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プロフィール詳細
Dr. Peter B.に依頼
United States
Accomplished research scientist with extensive experience in early discovery research, lead optimization, and outsurcin
プロフィール概要
専門分野
サービス
Consulting
Scientific and Technical Consulting
職務経験
Project Manager
UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill
6月 2022 - 現在 
Principal Investigator
SGC, University of Toronto
5月 2009 - 6月 2022
Section Head medicinal Chemistry
GlaxoSmithKline
5月 1989 - 8月 2008
学歴
Ph.D., Chemistry
University of Sheffield
9月 1979 - 8月 1982
認定資格
-
Honored List
Marquis Who's Who
https://badges.marquiswhoswho.com/Badge/honoredlistee/aca8a85277814eb08fd604f4265523b2b0a9a06a7ba147b380da2018a39a82091月 2024 - 現在
出版物
PREPRINT
Muthu Ramalingam Bose, John D. Sears, Kacey M. Talbot, Yuan-Wei Norman Su, Scott Houliston, Mohammed Anwar Hossain, Zachary W. Davis-Gilbert, Chunqing Zhao, Hans J. Oh, Peter J. Brown, et al. (2025). Identification of Direct-acting nsP2 Helicase Inhibitors with Antialphaviral Activity .
Beatrice Chiew, Menachem J. Gunzburg, Caroline A. Foley, Hong Zeng, Aiping Dong, Peter J. Brown, Juliana The, Jacqueline L. Noris, Stephanie H. Cholensky, Biswaranjan Mohanty, et al. (2024). Exploring the Ligandability of 53BP1 Through Fragment-Based Approaches .
Anirban Ghoshal, Kesatebrhan Haile Asressu, Mohammad Anwar Hossain, Peter J. Brown, Eric M. Merten, John D. Sears, Sumera Perveen, Kenneth H. Pearce, Konstantin I. Popov, Nathaniel J. Moorman, et al. (2024). Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors ofChikungunyansP2 Cysteine Protease with Anti-alphavirus Activity .
JOURNAL ARTICLE
Eric M. Merten, John D. Sears, Tina M. Leisner, P. Brian Hardy, Anirban Ghoshal, Mohammad Anwar Hossain, Kesatebrhan Haile Asressu, Peter J. Brown, Edwin G. Tse, Michael A. Stashko, et al. (2024). Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach . Proceedings of the National Academy of Sciences.
Serah W. Kimani, Julie Owen, Stuart R. Green, Fengling Li, Yanjun Li, Aiping Dong, Peter J. Brown, Suzanne Ackloo, David Kuter, Cindy Yang, et al. (2023). Discovery of a Novel DCAF1 Ligand Using a Drug–Target Interaction Prediction Model: Generalizing Machine Learning to New Drug Targets . Journal of Chemical Information and Modeling.
Suzanne Ackloo, Albert A. Antolin, Jose Manuel Bartolome, Hartmut Beck, Alex Bullock, Ulrich A. K. Betz, Jark Böttcher, Peter J. Brown, Menorca Chaturvedi, Alisa Crisp, et al. (2023). Target 2035 – an update on private sector contributions . RSC Medicinal Chemistry.
(2021). A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6 . Journal of medicinal chemistry.
(2021). Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2 . Journal of medicinal chemistry.
(2021). Identification of small molecule allosteric modulators of 5,10-methylenetetrahydrofolate reductase (MTHFR) by targeting its unique regulatory domain . Biochimie.
(2020). Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response . Nature communications.
(2019). Discovery of a chemical probe for PRDM9 . Nature communications.
(2019). A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion . eLife.
(2019). Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase . Journal of medicinal chemistry.
(2019). Identification and characterization of the first fragment hits for SETDB1 Tudor domain . Bioorganic & medicinal chemistry.
(2019). Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3 . Nature chemical biology.
(2019). Structural and functional consequences of the STAT5BN642H driver mutation . Nature communications.
Junghyun L. Suh, Kimberly D. Barnash, Tigran M. Abramyan, Fengling Li, Juliana The, Isabelle A. Engelberg, Masoud Vedadi, Peter J. Brown, Dmitri B. Kireev, Cheryl H. Arrowsmith, et al. (2019). Discovery of selective activators of PRC2 mutant EED-I363M . Scientific Reports.
(2019). AKT drives SOX2 overexpression and cancer cell stemness in esophageal cancer by protecting SOX2 from UBR5-mediated degradation . Oncogene.
(2019). A chemical biology toolbox to study protein methyltransferases and epigenetic signaling . Nature communications.
(2018). A DNA-Encoded Library of Chemical Compounds Based on Common Scaffolding Structures Reveals the Impact of Ligand Geometry on Protein Recognition . ChemMedChem.
(2018). LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity . ACS medicinal chemistry letters.
(2018). Donated chemical probes for open science . eLife.
(2018). TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma . Oncotarget.
(2018). Discovery of Small-Molecule Antagonists of the H3K9me3 Binding to UHRF1 Tandem Tudor Domain . SLAS discovery : advancing life sciences R & D.
Kaniskan HÜ, Eram MS, Zhao K, Szewczyk MM, Yang X, Schmidt K, Luo X, Xiao S, Dai M, He F, et al.(2018). Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3) . Journal of medicinal chemistry.
(2018). Revealing the protein propionylation activity of the histone acetyltransferase MOF (males absent on the first) . The Journal of biological chemistry.
Han Z, Wu H, Kim S, Yang X, Li Q, Huang H, Cai H, Bartlett MG, Dong A, Zeng H, et al.(2018). Revealing the Protein Propionylation Activity of the Histone Acetyltransferase Males absent on the first (MOF) . The Journal of biological chemistry.
Houliston RS, Lemak A, Iqbal A, Ivanochko D, Duan S, Kaustov L, Ong MS, Fan L, Senisterra G, Brown PJ, et al.(2017). Conformational dynamics of the TTD-PHD histone reader module of the UHRF1 epigenetic regulator reveals multiple histone-binding states, allosteric regulation, and druggability . The Journal of biological chemistry.
Dahlin JL, Nelson KM, Strasser JM, Barsyte-Lovejoy D, Szewczyk MM, Organ S, Cuellar M, Singh G, Shrimp JH, Nguyen N, et al.(2017). Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors . Nature communications.
Xiong Y, Li F, Babault N, Wu H, Dong A, Zeng H, Chen X, Arrowsmith CH, Brown PJ, Liu J, et al.(2017). Structure-activity relationship studies of G9a-like protein (GLP) inhibitors . Bioorganic & medicinal chemistry.
Ackloo S, Brown PJ, Müller S(2017). Chemical probes targeting epigenetic proteins: Applications beyond oncology . Epigenetics.
Barnash KD, The J, Norris-Drouin JL, Cholensky SH, Worley BM, Li F, Stuckey JI, Brown PJ, Vedadi M, Arrowsmith CH, et al.(2017). Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2 . ACS combinatorial science.
Xiong Y, Li F, Babault N, Dong A, Zeng H, Wu H, Chen X, Arrowsmith CH, Brown PJ, Liu J, et al.(2017). Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase . Journal of medicinal chemistry.
Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, et al.(2017). The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity . Nature chemical biology.
Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, et al.(2016). Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8 . ACS medicinal chemistry letters.
Kaniskan HÜ, Eram MS, Liu J, Smil D, Martini ML, Shen Y, Santhakumar V, Brown PJ, Arrowsmith C, Vedadi M, et al.(2016). Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1) . MedChemComm.
Sun Y, Bell JL, Carter D, Gherardi S, Poulos RC, Milazzo G, Wong JW, Al-Awar R, Tee AE, Liu PY, et al.(2015). WDR5 Supports an N-Myc Transcriptional Complex That Drives a Protumorigenic Gene Expression Signature in Neuroblastoma . Cancer research.
Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, et al.(2015). Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia . Nature chemical biology.
(2013). Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction . ACS Medicinal Chemistry Letters.
Müller S, Brown PJ, Clinical pharmacology and therapeutics, 2012, vol. 92, no. 6, pp. 689-693, 2012 .
(2012). Structure–activity relationships of methyl-lysine reader antagonists . Med. Chem. Commun.
Wigle TJ, Provencher LM, Norris JL, Jin J, Brown PJ, Frye SV, Janzen WP(2010). Accessing protein methyltransferase and demethylase enzymology using microfluidic capillary electrophoresis . Chemistry & biology.
(2007). Design and synthesis of an array of selective androgen receptor modulators . Journal of combinatorial chemistry.
(2004). Selection, application, and validation of a set of molecular descriptors for nuclear receptor ligands . Combinatorial chemistry & high throughput screening.
(2003). Evaluation of the therapeutic potential of PPARalpha agonists for X-linked adrenoleukodystrophy . Molecular genetics and metabolism.
(2003). Evaluation of the therapeutic potential of PPARalpha agonists for X-linked adrenoleukodystrophy . Molecular genetics and metabolism.
(2003). Activation of peroxisome proliferator-activated receptor-alpha protects the heart from ischemia/reperfusion injury . Circulation.
(2001). Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis . Bioorganic & medicinal chemistry letters.
(2001). Effects of fenofibrate on lipid parameters in obese rhesus monkeys . Journal of lipid research.
(2001). The characterization of PPAR alpha ligand drug action in an in vivo model by comprehensive differential gene expression profiling . Functional & integrative genomics.
(2001). Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis . Bioorganic & medicinal chemistry letters.
(2001). A CONVENIENT SYNTHESIS OF THIOFIBRATE ANALOGS FROM ARYL SULFONYL CHLORIDES . Synthetic Communications.
(2000). The PPARs: from orphan receptors to drug discovery . Journal of medicinal chemistry.
(1999). A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity . Journal of medicinal chemistry.
(1999). Molecular recognition of fatty acids by peroxisome proliferator-activated receptors . Molecular cell.
(1998). Discovery of bioavailable inhibitors of secretory phospholipase A2 . Pharmaceutical biotechnology.
(1997). Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library . Chemistry & biology.
(1997). Generation of Secondary Alkyl Amines on Solid Support by Borane Reduction: Application to the Parallel Synthesis of PPAR Ligands . Synthesis.
(1997). Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma . Proceedings of the National Academy of Sciences of the United States of America.
Kliewer SA, Sundseth SS, Jones SA, Brown PJ, Wisely GB, Koble CS, Devchand P, Wahli W, Willson TM, Lenhard JM, et al.(1997). Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma . Proceedings of the National Academy of Sciences of the United States of America.
(1994). Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand: modification of the P1 and P2' residues . Journal of medicinal chemistry.
(1993). Isotope effects and alternative substrate reactivities for tryptophan 2,3-dioxygenase. The Journal of biological chemistry.
(1993). A high throughput fluorogenic substrate for interstitial collagenase (MMP-1) and gelatinase (MMP-9) . Analytical biochemistry.
(1992). HMG-CoA reductase inhibitors 4. Tetrazole series: conformational constraints and structural requirements at the hydrophobic domain . Bioorganic & Medicinal Chemistry Letters.
(1990). Synthesis, biological profile, and quantitative structure-activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors . Journal of medicinal chemistry.
(1989). A potent, tissue-selective, synthetic inhibitor of HMG-CoA reductase . Journal of medicinal chemistry.
(1985). Total Synthesis of (-)-Kopsinilam, (-)-Kopsinine, and the Bis-indole Alkaloids (-)-Norpleiomutine and (-)-Pleiomutine . Journal of the Chemical Society, Chemical Communications.
(1984). Synthesis of (.+-.)-10,22-dioxokopsane and (.+-.)-kopsanone, heptacyclic indole alkaloids. Synthetic and mechanistic studies . Journal of the American Chemical Society.
(1984). The indole 2-3-quinodimethane strategy for the synthesis of indole alkaloids . Accounts of Chemical Research.
(1983). Alkenyl sulphoxides as precursors to cyclopentenones and prostanoid β-side chains . Tetrahedron Letters.
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