosomal solute carrier MFSD1 facilitates highly selective dipeptide transport. (2024)  Proc Natl Acad Sci U S A, 121 (13): e2319686121. [PMID:38507452]
  • Activation of GPR81 by lactate drives tumour-induced cachexia.
     Liu X, Li S, Cui Q, Guo B, Ding W, Liu J, Quan L, Li X, Xie P, Jin L et al.. Activation of GPR81 by lactate drives tumour-induced cachexia. (2024)  Nat Metab, 6 (4): 708-723. [PMID:38499763]
  • The kainate receptor GluK2 mediates cold sensing in mice.
     Cai W, Zhang W, Zheng Q, Hor CC, Pan T, Fatima M, Dong X, Duan B, Xu XZS. The kainate receptor GluK2 mediates cold sensing in mice. (2024)  Nat Neurosci, 27 (4): 679-688. [PMID:38467901]
  • An evolutionarily conserved olfactory receptor is required for sex differences in blood pressure.
     Xu J, Choi R, Gupta K, Warren HR, Santhanam L, Pluznick JL. An evolutionarily conserved olfactory receptor is required for sex differences in blood pressure. (2024)  Sci Adv, 10 (12): eadk1487. [PMID:38507492]
  • Understanding the provenance and quality of methods is essential for responsible reuse of FAIR data.
     Weissgerber TL, Gazda MA, Nilsonne G, Ter Riet G, Cobey KD, Prieß-Buchheit J, Noro J, Schulz R, Tijdink JK, Bobrov E et al.. Understanding the provenance and quality of methods is essential for responsible reuse of FAIR data. (2024)  Nat Med, [Epub ahead of print]. [PMID:38514869]
  • Promoting gender equity in the scientific and health workforce is essential to improve women's health.
     Vieira Machado C, Araripe Ferreira C, de Souza Mendes Gomes MA. Promoting gender equity in the scientific and health workforce is essential to improve women's health. (2024)  Nat Med, 30 (4): 937-939. [PMID:38519768]

    • January 2024


  • Persistent complement dysregulation with signs of thromboinflammation in active Long Covid.
     Cervia-Hasler C, Brüningk SC, Hoch T, Fan B, Muzio G, Thompson RC, Ceglarek L, Meledin R, Westermann P, Emmenegger M et al.. Persistent complement dysregulation with signs of thromboinflammation in active Long Covid. (2024)  Science, 383 (6680): eadg7942. [PMID:38236961]
  • EPAC1 enhances brown fat growth and beige adipogenesis.
     Reverte-Salisa L, Siddig S, Hildebrand S, Yao X, Zurkovic J, Jaeckstein MY, Heeren J, Lezoualc'h F, Krahmer N, Pfeifer A. EPAC1 enhances brown fat growth and beige adipogenesis. (2024)  Nat Cell Biol, 26 (1): 113-123. [PMID:38195707]
  • Chemoproteomic development of SLC15A4 inhibitors with anti-inflammatory activity.
     Chiu TY, Lazar DC, Wang WW, Wozniak JM, Jadhav AM, Li W, Gazaniga N, Theofilopoulos AN, Teijaro JR, Parker CG. Chemoproteomic development of SLC15A4 inhibitors with anti-inflammatory activity. (2024)  Nat Chem Biol, 20 (8): 1000-1011. [PMID:38191941]
  • Insights for precision oncology from the integration of genomic and clinical data of 13,880 tumors from the 100,000 Genomes Cancer Programme.
     Sosinsky A, Ambrose J, Cross W, Turnbull C, Henderson S, Jones L, Hamblin A, Arumugam P, Chan G, Chubb D et al.. Insights for precision oncology from the integration of genomic and clinical data of 13,880 tumors from the 100,000 Genomes Cancer Programme. (2024)  Nat Med, 30 (1): 279-289. [PMID:38200255]
  • Structural basis of prostaglandin efflux by MRP4.
     Pourmal S, Green E, Bajaj R, Chemmama IE, Knudsen GM, Gupta M, Sali A, Cheng Y, Craik CS, Kroetz DL et al.. Structural basis of prostaglandin efflux by MRP4. (2024)  Nat Struct Mol Biol, 31 (4): 621-632. [PMID:38216659]
  • Biased agonists of GPR84 and insights into biological control.
     Luscombe VB, Wang P, Russell AJ, Greaves DR. Biased agonists of GPR84 and insights into biological control. (2024)  Br J Pharmacol, 181 (10): 1509-1523. [PMID:38148720]

    • November 2023


  • Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.
     Boby ML, Fearon D, Ferla M, Filep M, Koekemoer L, Robinson MC, COVID Moonshot Consortium‡, Chodera JD, Lee AA, London N et al.. Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors. (2023)  Science, 382 (6671): eabo7201. [PMID:37943932]

    • October 2023


  • The IUPHAR/BPS Guide to PHARMACOLOGY in 2024.
     Harding SD, Armstrong JF, Faccenda E, Southan C, Alexander SPH, Davenport AP, Spedding M, Davies JA. The IUPHAR/BPS Guide to PHARMACOLOGY in 2024. (2024)  Nucleic Acids Res, 52 (D1): D1438-D1449. [PMID:37897341]
  • ADCdb: the database of antibody-drug conjugates.
     Shen L, Sun X, Chen Z, Guo Y, Shen Z, Song Y, Xin W, Ding H, Ma X, Xu W et al.. ADCdb: the database of antibody-drug conjugates. (2024)  Nucleic Acids Res, 52 (D1): D1097-D1109. [PMID:37831118]
  • TTD: Therapeutic Target Database describing target druggability information.
     Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F. TTD: Therapeutic Target Database describing target druggability information. (2024)  Nucleic Acids Res, 52 (D1): D1465-D1477. [PMID:37713619]
  • Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
     Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW et al.. Functional screening and rational design of compounds targeting GPR132 to treat diabetes. (2023)  Nat Metab, 5 (10): 1726-1746. [PMID:37770763]
  • Genome-wide association analysis reveals insights into the molecular etiology underlying dilated cardiomyopathy.
     Zheng SL, Henry A, Cannie D, Lee M, Miller D, McGurk KA, Bond I, Xu X, Issa H, Francis Cet al.. Genome-wide association analysis reveals insights into the molecular etiology underlying dilated cardiomyopathy. (2023)  medRxiv, Preprint. DOI: https://www.medrxiv.org/content/10.1101/2023.09.28.23295408v1
  • An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism.
     Lees JA, Dias JM, Rajamohan F, Fortin JP, O'Connor R, Kong JX, Hughes EAG, Fisher EL, Tuttle JB, Lovett G et al.. An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism. (2023)  Nat Commun, 14 (1): 5938. [PMID:37741852]
  • Cryo-EM structures of human GPR34 enable the identification of selective antagonists.
     Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P et al.. Cryo-EM structures of human GPR34 enable the identification of selective antagonists. (2023)  Proc Natl Acad Sci U S A, 120 (39): e2308435120. [PMID:37733739]