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  1. Seminar at MSBoston 2014:  Phase 2 results of the RADIANCE trial...
  2. MS Drug Discovered at TSRI Is Safe and Effective in Phase II Study   
  3. Scripps Research Institute Scientists Identify First Potentially Effective Therapy for Human Prion Disease   
  4. Probe from SRIMSC Enters Phase II/III Clinical trials.   
  5. The Scripps Molecular Screening Center becomes the first to have 1000 AIDs in PubChem!   
  6. Receptos Scientists Publish Determination of a High Resolution S1P1 Structure in Science   
  7. NIH Common Fund researchers uncover structure of important target for drug design   
  8. NIH Research Matters: Designing New Diabetes Drugs   
  9. Discovery of a treatable mechanism for avoiding the deadly response to flu: North County Times, Eurekalert [1, 2]    
  10. Nature: Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand   
  11. Scripps Research and MIT scientists discover class of potent anti-cancer compounds    
  12. MLP Probe Project Leads to First in Human Studies    
  13. Business Wire:   Receptos Initiates Clinical Trials for S1P1 Agonist Program, Aimed at Multiple Sclerosis   
  14. Nature:   Quantitative reactivity profiling predicts functional cysteines in proteomes.

  15. Nature:   Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARc by Cdk5.
  16. Discovery and optimization of chemical probes to define important molecular signals in medicine.
  17. Nature Reviews Drug Discovery article:   Chemical modulators of S1P receptors as barrier-oriented therapeutic molecules.
  18. Nature Chemical Biology article: S1P1 signaling just keeps going and going and going…
  19. Nature Biotechnology article:   Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.
Home » Publications
Publications

 

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Conn PM, Smith E, Hodder P, Janovick JA, Smithson DC.
High Throughput Screen for Pharmacoperones of the Vasopressin Type 2 Receptor.

 
Thomas PW, Spicer T, Cammarata M, Brodbelt JS, Hodder P, Fast W
An altered zinc-binding site confers resistance to a covalent inactivator of New Delhi metallo-beta-lactamase-1 (NDM-1) discovered by high-throughput screening.

1 Google Scholar Citation
 
Karapetyan YE, Sferrazza GF, Zhou M, Ottenberg G, Spicer T, Chase P, Fallahi M, Hodder P, Weissmann C, Lasmézas CI.
Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents.

1 Google Scholar Citation
 
Yang H, Pinello CE, Luo J, Li D, Wang Y, Zhao LY, Jahn SC, Saldanha SA, Planck J, Geary KR, Ma H, Law BK, Roush WR, Hodder P, Liao D.
Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents.

1 Google Scholar Citation
 
George Cisar EA, Nguyen N, Rosen H.
A GTP affinity probe for proteomics highlights flexibility in purine nucleotide selectivity.

2 Google Scholar Citations
 
Matheu MP, Teijaro JR, Walsh KB, Greenberg ML, Marsolais D, Parker I, Rosen H, Oldstone MB, Cahalan MD.
Three Phases of CD8 T Cell Response in the Lung Following H1N1 Influenza Infection and Sphingosine 1 Phosphate Agonist Therapy.

 
Guerrero M, Urbano M, Schaeffer MT, Brown S, Rosen H, Roberts E.
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.

 
Khan PM, El-Gendy Bel-D, Kumar N, Garcia-Ordonez R, Lin L, Ruiz CH, Cameron MD, Griffin PR, Kamenecka TM.
Small molecule amides as potent ROR-? selective modulators.

 
Stevens RC, Cherezov V, Katritch V, Abagyan R, Kuhn P, Rosen H, Wüthrich K.
The GPCR Network: a large-scale collaboration to determine human GPCR structure and function.

18 Google Scholar Citations
 
Stevens RC, Cherezov V, Katritch V, Abagyan R, Kuhn P, Rosen H, Wüthrich K.
The GPCR Network: a large-scale collaboration to determine human GPCR structure and function.

18 Google Scholar Citations
 
Jacobs J, Grum-Tokars V, Zhou Y, Turlington M, Saldanha SA, Chase P, Eggler A, Dawson ES, Baez-Santos YM, Tomar S, Mielech AM, Baker SC, Lindsley CW, Hodder P, Mesecar A, Stauffer SR.
Discovery, synthesis, and structure-based optimization of a series of N-(tert-Butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease.

2 Google Scholar Citations
 
Nagano JM, Hsu KL, Whitby LR, Niphakis MJ, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder P, Srinivasan P, Gonzalez TD, Rosen H, Bahnson BJ, Cravatt BF.
Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2).

1 Google Scholar Citation
 
Oldstone MBA, Teijaro JR, Walsh KB, Rosen H.
Dissecting influenza virus pathogenesis uncovers a novel chemical approach to combat the infection.

3 Google Scholar Citations
 
Khan SH, Awasthi S, Guo C, Goswami D, Ling J, Griffin PR, Simons SS Jr, Kumar R.
Binding of the N-terminal region of coactivator TIF2 to the intrinsically disordered AF1 domain of the glucocorticoid receptor is accompanied by conformational reorganizations.

4 Google Scholar Citations
 
Hulleman JD, Brown SJ, Rosen H, Kelly JW.
A High-Throughput Cell-Based Gaussia Luciferase Reporter Assay for Identifying Modulators of Fibulin-3 Secretion.

1 Google Scholar Citation
 
Hsu KL, Tsuboi K, Adibekian A, Pugh H, Masuda K, Cravatt BF.
DAGLb inhibition perturbs a lipid network involved in macrophage inflammatory responses.

7 Google Scholar Citations
 
Hsu KL, Tsuboi K, Adibekian A, Pugh H, Masuda K, Cravatt BF.
DAGL? inhibition perturbs a lipid network involved in macrophage inflammatory responses.

7 Google Scholar Citations
 
Cahalan SM, Gonzalez-Cabrera PJ, Nguyen N, Guerrero M, George Cisar EA, Leaf NB, Brown SJ, Roberts E, Rosen H.
S1P1 Receptor Upregulation and Amelioration of Experimental Autoimmune Encephalomyelitis by an S1P1 Antagonist.

2 Google Scholar Citations
 
Chang MR, Goswami D, Mercer BA, Griffin PR.
The therapeutic potential of RORy modulators in the treatment of human disease.

 
Rosen H, Stevens RC, Hanson M, Roberts E, Oldstone MB.
Sphingosine-1-Phosphate and Its Receptors: Structure, Signaling and Influence.

5 Google Scholar Citations
 
Qin Q, Knapinska A, Dobri N, Madoux F, Chase P, Hodder P, Petrukhin K.
In Pursuit of Synthetic Modulators for the Orphan Retina-Specific Nuclear Receptor NR2E3.

2 Google Scholar Citations
 
Urbano M, Guerrero M, Zhao J, Velaparthi S, Adrian Saldanha S, Chase P, Wang Z, Civelli O, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E.
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7).

 
Ye L, Kleiner S, Wu J, Sah R, Gupta RK, Banks AS, Cohen P, Khandekar MJ, Boström P, Mepani RJ, Laznik D, Kamenecka TM, Song X, Liedtke W, Mootha VK, Puigserver P, Griffin PR, Clapham DE, Spiegelman BM.
TRPV4 Is a Regulator of Adipose Oxidative Metabolism, Inflammation, and Energy Homeostasis.

17 Google Scholar Citations
 
Pascal BD, Willis S, Lauer JL, Landgraf RR, West GM, Marciano D, Novick S, Goswami D, Chalmers MJ, Griffin PR.
HDX workbench: software for the analysis of H/D exchange MS data.

7 Google Scholar Citations
 
Solt LA, Kumar N, He Y, Kamenecka TM, Griffin PR, Burris TP.
Identification of a Selective ROR? Ligand That Suppresses T(H)17 Cells and Stimulates T Regulatory Cells.

6 Google Scholar Citations
 
Jo E, Bhhatarai B, Repetto E, Guerrero M, Riley S, Brown SJ, Kohno Y, Roberts E, Schurer SC, Rosen H.
Novel Selective Allosteric and Bitopic Ligands for the S1P3 Receptor.

5 Google Scholar Citations
 
Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder PS, Rosen H, Cravatt BF.
Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes.

10 Google Scholar Citations
 
1. Gonzalez-Cabrera PJ, Cahalan SM, Ferguson J, Rosen H.
S1P receptor modulators in cell trafficking therapeutics.

 
Dillon MB, Bachovchin DA, Brown SJ, Finn MG, Rosen H, Cravatt BF, Mowen KA.
Novel Inhibitors for PRMT1 Discovered by High-Throughput Screening Using Activity-Based Fluorescence Polarization.

3 Google Scholar Citations
 
Musille PM, Pathak MC, Lauer JL, Hudson WH, Griffin PR, Ortlund EA.
Antidiabetic phospholipid-nuclear receptor complex reveals the mechanism for phospholipid-driven gene regulation.

7 Google Scholar Citations
 
Amundsen SK, Spicer T, Karabulut AC, Londoño LM, Eberhardt C, Fernandez Vega V, Bannister TD, Hodder P, Smith GR.
Small-Molecule Inhibitors of Bacterial AddAB and RecBCD Helicase-Nuclease DNA Repair Enzymes.

1 Google Scholar Citation
 
Sarkisyan G, Cahalan S, Gonzalez-Cabrera P, Leaf N, Rosen H.
Real-time differential labeling of blood, interstitium and lymphatic and single-field analysis of vasculature dynamics in vivo.

2 Google Scholar Citations
 
Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC.
Crystal structure of a lipid G protein-coupled receptor.

145 Google Scholar Citations
 
Gonzalez-Cabrera PJ, Cahalan SM, Nguyen N, Sarkisyan G, Leaf NB, Cameron MD, Kago T, Rosen H.
S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis.

9 Google Scholar Citations
 
Kumar N, Lyda B, Chang MR, Lauer JL, Solt LA, Burris TP, Kamenecka T, Griffin PR.
Identification of SR2211: a potent synthetic ROR? selective modulator.

10 Google Scholar Citations
 
Burris TP, Busby SA, Griffin PR.
Targeting orphan nuclear receptors for treatment of metabolic diseases and autoimmunity.

13 Google Scholar Citations
 
Calamini B, Silva MC, Madoux F, Hutt DM, Khanna S, Chalfant MA, Saldanha SA, Hodder P, Tait BD, Garza D, Balch WE, Morimoto RI.
Small-molecule proteostasis regulators for protein conformational diseases.

46 Google Scholar Citations
 
Rillahan CD, Brown SJ, Register AC, Rosen H, Paulson JC.
High-throughput screening for inhibitors of sialyl- and fucosyltransferases.

5 Google Scholar Citations
 
Canny SA, Cruz Y, Southern MR, Griffin PR.
PubChem Promiscuity: a web resource for gathering compound promiscuity data from PubChem.

7 Google Scholar Citations
 
Guerrero M, Urbano M, Zhao J, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E.
Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P?-R) agonists.

3 Google Scholar Citations
 
Devarakonda S, Gupta K, Chalmers MJ, Hunt JF, Griffin PR, Van Duyne GD, Spiegelman BM.
Disorder-to-order transition underlies the structural basis for the assembly of a transcriptionally active PGC-1?/ERR? complex.

11 Google Scholar Citations
 
Gonzalez-Cabrera PJ, Cahalan SM, Nguyen N, Sarkisyan G, Leaf NB, Cameron M, Kago T, Rosen H.
S1P1 Receptor Modulation with Cyclical Recovery from Lymphopenia Ameliorates Mouse Model of Multiple Sclerosis.

9 Google Scholar Citations
 
Roth J, Minond D, Darout E, Liu Q, Lauer J, Hodder P, Fields GB, Roush WR.
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.

6 Google Scholar Citations
 
Urbano M, Guerrero M, Velaparthi S, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E.
Discovery, synthesis and SAR analysis of novel selective small molecule S1P(4)-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype.

1 Google Scholar Citation
 
Peatey CL, Spicer T, Hodder P, Trenholme KR, Gardiner DL.
A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes.

  14 Google Scholar Citations
 
Iwasaki A, Medzhitov R.
A new shield for a cytokine storm.

7 Google Scholar Citations
 
Teijaro JR, Walsh KB, Cahalan S, Fremgen DM, Roberts E, Scott F, Martinborough E, Peach R, Oldstone MB, Rosen H.
Endothelial Cells Are Central Orchestrators of Cytokine Amplification during Influenza Virus Infection.

94 Google Scholar Citations
 
Urbano M, Guerrero M, Zhao J, Velaparthi S, Schaeffer MT, Brown S, Rosen H, Roberts E.
SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P?) receptor.

6 Google Scholar Citations
 
Walsh KB, Teijaro JR, Rosen H, Oldstone MB.
Quelling the storm: utilization of sphingosine-1-phosphate receptor signaling to ameliorate influenza virus-induced cytokine storm.

11 Google Scholar Citations
 
Tsuboi K, Bachovchin DA, Speers AE, Spicer TP, Fernandez-Vega V, Hodder P, Rosen H, Cravatt BF.
Potent and Selective Inhibitors of Glutathione S-transferase Omega 1 that Impair Cancer Drug Resistance.

9 Google Scholar Citations
 
Choi JH, Banks AS, Kamenecka TM, Busby SA, Chalmers MJ, Kumar N, Kuruvilla DS, Shin Y, He Y, Bruning JB, Marciano DP, Cameron MD, Laznik D, Jurczak MJ, Schürer SC, Vidovi? D, Shulman GI, Spiegelman BM, Griffin PR.
Antidiabetic actions of a non-agonist PPAR? ligand blocking Cdk5-mediated phosphorylation.

106 Google Scholar Citations
 
Bialkowska A, Crisp M, Bannister T, He Y, Chowdhury S, Schurer S, Chase P, Spicer T, Madoux F, Tian C, Hodder P, Zaharevitz D, Yang VW.
Identification of Small-Molecule Inhibitors of the Colorectal Cancer Oncogene Kruppel-Like Factor 5 Expression by Ultrahigh-Throughput Screening.

9 Google Scholar Citations
 
West GM, Chien EY, Katritch V, Gatchalian J, Chalmers MJ, Stevens RC, Griffin PR.
Ligand-Dependent Perturbation of the Conformational Ensemble for the GPCR Beta(2) Adrenergic Receptor Revealed by HDX.

29 Google Scholar Citations
 
Walsh KB, Teijaro JR, Wilker PR, Jatzek A, Fremgen DM, Das SC, Watanabe T, Hatta M, Shinya K, Suresh M, Kawaoka Y, Rosen H, Oldstone MB.
Suppression of cytokine storm with a sphingosine analog provides protection against pathogenic influenza virus.

40 Google Scholar Citations
 
Lone AM, Bachovchin DA, Westwood D, Speers AE, Spicer TP, Fernandez-Vega V, Chase P, Hodder P, Rosen H, Cravatt BF, Saghatelian A.
A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors.

6 Google Scholar Citations
 
Guerrero M, Urbano M, Velaparthi S, Zhao J, Schaeffer MT, Brown S, Rosen H, Roberts E.
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.

6 Google Scholar Citations
 
Bachovchin DA, Zuhl AM, Speers AE, Wolfe MR, Weerapana E, Brown SJ, Rosen H, Cravatt BF.
Discovery and Optimization of Sulfonyl Acrylonitriles as Selective, Covalent Inhibitors of Protein Phosphatase Methylesterase-1.

13 Google Scholar Citations
 
Lee JM, Lee YK, Mamrosh JL, Busby SA, Griffin PR, Pathak MC, Ortlund EA, Moore DD.
A nuclear-receptor-dependent phosphatidylcholine pathway with antidiabetic effects.

47 Google Scholar Citations
 
Adibekian A, Martin BR, Wang C, Hsu KL, Bachovchin DA, Niessen S, Hoover H, Cravatt BF.
Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors.

44 Google Scholar Citations
 
Jetten A.M.
Immunology: A helping hand against autoimmunity

8 Google Scholar Citations
 
Lee Y, Choi JY, Fu H, Harvey C, Ravindran S, Roush WR, Boothroyd JC, Khosla C.
Chemistry and biology of macrolide antiparasitic agents.

5 Google Scholar Citations
 
Solt LA, Kumar N, Nuhant P, Wang Y, Lauer JL, Liu J, Istrate MA, Kamenecka TM, Roush WR, Vidovic D, Schürer SC, Xu J, Wagoner G, Drew PD, Griffin PR, Burris TP
Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand

83 Google Scholar Citations
 
Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Wang Y, Busby SA, Pascal BD, Garcia-Ordonez RD, Bruning JB, Istrate MA, Kojetin DJ, Dodge JA, Burris TP, Griffin PR.
DNA binding alters coactivator interaction surfaces of the intact VDR-RXR complex.

45 Google Scholar Citations
 
Baillargeon P, Scampavia L, Einsteder R, Hodder P
Monitoring of HTS Compound Library Quality via a High-Resolution Image Acquisition and Processing Instrument

2 Google Scholar Citations
 
Bachovchin DA, Mohr JT, Speers AE, Wang C, Berlin JM, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Schürer SC, Nomura DK, Rosen H, Fu GC, Cravatt BF
Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors

22 Google Scholar Citations
 
Schürer, S.C.; Vempati, U.; Smith, R.; Southern, M.R.; Lemmon, V.
BioAssay Ontology Annotations Facilitate Cross-Analysis of Diverse High-throughput-Screening Data Sets

15 Google Scholar Citations
 
Calahan SM, Gonzalez-Cabrera PJ, Sarkisyan G, Nguyen N, Schaeffer MT, Huang L, Yeager A, Clemons B, Scott F, Rosen H
Actions of a picomolar short-acting S1P1 agonist in S1P1-eGFP knock-in mice

13 Google Scholar Citations
 
Chalmers MJ, Busby SA, Pascal BD, West GM, Griffin PR.
Differential hydrogen/deuterium exchange mass spectrometry analysis of protein-ligand interactions.

26 Google Scholar Citations
 
Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ.
Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.

39 Google Scholar Citations
 
Willis S, Griffin PR.
Mutual information identifies sequence positions conserved within the nuclear receptor superfamily: approach reveals functionally important regions for DNA binding specificity.

 
Istrate MA, Spicer TP, Wang Y, Bernard JA, Helvering LM, Bocchinfuso WP, Richardson TI, Zink R, Kumar N, Montrose-Rafizadeh C, Dodge J, Hodder P, Griffin PR.
Development of an HTS-Compatible Assay for Discovery of ROR{alpha} Modulators Using AlphaScreen(R) Technology.

 
Southern M, Griffin P.
A Java API for working with PubChem data-sets.

2 Google Scholar Citations
 
Wright E, Busby SA, Wisecarver S, Vincent J, Griffin PR, Fernandez EJ.
Helix 11 dynamics is critical for constitutive androstane receptor activity.

7 Google Scholar Citations
 
Vidovic D., Busby S.A., Griffin P.R., Schürer S.C.
A Combined Ligand- and Structure-Based Virtual Screening Protocol Identifies Submicromolar PPAR? Partial Agonists

14 Google Scholar Citations
 
Kumar N, Kojetin D, Solt L, Kumar K, Nuhant P, Duckett D, Cameron M, Butler A, Roush W, Griffin PR, Burris TP.
Identification of ML176 (SR3335): a Synthetic ROR? Selective Inverse Agonist.

14 Google Scholar Citations
 
Doghman M, Madoux F, Hodder P, Lalli E.
Identification and characterization of steroidogenic factor-1 inverse agonists.

2 Google Scholar Citations
 
Weerapana E, Wang C, Simon GM, Richter F, Khare S, Dillon MB, Bachovchin DA, Mowen K, Baker D, Cravatt BF.
Quantitative reactivity profiling predicts functional cysteines in proteomes.

151 Google Scholar Citations
 
Hydrogen/Deuterium Exchange Reveals Distinct Agonist/Partial Agonist Receptor Dynamics within Vitamin D Receptor/Retinoid X Receptor Heterodimer.
Zhang J, Chalmers M.J., Stayrook K.R., Burris L.L., Garcia-Ordonez R.D., Pascal B.D., Burris T.P., Dodge J.A., Griffin P.R.

25 Google Scholar Citations
 
Marsolais, D., Yagi, S., Kago, T., Leaf, N. & Rosen, H.
Modulation of chemokines and allergic airway inflammation by selective local S1P1 agonism in lung.

10 Google Scholar Citations
 
Madoux F, Simanski S, Chase P, Mishra JK, Roush WR, Ayad NG, Hodder P.
An ultra-high throughput cell-based screen for wee1 degradation inhibitors.

5 Google Scholar Citations
 
Chalmers MJ, Pascal BD, Willis S, Zhang J, Iturria SJ, Dodge JA, Griffin PR.
Methods for the Analysis of High Precision Differential Hydrogen Deuterium Exchange Data.

12 Google Scholar Citations
 
Knuckley B, Jones JE, Bachovchin DA, Slack J, Causey CP, Brown SJ, Rosen H, Cravatt BF, Thompson PR.
A fluopol-ABPP HTS assay to identify PAD inhibitors.

16 Google Scholar Citations
 
Wang Y, Kumar N, Nuhant P, Cameron MD, Istrate MA, Roush WR, Griffin PR, Burris TP.
Identification of a Synthetic Agonist for the Orphan Nuclear Receptors RORalpha and RORgamma, SR1078.

21 Google Scholar Citations
 
Gianni D, Taulet N, Zhang H, Dermardirossian C, Kister J, Martinez L, Roush WR, Brown SJ, Bokoch G, Rosen H.
A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells.

37 Google Scholar Citations
 
Jang Hyun Choi, Alexander S. Banks, Jennifer L. Estall1, Shingo Kajimura1, Pontus Bostrom, Dina Laznik, Jorge L. Ruas, Michael J. Chalmers, Theodore M. Kamenecka, Matthias Bluher, Patrick R. Griffin & Bruce M. Spiegelman
Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARc by Cdk5

257 Google Scholar Citations
 
Weide T, Saldanha SA, Minond D, Spicer TP, Fotsing JR, Spaargaren M, Frère JM, Bebrone C, Sharpless KB, Hodder PS, Fokin VV.
NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-beta-Lactamase: Synthesis and Structure-Activity Studies.

12 Google Scholar Citations
 
Solt LA, Griffin PR, Burris TP.
Ligand regulation of retinoic acid receptor-related orphan receptors: implications for development of novel therapeutics.

17 Google Scholar Citations
 
Brunell D, Weissbach H, Hodder P, Brot N.
A High-Throughput Screening Compatible Assay for Activators and Inhibitors of Methionine Sulfoxide Reductase A.

4 Google Scholar Citations
 
Kumar N., Solt L.A., Wang Y., Rogers P.M., Bhattacharyya G., Kamenecka T.M., Stayrook K.R., Crumbley C., Floyd Z.E., Gimble J.M., Griffin P.R., and Burris T.P.
Regulation of Adipogenesis by Natural and Synthetic REV-ERB Ligands

36 Google Scholar Citations
 
Grimm C, Jörs S, Saldanha SA, Obukhov AG, Pan B, Oshima K, Cuajungco MP, Chase P, Hodder P, Heller S.
Small Molecule Activators of TRPML3.

26 Google Scholar Citations
 
A second class of nuclear receptors for oxysterols: Regulation of RORalpha and RORgamma activity by 24S-hydroxycholesterol (cerebrosterol).
Wang Y, Kumar N, Crumbley C, Griffin PR, Burris TP.

32 Google Scholar Citations
 
Kota S, Scampavia L, Spicer T, Beeler AB, Takahashi V, Snyder JK, Porco JA, Hodder P, Strosberg AD.
A time-resolved fluorescence-resonance energy transfer assay for identifying inhibitors of hepatitis C virus core dimerization.

11 Google Scholar Citations
 
Walsh KB, Marsolais D, Welch MJ, Rosen H, Oldstone MB.
Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection.

9 Google Scholar Citations
 
Wang Y, Kumar N, Solt LA, Richardson TI, Helvering LM, Crumbley C, Garcia-Ordonez RD, Stayrook KR, Zhang X, Novick S, Chalmers MJ, Griffin PR, Burris TP.
Modulation of retinoic acid receptor-related orphan receptor alpha and gamma activity by 7-oxygenated sterol ligands.

56 Google Scholar Citations
 
Bachovchin DA, Wolfe MR, Masuda K, Brown SJ, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF.
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).

13 Google Scholar Citations
 
Minond D, Saldanha SA, Subramaniam P, Spaargaren M, Spicer T, Fotsing JR, Weide T, Fokin VV, Sharpless KB, Galleni M, Bebrone C, Lassaux P, Hodder P.
Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.

20 Google Scholar Citations
 
Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez R, Burris TP, Griffin PR.
The benzenesulfonamide T0901317 is a novel RORa/g Inverse Agonist.

49 Google Scholar Citations
 
Brothers SP, Saldanha SA, Spicer TP, Cameron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS.
Selective and Brain Penetrant Neuropeptide Y Y2 Receptor Antagonists Discovered by Whole-Cell High Throughput Screening.

23 Google Scholar Citations
 
Noël R, Song X, Jiang R, Chalmers MJ, Griffin PR, Kamenecka TM.
Efficient methodology for the synthesis of 3-amino-1,2,4-triazoles.

7 Google Scholar Citations
 
Cudic M, Burstein GD, Fields GB, Lauer-Fields J.
Analysis of flavonoid-based pharmacophores that inhibit aggrecanases (ADAMTS-4 and ADAMTS-5) and matrix metalloproteinases through the use of topologically constrained peptide substrates.

9 Google Scholar Citations
 
Dai SY, Burris TP, Dodge JA, Montrose-Rafizadeh C, Wang Y, Pascal BD, Chalmers MJ, Griffin PR.
Unique Ligand Binding Patterns Between Estrogen Receptor and Revealed by Hydrogen/Deuterium Exchange.

24 Google Scholar Citations
 
Lauer-Fields JL, Chalmers MJ, Busby SA, Minond D, Griffin PR, Fields GB.
Identification of specific hemopexin-like domain residues that facilitate matrix metalloproteinase collagenolytic activity.

33 Google Scholar Citations
 
Cahalan S., and Rosen H.
S1P1 signaling just keeps going and going and going…

 
Bachovchin DA, Brown SJ, Rosen H, Cravatt BF.
Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.

83 Google Scholar Citations
 
Doghman M, Cazareth J, Douguet D, Madoux F, Hodder P, Lalli E.
Inhibition of adrenocortical carcinoma cells proliferation by SF-1 inverse agonists.

37 Google Scholar Citations
 
Stephan C. Schürer, Steven J. Brown, Pedro Gonzales Cabrera, Marie-Therese Schaeffer, Jacqueline Chapman, Euijung Jo, Peter Chase, Tim Spicer,  Peter Hodder and Hugh Rosen.
Ligand-binding pocket shape differences between S1P1 and S1P3 determine efficiency of chemical probe identification by uHTS.

34 Google Scholar Citations
 
Gonzalez-Cabrera PJ, Jo E, Sanna MG, Brown S, Leaf N, Marsolais D, Schaeffer MT, Chapman J, Cameron M, Guerrero M, Roberts E, Rosen H.
Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like head-group interactions.

42 Google Scholar Citations
 
David Marsolais, Bumsuk Hahm, Kurt H. Edelmann, Kevin B. Walsh, Miguel Guerrero, Yasuko Hatta, Yoshihiro Kawaoka, Edward Roberts, Michael B. A. Oldstone and Hugh Rosen.
Local not systemic modulation of dendritic cell S1P receptors in lung blunts virus-specific immune responses to influenza.

30 Google Scholar Citations
 
Rosen, H., P. Gonzalez-Cabrera, D. Marsolais, S. Cahalan, A.S. Don, and M.G. Sanna.
Modulating tone: the overture of S1P receptor immunotherapeutics.

54 Google Scholar Citations
 
Dai SY, Chalmers MJ, Bruning J, Bramlett KS, Osborne HE, Montrose-Rafizadeh C, Barr RJ, Wang Y, Wang M, Burris TP, Dodge JA, Griffin PR.
Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method.

41 Google Scholar Citations
 
A.S. Don, H. Rosen.
A fluorescent plate reader assay for ceramide kinase.

9 Google Scholar Citations
 
Roth, J., F. Madoux, P. Hodder, and W.R. Roush. 2008.
Synthesis of Small Molecule Inhibitors of the Orphan Nuclear Receptor Steroidogenic Factor-1 (NR5A1) Based on Isoquinolinone Scaffolds.

20 Google Scholar Citations
 
Madoux, F., X. Li, P. Chase, G. Zastrow, M. Cameron, J. Conkright, P. Griffin, S. Thacher, and P. Hodder.
Potent, selective and cell penetrant inhibitors of SF-1 by functional uHTS.

28 Google Scholar Citations
 
Nakai, R., C.M. Salisbury, H. Rosen, and B.F. Cravatt.
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.

13 Google Scholar Citations
 
Lauer-Fields, J.L., D. Minond, P.S. Chase, P.E. Baillargeon, S.A. Saldanha, R. Stawikowska, P. Hodder, and G.B. Fields.
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.

28 Google Scholar Citations
 
Niessen, F., F. Schaffner, C. Furlan-Freguia, R. Pawlinski, G. Bhattacharjee, J. Chun, C.K. Derian, P. Andrade-Gordon, H. Rosen, and W.Ruf.
Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation.

159 Google Scholar Citations
 
Guha, R., and S. Schurer.
Utilizing high throughput screening data for predictive toxicology models: protocols and application to MLSCN assays.

30 Google Scholar Citations
 
Lauer-Fields JL, Spicer TP, Chase PS, Cudic M, Burstein GD, Nagase H, Hodder P, Fields GB.
Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate.

11 Google Scholar Citations
 
Don AS, Rosen H.
A lipid binding domain in sphingosine kinase 2.

18 Google Scholar Citations
 
Marsolais D, Hahm B, Walsh KB, Edelmann KH, McGavern D, Hatta Y, Kawaoka Y, Rosen H, Oldstone MB.
A critical role for the sphingosine analog AAL-R in dampening the cytokine response during influenza virus infection.

46 Google Scholar Citations
 
Niessen F, Furlan-Freguia C, Fernandez JA, Mosnier LO, Castellino FJ, Weiler H, Rosen H, Griffin JH, Ruf W.
Endogenous EPCR/aPC-PAR1 signaling prevents inflammation-induced vascular leakage and lethality.

54 Google Scholar Citations
 
Thomas Schröter, Dmitriy Minond, Amiee Weiser, Chinh Dao, Jeff Habel, Timothy Spicer, Peter Chase, Pierre Baillargeon, Louis Scampavia, Stephan Schürer, Caty Chung, Chris Mader, Mark Southern, Nick Tsinoremas, Philip LoGrasso and Peter Hodder.
Comparison of Miniaturized Time-Resolved Fluorescence Resonance Energy Transfer and Enzyme-Coupled Luciferase High-Throughput Screening Assays to Discover Inhibitors of Rho-Kinase II (ROCK-II).

32 Google Scholar Citations
 
Rosen, H., Gozalez-Cabrera P., Sanna M., and Brown S.
Sphingosine 1-phosphate receptor signaling.

179 Google Scholar Citations
 
Marsolais, D., and Rosen H.
Chemical modulators of S1P receptors as barrier-oriented therapeutic molecules

76 Google Scholar Citations
 
Fazilleau N., McHeyzer-Williams L., Rosen H., and McHeyzer-Wilaims M.
Follicular helper T cell function is regulated by the strength of TCR binding.

139 Google Scholar Citations
 
Tsukada, Y.T., M.G. Sanna, H. Rosen, and R.A. Gottlieb.
S1P1-selective agonist SEW2871 exacerbates reperfusion arrhythmias.

20 Google Scholar Citations
 
Lee H-K, Brown SJ, Rosen H, Tobias PS
Application of beta-lactamase Enzyme Complementation to the High-Throughput Screening of Toll-Like Receptor Signaling Inhibitors.

16 Google Scholar Citations
 
Don A, Martinez-Lamenca C, Webb WR, Proia RL, Roberts E, Rosen H
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogs.

38 Google Scholar Citations
 
Gonzalez-Cabrera P, Hla T, Rosen H
Mapping pathways downstream of sphingosine 1-phosphate subtype 1 by differential chemical perturbation and proteomics.

64 Google Scholar Citations
 
Rosen H, Sanna MG, Cahalan S, Gonzalez-Cabrera P
Tipping the gatekeeper: S1P regulation of stromal barrier function.

110 Google Scholar Citations
 
Feng Y, Cameron MD, Frackowiak B, Griffin E, Lin L, Ruiz C, Schröter T, LoGrasso P.
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.

23 Google Scholar Citations
 
Sanna MG, Wang SK, Gonzalez-Cabrera P, Don A, Marsolais D, Jo E, Cheng WC, Wong CH, Rosen H.
Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo.

240 Google Scholar Citations
 
Alfonso C, McHeyzer-Williams MG, Rosen H
CD69 down-modulation and inhibition of thymic egress by short and long-term selective chemical agonism of S1P1 receptors.

45 Google Scholar Citations
 
Chun, J. and H. Rosen.
Lysophospholipid receptors as potential drug targets in tissue transplantation and autoimmune diseases.

67 Google Scholar Citations
 
Wei SH, Rosen H, Matheu MP, Sanna MG, Wang SK, Jo E, Wong CH, Parker I, Cahalan MD.
Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses.  

218 Google Scholar Citations
 
Martinez X, Kreuwel HTC, Redmond WL, Trenney R, Hunter K, Rosen H, Sarvetnick N, Wicker LS, Sherman LA.
CD8+ T cell tolerance in NOD mice is restored by insulin dependent diabetes (Idd) resistance alleles.

27 Google Scholar Citations
 
Rosen H.
Chemical approaches to the lysophospholipid receptors.

9 Google Scholar Citations
 
Jo E, Sanna MG, Gonzalez-Cabrera PJ, Thangada S, Tigy G, Osborne DA, Hla T, Parrill AL, Rosen H.
S1P1-selective in vivo-active agonist from high throughput screening: Off-the-shelf chemical probes of receptor interactions, signaling and fate.

163 Google Scholar Citations
 
Rosen, H. & Goetzl, E.J.
Sphingosine 1-phosphate and its receptors: An autocrine and paracrine network.

453 Google Scholar Citations
 
Gong Q, Ou Q, Ye S, Lee WP, Cornelius J, Diehl L, Lin WY, Hu Z, Lu Y, Chen Y, Wu Y, Meng YG, Gribling P, Lin Z, Nguyen K, Tran T, Zhang Y, Rosen H, Martin F, Chan AC.
Importance of cellular microenvironment and circulatory dynamics in B cell immunotherapy.

321 Google Scholar Citations
 
Sanna, G., Liao, J., Jo, E., Alfonso, C., Ahn, M., Peterson, M., Webb, B., Lefebvre, S., Chun, J., Gray, N., Rosen, H.
Spingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.

405 Google Scholar Citations
 


MS Drug Discovered at TSRI is Safe and Effective in Phase II Study

 

A compound discovered and synthesized in The Scripps Research Institute (TSRI) labs of Professors Hugh Rosen and Edward Roberts has provided positive results for safety and efficacy in Phase 2 clinical trials for relapsing multiple sclerosis, according to Receptos, the biopharmaceutical company developing the drug for approval by the US Food and Drug Administration.

“The Rosen and Roberts laboratories are very gratified to see these direct improvements in the lives of patients and families dealing with this debilitating illness,” said Rosen. “These data support our labs' approach at TSRI—that discovery of fundamental mechanisms in chemical biology provides the foundation for intelligent intervention in disease processes. Meeting the needs of patients and their families is our high calling in biomedical science.”

The drug candidate, RPC1063, was first discovered at TSRI from work in the National Institutes of Health (NIH) Molecular Libraries Initiative. The randomized, double-blind Phase 2 study assessed the efficacy, safety and tolerability of two orally administered doses of RPC1063 against placebo in 258 patients with relapsing multiple sclerosis across 77 sites in 13 countries. There was a highly statistically significant 86 percent reduction in MRI measures of disease activity.

A Phase 3 trial—a randomized, double-blind study involving 1,200 patients with relapsing multiple sclerosis—was launched in December 2013.

The detailed clinical abstract can be found  here.

Copyright (c) 2008-2011 TSRI.