1. Discovery and optimization of chemical probes to define important molecular signals in medicine.
  2. Nature Reviews Drug Discovery article:   Chemical modulators of S1P receptors as barrier-oriented therapeutic molecules.   
  3. Nature Chemical Biology article: S1P1 signaling just keeps going and going and going…   
  4. Nature Biotechnology article:   Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.   
Home » Publications » Probe Publications
Probe Publications
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 ROR{alpha}/{gamma} Inverse Agonist.

 
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.

 
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.

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

5 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.

 
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.

2 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.

13 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.

3 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.

5 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.

3 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.

3 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.

5 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.

7 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.

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

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

9 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.

6 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.

17 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.

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

34 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.

4 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.

84 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.

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

42 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.  

108 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.

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

7 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.

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

263 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.

172 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.

197 Google Scholar Citations
 
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