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
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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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [PMID:38961287] -
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 ofβ -arrestin to metabolic phenotypes. (2024) Nat Metab, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [PMID:38769396] -
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, [Epub ahead of print]. [PMID:38744981] -
Atypical chemokine receptors in the immune system.
Comerford I, McColl SR. Atypical chemokine receptors in the immune system. (2024) Nat Rev Immunol, [Epub ahead of print]. [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] -
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, [Epub ahead of print]. [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] -
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, [Epub ahead of print]. [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, [Epub ahead of print]. [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, [Epub ahead of print]. [PMID:38519768] -
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, [Epub ahead of print]. [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, [Epub ahead of print]. [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. (2023) Br J Pharmacol, [Epub ahead of print]. [PMID:38148720] -
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] -
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] -
The Batten disease gene product CLN5 is the lysosomal bis(monoacylglycero)phosphate synthase.
Medoh UN, Hims A, Chen JY, Ghoochani A, Nyame K, Dong W, Abu-Remaileh M. The Batten disease gene product CLN5 is the lysosomal bis(monoacylglycero)phosphate synthase. (2023) Science, 381 (6663): 1182-1189. [PMID:37708259] -
Neuromedin U programs eosinophils to promote mucosal immunity of the small intestine.
Li Y, Liu S, Zhou K, Wang Y, Chen Y, Hu W, Li S, Li H, Wang Y, Wang Q et al.. Neuromedin U programs eosinophils to promote mucosal immunity of the small intestine. (2023) Science, 381 (6663): 1189-1196. [PMID:37708282] -
Exploring DrugCentral: from molecular structures to clinical effects.
Halip L, Avram S, Curpan R, Borota A, Bora A, Bologa C, Oprea TI. Exploring DrugCentral: from molecular structures to clinical effects. (2023) J Comput Aided Mol Des, 37 (12): 681-694. [PMID:37707619] -
Role of sphingolipids in the host-pathogen interaction.
Matos GS, Fernandes CM, Del Poeta M. Role of sphingolipids in the host-pathogen interaction. (2023) Biochim Biophys Acta Mol Cell Biol Lipids, 1868 (11): 159384. [PMID:37673393] -
Dynamic lipidome alterations associated with human health, disease and ageing.
Hornburg D, Wu S, Moqri M, Zhou X, Contrepois K, Bararpour N, Traber GM, Su B, Metwally AA, Avina M et al.. Dynamic lipidome alterations associated with human health, disease and ageing. (2023) Nat Metab, 5 (9): 1578-1594. [PMID:37697054] -
Global analysis of aging-related protein structural changes uncovers enzyme-polymerization-based control of longevity.
Paukštytė J, López Cabezas RM, Feng Y, Tong K, Schnyder D, Elomaa E, Gregorova P, Doudin M, Särkkä M, Sarameri J et al.. Global analysis of aging-related protein structural changes uncovers enzyme-polymerization-based control of longevity. (2023) Mol Cell, 83 (18): 3360-3376.e11. [PMID:37699397] -
Mitochondrial degradation: Mitophagy and beyond.
Uoselis L, Nguyen TN, Lazarou M. Mitochondrial degradation: Mitophagy and beyond. (2023) Mol Cell, 83 (19): 3404-3420. [PMID:37708893] -
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] -
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, 75 (6): 1233-1318. [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. (2024) Nat Chem Biol, 20 (1): 74-82. [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] -
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, 299 (8): 105078. [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]. [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, 26 (8): 1339-1351. [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, 25 (8): 1085-1086. [PMID:37474818]
