Xu Laboratory

Selected Publications


Zhao LH*, Ma S*, Sutkeviciute I*, Shen DD*, Zhou XE, de Waal PW, Li CH, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanbe T, Gradella TJ, Melcher K, Wang MW#, Vilardaga JP#, Xu HE#, Zhang Y#. 2019. Structure and dynamics of the active human parathyroid hormone receptor-1. Science
* Equal contributions 
# Co-corresponding authors

Yan Y, Zhou EX, Novick SJ, Shaw SJ, Li Y, Brunzelle JS, Hitoshi Y, Griffin PR, Xu HE, Melcher K. 2019. Structures of AMP-activated protein kinase bound to novel pharmacological activators in phosphorylated, non-phosphorylated and nucleotide-free states. J Biol Chem 294(3):953–967.


Gu X, Bridges MD, Yan Y, de Waal PW, Zhou EX, Suino-Powell KM, Xu HE, Hubbell WL, Melcher K. 2018. Conformational heterogeneity of the allosteric drug and metabolite (ADaM) site in AMP-activated protein kinase (AMPK). J Biol Chem 293(44):16994–17007.

Li H, Zhao L, Singh R, Ham JN, Fadoju DO, Beah LJH, Zhang Y, Xu Y, Xu HE, Gambello MJ. 2018. The first pediatric case of glucagon receptor defect due to biallelic mutations in GCGR is identified by newborn screening of elevated argenine. Mole Genet Metab Rep 17:46–52.

Yang S, Wu T, Xu TH, de Waal PW, He Y, Pu M, Chen Y, DeBruine ZJ, Zhang B, Zaidi SA, Popov P, Guo Y, Han GW, Lu Y, Suino-Powell K, Song S, Harikumar KG, Miller LJ, Katritch V, Xu HE, Shui W, Stevens RC, Melcher K, Zhao S, Xu F. 2018. Crystal structure of the Frizzled 4 receptor in a ligand-free state. Nature.

Yin W, Zhou XE, Yang D, de Waal PW, Want M, Dai A, Cai X, Haung CY, Liu P, Wang X, Yin Y, Liu B, Zhou Y, Wang J, Liu H, Caffrey M, Melcher K, Xu Y, Wang MW, Xu HE, Jiang Y. 2018. Crystal structure of the human 5-HT1B serotonin receptor bound to an inverse agonist. Cell Disc 4(12).

Kang Y*, Kuybeda O*, de Waal PW*, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE. 2018. Cryo-EM structure of human rhodopsin bound to an inhibitory G proteinNature.


Zhou XE, He Y, de Waal PW, Gao X, Kang Y, Van Eps N, Yin Y, Pal K, Goswami D, White TA, Barty A, Latorraca NR, Chapman HN, Hubbell WL, Dror RO, Stevens RC, Cherezov V, Gurevich VV, Griffin PR, Ernst OP, Melcher K, Xu HE. 2017. Identification of phosphorylation codes for arrestin recruitment by G protein-coupled receptors. Cell 170(3):457–469.e13.
*Cover of Cell


Golani LK, Wallace-Povirk A, Deis SM, Wong J, Ke J, Gu X, Raghaven S, Wilson MR, Li X, Polin L, de Waal PW, White K, Kushner J, O’Connor C, Hou Z, Xu HE, Melcher K, Dann CE 3rd, Matherly LH, Gangjee A. 2016. Tumor targeting with novel 6-substituted phyrrolo [2,3-d] pyrimidine antifolates with heteroatom bridge substitutions via cellular uptake by folate receptor a and the proteon-coupled folate transporter and inhibitor of de novo purine nucleotide biosynthesis. J Med Chem 59(17):7856–7876.

Zhou XE, Gao X, Barty A, Kang Y, He Y, Liu W, Ishchenko A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Suino-Powell KM, Boutet S, Williams GJ,Wang M, Li D, Caffrey M, Chapman HN, Spence JC, Fromme P, Weierstall U, Stevens RC, Cherezov V, Melcher K, Xu HE. 2016. X-ray laser diffraction for structure determination of the rhodopsin-arrestin complexSci Data 3:160021.


Ke J, Ma H, Gu X, Thelen A, Brunzelle JS, Li J, Xu HE, Melcher K. 2015. Structural basis for recognition of diverse transcriptional repressors by the TOPLESS family of corepressorsSci Adv 1(6):e1500107.

Zhang F*, Yao J*, Ke J*, Zhang L, Lam VQ, Xin X-F, Zhou XE, Chen J, Brunzelle J, Griffin PR, Zhou M, Xu HE, Melcher K, He YS. 2015. Structural basis of JAZ-mediated repression of MYC transcription factors in jasmonate signalingNature 525:269–273.

Kang Y, Zhou XE Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MHE, Zhang C, Moeller A, West GM, Pascal B, Eps NV, Caro1 LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi XY, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad C, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JCH, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE. 2015. Crystal structure of rhodopsin bound to arrestin determined by femtosecond X-ray laser. Nature 532:561–567.
*Featured in Nature News & Views

Zhi X, Zhou XE, He Y, Searose-Xu K, Zhang CL, Tsai CC, Melcher K, Xu HE. 2015. Structural basis for corepressor assembly by the orphan nuclear receptor TLXGenes Dev 29(4):440–450.


Sridharamurthy M, Kovach A, Zhao Y, Zhu JK, Xu HE, Swaminathan K, Melcher K. 2014. H2O2 inhibits ABA-signaling protein phosphatase HAB1PLoS One 9(12):e113643.

Li X*, Wang L*, Zhou XE*, Ke J, de Waal PW, Gu X, Tan MHE, Wang D, Wu D, Xu HE, Melcher K. 2014. Structural basis of AMPK regulation by adenine nucleotides and glycogenCell Res 25(1):50–66.

*Authors contributed equally this work
**Highlighted in editorial in Cell Research

He Y, Yi W, Powell K, Zhou XE, Tolbert D, Tang X, Yang JC, Yang H, Shi J, Hou L, Jiang H, Melcher K, Xu HE. 2014. Structures and mechanism for the design of highly potent glucocorticoidsCell Res 24:713 –726.

Ng LM, Melcher K, Teh BT, Xu HE. 2014. Abscisic acid perception and signaling: structural mechanisms and applicationsActa Pharma Sin 35(5):567–584.

Tan MH, Li JY, Xu HE, Melcher K, Yong EL. 2014. Androgen receptor: structure, prostate cancer, and drug discoveryActa Pharma Sin 36(1):3–23.

Tan JZ, Yan Y, Wang XX, Jiang Y, Xu HE. 2014. EZH2: biology, disease, and structure-based drug discoveryActa Pharma Sin 35(2):161–174.

Zhi X, Zhou XE, He Y, Zechner C, Suino-Powell KM, Kliewer SA, Melcher K, Mangelsdorf DJ, Xu HE. 2014. Structural insights into gene repression by the orphan nuclear receptor SHPProc Natl Acad Sci U S A 111(2):839–844.


Ban T, Ke J, Chen R, Gu X, Tan MH, Zhou XE, Kang Y, Melcher K, Zhu JK, Xu HE. 2013. Structure of a PLS-class pentatricopeptide repeat protein provides insights into mechanism of RNA recognitionJ Biol Chem 288(44):31540–31548.     PubMed     Article

Cao M, Liu X, Zhang Y, Xue X, Zhou XE, Melcher K, Gao P, Wang F, Zeng L, Zhao Y, Zhao Y, Deng P, Zhong D, Zhu JK, Xu HE, Xu Y. 2013. An ABA-mimicking ligand that reduces water loss and promotes drought resistance in plantsCell Res 23(8):1043–1054.

Chen C, Ke J, Zhou XE, Yi W, Brunzelle JS, Li J, Yong EL,  Xu HE, Melcher K. 2013. Structural basis for molecular recongition of folic acid by folate receptorsNature 500: 486–489.

Jiang L, Liu X, Xiong G, Liu H, Chen F, Wang L, Meng X, Liu G, Yu H, Yuan Y, Yi W, Zhao L, Ma H, He Y, Wu Z, Melcher K, Qian Q, Xu HE, Wang Y, Li J. 2013. DWARF 53 acts as a repressor of stringolactone signalling in riceNature 504(7480):401–405.

Joiner DM, Ke J, Zhong Z, Xu HE, Williams BO. 2013. LRP5 and LRP6 in development and diseaseTrends Endocrinol Metab 24(1):31–39.

Ke J, Chen RZ, Ban T, Zhou XE, Gu X, Tan MH, Chen C, Kang Y, Brunzelle JS, Zhu JK, Melcher K, Xu HE. 2013. Structural basis for RNA recognition by a dimeric PPR-protein complexNat Struct Mol Biol 20(12):1377–1382.

Ke J, Harikumar KG, Jurecky C, Chen C, Gu X, Wang L, Parker N, Cheng Z, Xu W, Williams BO, Melcher K, Miller LJ, Xu HE. 2013. Structure and function of Norrin in assembly and activation of a Frizzled 4–Lrp5/6 complexGenes Dev 27(21):2305–2319.

Ke J, Xu HE, Williams BO. 2013. Lipid modification in Wnt structure and functionCurr Opin Lipidol 24(2):129–133.

Lash LL, Wallar BJ, Turner JD, Vroegop SM, Kilkuskie RE, Kitchen-Goosen SM, Xu HE, Alberts AS. 2013. Small-molecule intramimics of formin auto-inhibition: a new strategy to target the cytoskeletal remodeling machinery in cancer cellsCancer Res 73(22):6793–6803.

Li Q, Yan Y, Wang X, Gong B, Tang X, Shi J, Xu HE, Yi W. 2013. Water as a green solvent for efficient synthesis of isocoumarins through microwave-accelerated and Rh/Cu-catalyzed C-H/O-H bond functionalization. RSC Advances 3(45):23402–23408.

Pal K , Melcher K, Xu HE. 2013. Structure modeling using genetically engineered crosslinkingCell 155(6):1207–1208.

Tan MH, Zhou XE, Soon FF, Li X, Li J, Yong EL, Melcher K, Xu HE. 2013. The crystal structure of the orphan nuclear receptor NR2E3/PNR ligand binding domain reveals a dimeric auto-repressed conformationPLoS One 8(9):e74359.

Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W,  Xu HE, Cherezov V, Roth BL, Stevens RC. 2013. Structural features for functional selectivity at serotonin receptorsScience 340(6132):615–619.

Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou EX, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. 2013. Structural basis for molecular recognition at serotonin receptorsScience 340(6132):610–614.

Wang X, Yunnan Y, Gong B, Tang X, Li Q, Meng Y, Xu HE, Yi W. 2013. Efficient synthesis of functionalized 1-oxo-1-phenyl-2-acetic acids through Ru(II)-catalyzed transfer hydrogenation. Bulletin of the Korean Chemical Society 34(10):3143–3146.

West GM, Pascal BD, Ng LM, Soon FF, Melcher K, Xu HE, Chalmers MJ, Griffin PR. 2013. Protein conformation ensembles monitored by HDX reveal a structural rationale for abscisic acid signaling protein affinities and activitiesStructure 21(2):229–235.

Zhao LH, Zhou XE, Wu ZS, Yi W, Xu Y, Li S, Xu TH, Liu Y, Chen RZ, Kovach A, Kang Y, Hou L, He Y, Xie C, Song W, Zhong D, Xu Y, Wang Y, Li J, Zhang C, Melcher K, Xu HE. 2013. Crystal structures of two phytohormone signal-transducing α/β hydrolases: karrikin-signaling KAI2 and stringolactone-signaling DWARF14Cell Res 23(3):436–439.


Blind RD, Pineda-Torra I, Xu Y, Xu HE, Garabedian MJ. 2012. Ligand structural motifs can decouple glucorticoid receptor transcriptional activation from target promoter occupancyBiochem Biophys Res Comm 420(4):839–844.

Fu T, Choi SE, Kim DH, Seok S, Suino-Powell KM, Xu HE, Kemper JK. 2012. Aberrantly elevated microRNA-34a in obesity attenuates hepatic responses to FGF19 by targeting a membrane coreceptor β-KlothoProc Natl Acad Sci U S A 109(40):16137–16142.

Ke J, Zhang C, Harikumar KG, Zylstra-Diegel CR, Wang L, Mowry LE, Miller LJ, Williams BO, Xu HE. 2012. Modulation of β-catenin signaling by glucagon receptor activationPLoS One 7(3): e33676.

Martin KR, Narang P, Xu Y, Kauffman AL, Petit J, Xu HE, Meurice N, MacKeigan JP. 2012. Identification of small molecule inhibitors of PTPσ through an integrative virtual and biochemical approachPLoS One 7(11):e50217.

Pal K, Melcher K, Xu HE. 2012. Structure and mechanism for recognition of peptide hormones by Class B G protein-coupled receptorsActa Pharma Sin 33(3): 300–311.

Soon FF, Ng LM, Zhou XE, West GM, Kovach A, Tan MH, Suino-Powell KM, He Y, Xu Y, Chalmers MJ, Brunzelle JS, Zhang H, Yang H, Jiang H, Li J, Yong EL, Cutler S, Zhu JK, Griffin PR, Melcher K, Xu HE. 2012. Molecular mimicry regulates ABA signaling by SnRK2 kinases and PP2C phosphatasesScience 335(6064):85–88.

Soon FF, Suino-Powell KM, Li J, Yong EL, Xu HE, Melcher K. 2012. Abscisic acid signaling: thermal stability shift assays as tool to analyze hormone perception and signal transductionPLoS One 7(10): e47857.

Tiong CT, Chen C, Zhang SJ, Li J, Soshilov A, Denison MS, Lee LS, Tam VH, Wong SP, Xu HE, Yong EL. 2012. A novel prenylflavone restricts breast cancer cell growth through AhR-mediated destabilization of ERα proteinCarcinogenesis 33(5):1089–1097.

Xu HE, Xiao RP. 2012. A new era for GPCR research: structures, biology and drug discoveryActa Pharma Sin 33(3):289–290.

Yu S, Xu HE. 2012. Couple dynamics: PPARγ and its ligand partnersStructure 20(1): 2–4.

Zhi X, Zhou XE, Melcher K, Motola DL, Gelmedin V, Hawdon J, Kliewer SA, Mangelsdorf DJ, Xu HE. 2012. Structural conservation of ligand binding reveals a bile acid–like signaling pathway in nematodesJ Biol Chem 287(7):4894–4903.

Zhou EX, Melcher K, Xu HE. 2012. Structure and activation of rhodopsinActa Pharma Sin 33(3):291–299.

Zhou XE, Soon FF, Ng LM, Kovach A, Suino-Powell KM, Li J, Yong EL, Zhu JK, Xu HE, Melcher K. 2012. Catalytic mechanism and kinase interactions of ABA-signaling PP2C phosphatasesPlant Signal Behav 7(5):581–588.


He Y, Xu Y, Zhang C, Gao X, Dykema KJ, Martin KR, Ke J, Hudson EA, Khoo SK, Resau JH, Alberts AS, MacKeigan JP, Furge KA, Xu HE. 2011. Identification of a lysosomal pathway that modulates glucocorticoid signaling and the inflammatory responseSci Signal 4(180): ra44.

Kir S, Beddow SA, Samuel VT, Miller P, Previs SF, Suino-Powell K, Xu HE, Shulman GI, Kliewer SA, Mangelsdorf DJ. 2011. FGF19 as a postprandial, insulin-independent activator of hepatic protein and glycogen synthesisScience 331(6024):1621–1624.

Martin KR, Xu Y, Looyenga BD, Davis RJ, Wu CL, Tremblay ML, Xu HE, MacKeigan JP. 2011. Identification of PTP{sigma} as an autophagic phosphataseJ Cell Sci 124(Pt 5): 812-819.

Niemi NM, Lanning NJ, Klomp JA, Tait SW, Xu Y, Dykema KJ, Murphy LO, Gaither LA, Xu HE, Furge KA, Green DR, MacKeigan JP. 2011. MK-STYX, a catalytically inactive phosphatase regulating mitochondrial dependent apoptosisMol Cell Biol 31(7):1357-1368.

Soon FF, Ng LM, Zhou XE, West GM, Kovach A, Tan MH, Suino-Powell KM, He Y, Xu Y, Chalmers MJ, Brunzelle JS, Zhang H, Yang H, Jiang H, Li J, Yong EL, Cutler S, Zhu JK, Griffin PR, Melcher K, Xu HE. 2012. Molecular mimicry regulates ABA signaling by SnRK2 kinases and PP2C phosphatasesScience 335(6064):85-88.

Xie Q, Wondergem R, Shen Y, Cavey G, Ke J, Thompson R, Bradley R, Daughtery-Holtrop J, Xu Y, Chen E, Omar H, Rosen N, Wenkert D, Xu HE, Vande Woude GF. 2011. Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasionProc Natl Acad Sci U S A 108(10):4105-4110.

Zhou XE, Suino-Powell KM, Xu Y, Chan CW, Tanabe O, Kruse SW, Reynolds R, Engel JD, Xu HE. 2011. The orphan nuclear receptor TR4 is a vitamin A-activated nuclear receptorJ Biol Chem 286(4): 2877-2885.


Melcher K, Xu Y, Ng LM, Zhou XE, Soon FF, Chinnusamy V, Suino-Powell KM, Kovach A, Tham FS, Cutler SR, Li J, Yong EL, Zhu JK, Xu HE. 2010. Identification and mechanism of ABA receptor antagonismNat Struct Mol Biol 17(9):1102-1108.

Pioszak AA, Harikumar KG, Parker NR, Miller LJ, Xu HE. 2010. Dimeric arrangement of the parathyroid hormone receptor and a structural mechanism for ligand-induced dissociationJ Biol Chem 285(16):12435-12444.

Schopfer FJ, Cole MP, Groeger AL, Chen CS, Khoo NK, Woodcock SR, Golin-Bisello F, Motanya UN, Li Y, Zhang J, Garcia-Barrio MT, Rudolph TK, Rudolph V, Bonacci G, Baker PR, Xu HE, Batthyany CI, Chen YE, Hallis TM, Freeman BA. 2010. Covalent peroxisome proliferator–activated receptor γ binding to nitro-fatty acids: endogenous ligands act as selective modulatorsJ Biol Chem 285(16): 12321–12333.

Tolbert WD, Daugherty-Holtrop J, Gherardi E, Vande Woude GF, Xu HE. 2010. Structural basis for agonism and antagonism of hepatocyte growth factorProc Natl Acad Sci U S A 107(30):13264–13269.

Pioszak AA, Xu HE. 2008. Molecular recognition of parathyroid hormone–related peptide (PTHrP) by the extracellular domain of its G protein–coupled receptor PTH1RProc Natl Acad Sci U S A 105(13): 5034–5039.

Zhou XE, Suino-Powell KM, Li J, He Y, MacKeigan JP, Melcher K, Yong EL, Xu HE. 2010. Identification of SRC3/AIB1 as a preferred coactivator for hormone-activated androgen receptorJ Biol Chem 285(12):9161–9171.

Zhou XE, Suino-Powell K, Ludidi PL, McDonnell DP, Xu HE. 2010. Expression, purification and primary crystallographic study of human androgen receptor in complex with DNA and coactivator motifsProtein Expr Purif 71(1):21–27.


Chakravarthy MV, Lodhi IJ, Yin L, Malapaka RV, Xu HE, Turk J, Semenkovich CF. 2009. Identification of a physiologically relevant endogenous ligand for PPARα in liverCell 138(3):476–488.

Knudsen BS, Zhao P, Resau J, Cottingham S, Gherardi E, Xu HE, Berghuis B, Daugherty J, Grabinski T, Toro J, Giambernardi T, Skinner RS, Gross M, Hudson E, Kort E, Lengyel E, Ventura A, West RA, Xie Q, Hay R, Vande Woude GF, Cao B. 2009. A novel multipurpose monoclonal antibody for evaluating human c-Met expression in preclinical and clinical settingsAppl Immunohistochem Mol Morphol 17(1):56–67.

Melcher K, Ng LM, Zhou XE, Soon FF, Xu Y, Suino-Powell KM, Park SY, Weiner FF, Fujii H, Chinnusamy V, Kovach A, Li J, Wang Y, Li J, Peterson FC, Jensen DR, Yong EL, Volkman BF, Cutler SR, Zhu JK, Xu HE. 2009. A gate-latch-lock mechanism for hormone signalling by abscisic acid receptorsNature 462(7273):602–608.

Miao J, Xiao Z, Kanamaluru D, Min G, Yau PM, Veenstra TD, Ellis E, Strom S, Suino-Powell K, Xu HE, Kemper JK. 2009. Bile acid signaling pathways increase stability of small heterodimer partner (SHP) by inhibiting ubiquitin-proteasomal degradationGenes Dev 23(8):986–996.

Pioszak A, Parker NR, Gardella TJ, Xu HE. 2009. Structural basis for parathyroid hormone-related protein binding to the parathyroid hormone receptor and design of conformation-selective peptidesJ Biol Chem 21(2):196–211.

Wang Z, Zhou XE, Motola DL, Gao X, Suino-Powell K, Conneely A, Ogata C, Sharma KK, Auchus RJ, Lok JB, Hawdon JM, Kliewer SA, Xu HE, Mangelsdorf DJ. 2009. Identification of the nuclear receptor DAF-12 as a therapeutic target in parasitic nematodesProc Natl Acad Sci U S A 106(23):9138–9143.


Kruse SW, Suino-Powell K, Zhou XE, Kretschman JE, Reynolds R, Vonrhein C, Xu Y, Wang L, Tsai SY, Tsai MJ, Xu HE. 2008. Identification of COUP-TFII orphan nuclear receptor as a retinoic acid-activated receptorPLoS Biol 6(9):e227.

Li Y, Kovach A, Suino-Powell K, Martynowski D, Xu HE. 2008. Structural and biochemical basis for the binding selectivity of peroxisome proliferator-activated receptor γ to PGC-1αJ Biol Chem 283(27): 19132–19139.

Li Y, Zhang J, Schopfer FJ, Martynowski D, Garcia-Barrio MT, Kovach A, Suino-Powell K, Baker PR, Freeman BA, Chen YE, Xu HE. 2008. Molecular recognition of nitrated fatty acids by PPARgNat Struct Mol Biol 15(8): 865–867.

Pioszak AA, Parker NR, Suino-Powell K, Xu HE. 2008. Molecular recognition of corticotropin releasing factor by its G protein-coupled receptor CRFR1J Biol Chem 283(47): 32900–32912.

Pioszak AA, Xu HE. 2008. Molecular recognition of parathyroid hormone by its G protein-coupled receptorProc Natl Acad Sci U S A 105(13):5034–5039.

Suino-Powell K, Xu Y, Zhang C, Tao YG, Tolbert WD, Simons Jr. SS, Xu HE. 2008. Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazolMol Cell Biol 28(6):1915–1923. 

Xu HE, Li Y. 2008. Ligand-dependent and –independent regulation of PPARg and orphan nuclear receptorsSci Signal 1(48): pe52.


Guo D, Sarkar J, Suino-Powell K, Xu Y, Matsumoto K, Jia Y, Yu S, Khare S, Haldar K, Rao MS, Foreman JE, Monga SPS, Peters JM, Xu HE, Reddy JK. 2007. Induction of nuclear translocation of constituitive androstane receptor by peroxisome proliferator-activated receptor α synthetic ligands in mouse liverJ Biol Chem 282(50): 36766–36776.

Tolbert WD, Daugherty J, Gao C, Xie Q, Miranti C, Gherardi E, Vande Woude GF, Xu HE. 2007. A mechanistic basis for converting a receptor tyrosine kinase agonist to an antagonistProc Natl Acad Sci U S A 104(37): 4592–14597.


Choi M, Moschetta A, Bookout AL, Peng L, Umetani M, Holmstrom SR, Suino-Powell K, Xu HE, Richardson JA, Gerard RD, Mangelsdorf DJ, Kliewer SA. 2006. Identification of a hormonal basis for gallbladder fillingNat Med 12(11): 1253–1235.

Motola DL, Cummins CL, Rottiers V, Sharma KK, Li T, Li Y, Suino-Powell K, Xu HE, Auchus RJ, Antebi A, Mangelsdorf DJ. 2006. Identification of ligands for DAF-12 that govern dauer formation and reproduction in C. elegansCell 124(6): 1209–1223.


Li Y, Choi M, Cavey G, Daugherty J, Suino K, Kovach A, Bingham NC, Kliewer SA, Xu HE. 2005. Crystallographic identification and functional characterization of phospholipids as ligands for the orphan nuclear receptor steroidogenic factor-1Mol Cell 17(4):491–502.

Li Y, Choi M, Suino K, Kovach A, Daugherty J, Kliewer SA, Xu HE. 2005. Structural and biochemical basis for selective repression of the orphan nuclear receptor liver receptor homolog 1 by small heterodimer partnerProc Natl Acad Sci U S A 102(27):9505–9510.

Li Y, Suino K, Daugherty J, Xu HE. 2005. Structural and biochemical mechanisms for the specificity of hormone binding and coactivator assembly by mineralocorticoid receptorMol Cell 19(3):367–380.


Suino K, Peng L, Reynolds R, Li Y, Cha JY, Repa JJ, Kliewer SA, Xu HE. 2004. The nuclear xenobiotic receptor CAR: structural determinants of constitutive activation and heterodimerizationMol Cell 16(6): 893–906.


Li Y, Lambert MH, Xu HE. 2003. Activation of nuclear receptors: a perspective from structural genomicsStructure 11(7):741–746.


Bledsoe RK, Montana VG, Stanley TB, Delves CJ, Apolito CJ, McKee DD, Consler TG, Parks DJ, Stewart EL, Willson TM, Lambert MH, Moore JT, Pearce KH, Xu HE. 2002. Crystal structure of the glucocorticoid receptor ligand binding domain reveals a novel mode of receptor dimerization and coactivator recognitionCell 110(1): 93–105.

Xu HE, Stanley TB, Montana VG, Lambert MH, Shearer BG, Cobb JE, McKee DD, Galardi CM, Plunket KD, Nolte RT, Moore JT, Kliewer SA, Willson TM, Stimmel JB.2002. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalphaNature 415(6873): 813–817.


Melcher K, and Xu HE. 2001. Gal80-Gal80 interaction on adjacent Gal4p binding sites is required for complete GAL gene repressionEMBO J 20(4): 841–851.

Oliver Jr. WR, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Snaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM. 2001. A selective peroxisome proliferator-activated receptor agonist promotes reverse cholesterol transportProc Natl Acad Sci U S A 98(9): 5306–5311.

Xu HE,  Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe Jr. RT, McKee DD, Moore JT, Willson TM. 2001. Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptorsProc Natl Acad Sci U S A 98(24): 13119–13124.


Gampe RT, Montana VG, Lambert MH, Miller AB, Bledsoe RK, Milburn MV, Kliewer SA, Willson TM, Xu HE. 2000. Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptorsMol Cell 5(3): 545–555.

Gampe Jr. RT, Montana VG, Lambert MH, Wisely GB, Milburn MV, Xu HE. 2000. Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helixGenes Dev 14(17): 2239–2241. 


Xu HE, Lambert MH, Montana VG, Parks DJ, Blanchard SG, Brown PJ, Sternbach DD, Lehmann LM, Wisely GB, Willson TM, Kliewer SA, Milburn MV. 1999. Molecular recognition of fatty acids by peroxisome proliferator-activated receptorsMol Cell 3(3): 397–403.

Xu HE, Rould MA, Xu W, Epstein JA, Pabo CO. 1999. Crystal structure of the human Pax6 paired domain-DNA complex reveals specific roles for the linker region and carboxy-terminal subdomain in DNA bindingGenes Dev 13(10): 1263–1275.