has collaborator Chien, Jeremy Associate Professor in Division of Molecular Medicine Lee, Sam A Associate Professor Matlawska-Wasowska, Ksenia Faculty Member Oprea, Tudor I. Professor Wandinger-Ness, Angela Professor
selected publications academic article Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.. Journal of medicinal chemistry. 63:10984-11011. 2020 A Selective Ligand for Estrogen Receptor Proteins Discriminates Rapid and Genomic Signaling.. Cell chemical biology. 26:1692-1702.e5. 2019 Autophagy, Inflammation, and Metabolism (AIM) Center in its second year.. Autophagy. :1-5. 2019 Activation of Rho Family GTPases by Small Molecules.. ACS chemical biology. 13:1514-1524. 2018 High-Throughput Flow Cytometry Identifies Small-Molecule Inhibitors for Drug Repurposing in T-ALL.. SLAS Discovery. 23:732-741. 2018 Pharos: Collating protein information to shed light on the druggable genome.. Nucleic acids research. 45:D995-D1002. 2017 Novel ABCG2 Antagonists Reverse Topotecan-Mediated Chemotherapeutic Resistance in Ovarian Carcinoma Xenografts.. Molecular cancer therapeutics. 15:2853-2862. 2016 Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia. 2016 ----Cyclic AMP efflux inhibitors as potential therapeutic agents for leukemia.. Oncotarget. :-. 2016 Badapple: promiscuity patterns from noisy evidence.. Journal of cheminformatics. 8:-. 2016 Discovery of Small-Molecule Nonfluorescent Inhibitors of Fluorogen-Fluorogen Activating Protein Binding Pair.. Journal of biomolecular screening. :-. 2015 R-ketorolac Targets Cdc42 and Rac1 and Alters Ovarian Cancer Cell Behaviors Critical for Invasion and Metastasis.. Molecular cancer therapeutics. :-. 2015 A novel pharmacologic activity of ketorolac for therapeutic benefit in ovarian cancer patients.. Clinical cancer research : an official journal of the American Association for Cancer Research. :-. 2015 A high-throughput phenotypic screen of cytotoxic T lymphocyte lytic granule exocytosis reveals candidate immunosuppressants.. Journal of biomolecular screening. 20:359-371. 2015 A Pan-GTPase Inhibitor as a Molecular Probe. 2015 FRET detection of lymphocyte function-associated antigen-1 conformational extension.. Molecular biology of the cell. 26:43-54. 2015 Novel Activities of Select NSAID R-Enantiomers against Rac1 and Cdc42 GTPases. 2015 Pharmaceutical screen identifies novel target processes for activation of autophagy with a broad translational potential.. Nature communications. 6:-. 2015 Quantitative Bead-Based Flow Cytometry for Assaying Rab7 GTPase Interaction with the Rab-Interacting Lysosomal Protein (RILP) Effector Protein. 2015 Relationship of light scatter change and cdc42-regulated actin status.. Cytometry. Part B, Clinical cytometry. :-. 2015 The evaluation of thioridazine as a hematopoietic progenitor cell mobilizing agent in healthy human subjects.. Journal of clinical pharmacology. :-. 2014 A high throughput flow cytometric assay platform targeting transporter inhibition.. Drug discovery today. Technologies. 12:e95-103. 2014 Selective chemical inhibition of agr quorum sensing in Staphylococcus aureus promotes host defense with minimal impact on resistance. 2014 An automated high-throughput cell-based multiplexed flow cytometry assay to identify novel compounds to target Candida albicans virulence-related proteins. 2014 Carbon monoxide down-regulates α4β1 integrin-specific ligand binding and cell adhesion: a possible mechanism for cell mobilization.. BMC immunology. 15:-. 2014 Identification of Isoxsuprine Hydrochloride as a Neuroprotectant in Ischemic Stroke through Cell-Based High-Throughput Screening. 2014 Real-time detection of protein trafficking with high-throughput flow cytometry (HTFC) and fluorogen-activating protein (FAP) base biosensor.. Current protocols in cytometry / editorial board, J. Paul Robinson, managing editor ... [et al.]. 67:-. 2014 Targeting GTPases in Parkinson's disease: comparison to the historic path of kinase drug discovery and perspectives.. Frontiers in molecular neuroscience. 7:-. 2014 High-throughput flow cytometry compatible biosensor based on fluorogen activating protein technology.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 83:220-226. 2013 Characterization of a Cdc42 GTPase Inhibitor and its Use as a Molecular Probe.. The Journal of biological chemistry. :8531. 2013 Characterization of a Cdc42 protein inhibitor and its use as a molecular probe. 2013 Fluorescent substrates for flow cytometric evaluation of efflux inhibition in ABCB1, ABCC1, and ABCG2 transporters.. Analytical biochemistry. 437:77-87. 2013 The University of New Mexico Center for Molecular Discovery.. Combinatorial chemistry & high throughput screening. 17:256-265. 2013 A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition.. ACS chemical biology. 7:1095-1108. 2012 A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition.. ACS chemical biology. 7:1095-1108. 2012 A Selective ATP-Binding Cassette Subfamily G Member 2 Efflux Inhibitor Revealed via High-Throughput Flow Cytometry.. Journal of biomolecular screening. :-. 2012 A novel flow cytometric HTS assay reveals functional modulators of ATP binding cassette transporter ABCB6.. PloS one. 7:-. 2012 Aspects of VLA-4 and LFA-1 regulation that may contribute to rolling and firm adhesion.. Frontiers in immunology. 3:-. 2012 Cluster cytometry for high-capacity bioanalysis.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 81:419-429. 2012 Discovery of regulators of receptor internalization with high-throughput flow cytometry.. Molecular pharmacology. 82:645-657. 2012 Identification of a small molecule yeast TORC1 inhibitor with a multiplex screen based on flow cytometry.. ACS chemical biology. 7:715-722. 2012 Inhibitors of V-ATPase proton transport reveal uncoupling functions of tether linking cytosolic and membrane domains of V0 subunit a (Vph1p).. The Journal of biological chemistry. 287:10236-10250. 2012 Overview: assays for studying integrin-dependent cell adhesion.. Methods in molecular biology (Clifton, N.J.). 757:3-14. 2012 Targeting the Transposase Domain of the DNA Repair Component Metnase to Enhance Chemotherapy.. Cancer research. 72:6200-6208. 2012 GPR30 expression is required for the mineralocorticoid receptor-independent rapid vascular effects of aldosterone.. Hypertension (Dallas, Tex. : 1979). 57:442-451. 2011 A miniature Couette to generate shear for flow cytometry: studying real-time modulation of intracellular calcium in monocytic cells.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 79:233-240. 2011 Associating Drugs, Targets and Clinical Outcomes into an Integrated Network Affords a New Platform for Computer-Aided Drug Repurposing.. Molecular informatics. 30:100-111. 2011 Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists.. The Journal of biological chemistry. 286:5455-5463. 2011 Drug Repurposing from an Academic Perspective.. Drug discovery today. Therapeutic strategies. 8:61-69. 2011 Drug Repurposing from an Academic Perspective.. Drug discovery today. Therapeutic strategies. 8:61-69. 2011 Drug Repurposing from an Academic Perspective.. Drug discovery today. Therapeutic strategies. 8:61-69. 2011 High-throughput screen for the chemical inhibitors of antiapoptotic bcl-2 family proteins by multiplex flow cytometry.. Assay and drug development technologies. 9:465-474. 2011 Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity.. The Journal of steroid biochemistry and molecular biology. 127:358-366. 2011 Is prolonged stem cell mobilization detrimental for hematopoiesis?. Medical hypotheses. 77:1111-1113. 2011 Microbial efflux pump inhibition: tactics and strategies.. Current pharmaceutical design. 17:1291-1302. 2011 Nitric oxide/cGMP pathway signaling actively down-regulates ?4?1-integrin affinity: an unexpected mechanism for inducing cell de-adhesion.. BMC immunology. 12:-. 2011 Quantum dots for quantitative flow cytometry.. Methods in molecular biology (Clifton, N.J.). 699:67-84. 2011 Real-time analysis of the inside-out regulation of lymphocyte function-associated antigen-1 revealed similarities to and differences from very late antigen-4.. The Journal of biological chemistry. 286:20375-20386. 2011 Simultaneous in vitro molecular screening of protein-peptide interactions by flow cytometry, using six Bcl-2 family proteins as examples.. Nature protocols. 6:943-952. 2011 Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.. Journal of medicinal chemistry. 53:1004-1014. 2010 A small molecule pan-inhibitor of Ras-superfamily GTPases with high efficacy towards Rab7 2010 High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.. Assay and drug development technologies. 8:37-46. 2010 Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs.. Organic & biomolecular chemistry. 8:2252-2259. 2010 Identification of a small GTPase inhibitor using a high-throughput flow cytometry bead-based multiplex assay.. Journal of biomolecular screening. 15:10-20. 2010 Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry.. Analytical biochemistry. 398:203-211. 2010 Influence of charge on cell permeability and tumor imaging of GPR30-targeted 111in-labeled nonsteroidal imaging agents.. ACS chemical biology. 5:681-690. 2010 Profiling a Selective Probe for RTG Branch of Yeast TORC1 Signaling Pathway 2010 Real-time partitioning of octadecyl rhodamine B into bead-supported lipid bilayer membranes revealing quantitative differences in saturable binding sites in DOPC and 1:1:1 DOPC/SM/cholesterol membranes. 2010 Recognition of decay accelerating factor and alpha(v)beta(3) by inactivated hantaviruses: Toward the development of high-throughput screening flow cytometry assays.. Analytical biochemistry. 402:151-160. 2010 Selective Bcl-2 Inhibitor Probes 2010 Selective Efflux Inhibition of ATP-binding Cassette Sub-family G Member 2 2010 Effect of DOTA position on melanoma targeting and pharmacokinetic properties of 111In-labeled lactam bridge-cyclized alpha-melanocyte stimulating hormone peptide.. Bioconjugate chemistry. 20:2162-2168. 2009 Detection of intracellular granularity induction in prostate cancer cell lines by small molecules using the HyperCyt high-throughput flow cytometry system.. Journal of biomolecular screening. 14:596-609. 2009 Detection of intracellular granularity induction in prostate cancer cell lines by small molecules using the HyperCyt high-throughput flow cytometry system.. Journal of biomolecular screening. 14:596-609. 2009 Detection of intracellular granularity induction in prostate cancer cell lines by small molecules using the HyperCyt high-throughput flow cytometry system.. Journal of biomolecular screening. 14:596-609. 2009 Detection of intracellular granularity induction in prostate cancer cell lines by small molecules using the HyperCyt high-throughput flow cytometry system.. Journal of biomolecular screening. 14:596-609. 2009 A novel fluorescent cross-reactive formylpeptide receptor/formylpeptide receptor-like 1 hexapeptide ligand.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 75:264-270. 2009 A crowdsourcing evaluation of the NIH chemical probes.. Nature chemical biology. 5:441-447. 2009 Chapter 11. Subsecond analyses of G-protein coupled-receptor ternary complex dynamics by rapid mix flow cytometry.. Methods in enzymology. 461:227-247. 2009 Conformational mAb as a tool for integrin ligand discovery.. Assay and drug development technologies. 7:507-515. 2009 Discovery of selective probes and antagonists for G-protein-coupled receptors FPR/FPRL1 and GPR30.. Current topics in medicinal chemistry. 9:1227-1236. 2009 Duplex high-throughput flow cytometry screen identifies two novel formylpeptide receptor family probes.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 75:253-263. 2009 High-content screening: flow cytometry analysis.. Methods in molecular biology (Clifton, N.J.). 486:151-165. 2009 In vivo effects of a GPR30 antagonist.. Nature chemical biology. 5:421-427. 2009 Real-time analysis of conformation-sensitive antibody binding provides new insights into integrin conformational regulation.. The Journal of biological chemistry. 284:14337-14346. 2009 A multifunctional androgen receptor screening assay using the high-throughput Hypercyt flow cytometry system.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 73:390-399. 2008 Estrogen signaling through the transmembrane G protein-coupled receptor GPR30.. Annual review of physiology. 70:165-190. 2008 Flow cytometry for real-time measurement of guanine nucleotide binding and exchange by Ras-like GTPases.. Analytical biochemistry. 381:258-266. 2008 GPR30: a novel therapeutic target in estrogen-related disease.. Trends in pharmacological sciences. 29:116-123. 2008 High-throughput screening for daunorubicin-mediated drug resistance identifies mometasone furoate as a novel ABCB1-reversal agent.. Journal of biomolecular screening. 13:185-193. 2008 Preclinical development of a neutral, estrogen receptor-targeted, tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative for imaging of breast and endometrial cancers.. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 49:978-986. 2008 The ins and outs of GPR30: a transmembrane estrogen receptor.. The Journal of steroid biochemistry and molecular biology. 109:350-353. 2008 Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.. ACS chemical biology. 2:536-544. 2007 High-throughput flow cytometry for drug discovery.. Expert opinion on drug discovery. 2:685-696. 2007 GPR30: A G protein-coupled receptor for estrogen.. Molecular and cellular endocrinology. 265-266:138-142. 2007 Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system.. The Journal of endocrinology. 193:311-321. 2007 Rapid-mix flow cytometry measurements of subsecond regulation of G protein-coupled receptor ternary complex dynamics by guanine nucleotides.. Analytical biochemistry. 371:10-20. 2007 Some mechanistic insights into GPCR activation from detergent-solubilized ternary complexes on beads.. Advances in protein chemistry. 74:95-135. 2007 Spectroscopic characterization of streptavidin functionalized quantum dots.. Analytical biochemistry. 364:193-203. 2007 The development of quantum dot calibration beads and quantitative multicolor bioassays in flow cytometry and microscopy.. Analytical biochemistry. 364:180-192. 2007 Linkage effects on binding affinity and activation of GPR30 and estrogen receptors ERalpha/beta with tridentate pyridin-2-yl hydrazine tricarbonyl-Re/(99m)Tc(I) chelates.. Journal of the American Chemical Society. 128:14476-14477. 2006 Steroid-binding G-protein-coupled receptors: new drug discovery targets for old ligands.. Expert opinion on drug discovery. 1:137-150. 2006 Screening for caspase-3 inhibitors: a new class of potent small-molecule inhibitors of caspase-3.. Journal of biomolecular screening. 11:277-285. 2006 Biomolecular screening of formylpeptide receptor ligands with a sensitive, quantitative, high-throughput flow cytometry platform.. Nature protocols. 1:59-66. 2006 Glutathione-S-transferase-green fluorescent protein fusion protein reveals slow dissociation from high site density beads and measures free GSH.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 69:326-334. 2006 Modulation of GPCR conformations by ligands, G-proteins, and arrestins.. Ernst Schering Foundation symposium proceedings. :211-228. 2006 Virtual and biomolecular screening converge on a selective agonist for GPR30.. Nature chemical biology. 2:207-212. 2006 A transmembrane intracellular estrogen receptor mediates rapid cell signaling.. Science (New York, N.Y.). 307:1625-1630. 2005 Inhibition of chemoattractant N-formyl peptide receptor trafficking by active arrestins.. Traffic (Copenhagen, Denmark). 6:87-99. 2005 ATP hydrolysis-dependent disassembly of the 26S proteasome is part of the catalytic cycle.. Cell. 121:553-565. 2005 Dissociation of I domain and global conformational changes in LFA-1: refinement of small molecule-I domain structure-activity relationships.. Biochemistry. 44:4322-4331. 2005 Dynamics of fluorescence dequenching of ostrich-quenched fluorescein biotin: a multifunctional quantitative assay for biotin.. Analytical biochemistry. 342:221-228. 2005 High-throughput screening with HyperCyt flow cytometry to detect small molecule formylpeptide receptor ligands.. Journal of biomolecular screening. 10:374-382. 2005 Integration of virtual screening with high-throughput flow cytometry to identify novel small molecule formylpeptide receptor antagonists.. Molecular pharmacology. 68:1301-1310. 2005 Post-high-throughput screening analysis: an empirical compound prioritization scheme.. Journal of biomolecular screening. 10:419-426. 2005 Small-volume rapid-mix device for subsecond kinetic analysis in flow cytometry.. Cytometry. Part A : the journal of the International Society for Analytical Cytology. 67:37-44. 2005 Techniques: GPCR assembly, pharmacology and screening by flow cytometry.. Trends in pharmacological sciences. 25:663-669. 2004 Real-time analysis of ternary complex on particles: direct evidence for partial agonism at the agonist-receptor-G protein complex assembly step of signal transduction. 2004 High-throughput microfluidic mixing and multiparametric cell sorting for bioactive compound screening.. Journal of biomolecular screening. 9:103-111. 2004 An investigation of liquid carryover and sample residual for a high-throughput flow cytometer sample delivery system.. Analytical chemistry. 76:3810-3817. 2004 Conformational regulation of alpha 4 beta 1-integrin affinity by reducing agents. "Inside-out" signaling is independent of and additive to reduction-regulated integrin activation.. The Journal of biological chemistry. 279:32435-32443. 2004 Flow cytometry for high-throughput, high-content screening.. Current opinion in chemical biology. 8:392-398. 2004 Near-simultaneous and real-time detection of multiple analytes in affinity microcolumns.. Analytical chemistry. 76:6266-6273. 2004 Alpha4beta1 integrin affinity changes govern cell adhesion. 2003 Functional capabilities of an N-formyl peptide receptor-G(alpha)(i)(2) fusion protein: assemblies with G proteins and arrestins.. Biochemistry. 42:7283-7293. 2003 High throughput screening of G-protein coupled receptors via flow cytometry.. Combinatorial chemistry & high throughput screening. 6:389-397. 2003 N-formyl peptide receptor phosphorylation domains differentially regulate arrestin and agonist affinity. 2003 FRET detection of cellular alpha4-integrin conformational activation.. Biophysical journal. 85:3951-3962. 2003 Ligand-receptor-G-protein molecular assemblies on beads for mechanistic studies and screening by flow cytometry.. Molecular pharmacology. 64:1227-1238. 2003 Release of ubiquitin-charged Cdc34-S - Ub from the RING domain is essential for ubiquitination of the SCF(Cdc4)-bound substrate Sic1.. Cell. 114:611-622. 2003 Performance of in-line microfluidic mixers in laminar flow for high-throughput flow cytometry.. BioTechniques. 33:220-226. 2002 Arrestin variants display differential binding characteristics for the phosphorylated N-formyl peptide receptor carboxyl terminus. 2002 Biomolecular recognition on well-characterized beads packed in microfluidic channels.. Analytical chemistry. 74:1149-1156. 2002 Flow cytometric analysis of ligand-receptor interactions and molecular assemblies.. Annual review of biophysics and biomolecular structure. 31:97-119. 2002 Partial phosphorylation of the N-formyl peptide receptor inhibits G protein association independent of arrestin binding.. The Journal of biological chemistry. 276:49195-49203. 2001 Real time analysis of the affinity regulation of alpha 4-integrin. The physiologically activated receptor is intermediate in affinity between resting and Mn(2+) or antibody activation.. The Journal of biological chemistry. 276:48670-48678. 2001 Regulation of formyl peptide receptor agonist affinity by reconstitution with arrestins and heterotrimeric G proteins.. The Journal of biological chemistry. 276:49204-49212. 2001 Real-time analysis of G protein-coupled receptor reconstitution in a solubilized system.. The Journal of biological chemistry. 276:22453-22460. 2001 HTPS flow cytometry: a novel platform for automated high throughput drug discovery and characterization.. Journal of biomolecular screening. 6:83-90. 2001 Plug flow cytometry extends analytical capabilities in cell adhesion and receptor pharmacology.. Cytometry. 43:211-216. 2001 High throughput flow cytometry.. Cytometry. 44:83-90. 2001 Analysis of free intracellular calcium by flow cytometry: multiparameter and pharmacologic applications.. Methods (San Diego, Calif.). 21:221-230. 2000 Solubilization and display of G protein-coupled receptors on beads for real-time fluorescence and flow cytometric analysis.. BioTechniques. 28:976-80, 982-5. 2000 Expression of P-selectin at low site density promotes selective attachment of eosinophils over neutrophils.. Journal of immunology (Baltimore, Md. : 1950). 165:404-410. 2000 The uncoupled state of the human formyl peptide receptor.. Journal of receptor and signal transduction research. 19:327-340. 1999 Multiple activation steps of the N-formyl peptide receptor.. Biochemistry. 38:2240-2247. 1999 Plug flow cytometry: An automated coupling device for rapid sequential flow cytometric sample analysis.. Cytometry. 37:156-159. 1999 Strategies for positioning fluorescent probes and crosslinkers on formyl peptide ligands.. Journal of receptor and signal transduction research. 18:187-221. 1998 Thymic overexpression of Ttg-1 in transgenic mice results in T-cell acute lymphoblastic leukemia/lymphoma.. Molecular and cellular biology. 12:4186-4196. 1992 Diazo coupling method for covalent attachment of proteins to solid substrates.. Bioconjugate chemistry. 17:359-365. article A Potent and Selective Inhibitor of Cdc42 GTPase 2010 Three small molecule pan activator families of Ras-related GTPases 2010 Autophagy, Inflammation, and Metabolism (AIM) Center of Biomedical Research Excellence: supporting the next generation of autophagy researchers and fostering international collaborations.. Autophagy. 925-929. 2018 Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.. 1252-1265. 2015 Flow Cytometry: Impact on Early Drug Discovery.. Journal of biomolecular screening. -. 2015
education and training Ph.D. in Chemistry, Stanford University Ph.D. in Chemistry, Stanford University 1972 - 1976 The Methodist Hospital , Department of Medicine 1977 - 1979 University of California, Santa Cruz , Division of Natural Sciences 1976 - 1977