Jason Witherington

Jason Witherington

Greater London, England, United Kingdom
2K followers 500+ connections

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About

I have over 25 years as a senior leader within the Life Science sector and I have a…

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Experience

Education

  • University of Pennsylvania Graphic

    University of Pennsylvania

    -

    Post-doctoral studies under the guidance of Professors Amos B. Smith III, Ralph Hirschmann and Stephen Benkovic

Publications

  • Human-​relevant near-​organ neuromodulation of the immune system via the splenic nerve

    Proceedings of the National Academy of Sciences of the United States of America

  • Quantification of clinically applicable stimulation parameters for precision near-​organ neuromodulation of human splenic nerves

    Communications biology

  • Effect of Superior Ovarian Nerve and Plexus Nerve Sympathetic Denervation on Ovarian-​Derived Infertility Provoked by Estradiol Exposure to Rats

    Frontiers in physiology

  • Structure-​based design of an N-​terminal bromodomain selective bromodomain and extraterminal (BET) inhibitor retaining an antiproliferative phenotype

    Abstracts of Papers, 258th ACS National Meeting & Exposition, San Diego, CA, United States, August 25-29, 2019

  • BET bromodomain inhibitors show anti-​papillomavirus activity in vitro and block CRPV wart growth in vivo

    Antiviral Research

  • Neuronal control of experimental colitis occurs via sympathetic intestinal innervation

    Neurogastroenterology & Motility

  • Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-​Phosphate Receptor 3 (S1P3)​-​Sparing S1P1 Agonists Active at Low Oral Doses

    Journal of Medicinal Chemistry

  • avigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists

    Journal of Medicinal Chemistry

  • avigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists

    Journal of Medicinal Chemistry

  • BET Inhibition As A Potential Therapy For Human Papillomavirus Infection

    Antimicrobial Agents and Chemotherapy

  • Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

    J. Med. Chem

  • Inhibition of Osteoclastogenesis and Inflammatory Bone Resorption by Targeting BET proteins and Epigenetic Regulation

    Nature Medicine.

  • Naphthyridines as Novel BET Family Bromodomain Inhibitors

    ChemMedChem

  • Optimization of S1P1 receptor agonists: effects of acidic, basic and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles

    J. Med. Chem

  • The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

    MedChemComm

  • Potent antimyeloma activity of the novel bromodomain inhibitors I-​BET151 and I-​BET762

    Blood

  • Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists

    Bioorg. Med. Chem. Lett

  • Selective inhibition of CD4+ T-cell cytokine production and autoimmunity BET protein and c-Myc inhibitors

    PNAS

  • The discovery of the benzazepine class of histamine H3 receptor antagonists

    Bioorg. Med. Chem. Lett

  • Application of chemoproteomics for the discovery of a new druggable epigenetic target class and potential therapeutic utility

    Abstracts of Papers, 244th ACS

  • Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151(GSK1210151A)

    Bioorg. Med. Chem. Lett

  • Place your BETs: the therapeutic potential of bromodomains

    Trends in Pharmacological Sciences

  • The utility of pharmacokinetic-pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists

    Xenobiotica

  • − Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose

    J. Med. Chem

  • Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate

    ACS Med. Chem. Lett

  • Progress in the discovery of small-molecule inhibitors of bromodomain-histone interactions

    J. Biomol. Screening

  • Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor

    Bioorg. Med. Chem. Lett

  • Functional and in situ hybridization evidence that preganglionic sympathetic vasoconstrictor neurons express ghrelin receptors

    Neuroscience

  • Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain

    Bioorg. Med. Chem. Lett

  • 5-hydroxyindalpine, an agonist at the putative 5-HT1P receptor, has no activity on human recombinant monoamine receptors but accelerates distension-induced peristalsis in mouse isolated colon

    Neurogastroenterology & Motility

  • Cognitive enhancing effects of ghrelin receptor agonists

    Psychopharmacology

  • Oral administration of a centrally acting ghrelin receptor agonist to conscious rats triggers defecation

    Neurogastroenterology & Motility

  • Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimization

    Bioorg. Med. Chem. Lett

  • GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models

    J. Pharm. & Exp. Ther

  • Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification

    Bioorg. Med. Chem. Lett

  • Therapeutic approaches towards the treatment of gastrointestinal disorders

    Drug News & Perspectives

  • 3-Amino pyrazoles as potent and selective glycogen kinase synthase 3 (GSK-3) inhibitors

    Glycogen Synthase Kinase 3 (GSK-3) and Its Inhibitors, Wiley

  • A new asymmetric synthesis of (+)-12b-epidevinylantirhine

    Tet. Lett

  • Anti-emetic activity of ghrelin in ferrets exposed to the cytotoxic anti-cancer agent cisplatin

    Neuroscience Lett

  • Complementary stereoselective conjugate addition reactions on indolo[2,3-a]quinolizine templates

    Tet. Lett

  • Evidence that stimulation of ghrelin receptors in the spinal cord initiates propulsive activity in the colon of the rat

    J. Physiology

  • Organolithium-Induced Alkylative Ring Opening of Aziridines: Synthesis of Unsaturated Amino Alcohols and Ethers

    J. Org. Chem

  • Pyridone derivatives as potent and selective VLA-4 integrin antagonists

    Bioorg. Med. Chem. Lett

  • Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists

    Bioorg. Med. Chem. Lett

  • Recent disclosures of clinical drug candidates

    Drug news & perspectives

  • − (1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors

    Bioorg. Med. Chem. Lett

  • Challenges facing drug discovery in vascular disease

    Drug news & perspectives

  • Organolithium-induced enantioselective alkylative double ring-opening of epoxides: synthesis of enantioenriched unsaturated amino alcohols

    Tetrahedron.

  • Unsaturated 1,2-amino alcohols and ethers aziridines and organolithiums

    Chem. Comm

  • 5-Aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)

    Bioorg. Med. Chem. Lett.

  • 5-Aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)

    Bioorg. Med. Chem. Lett.

  • 6-Aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)

    Bioorg. Med. Chem. Lett.

  • 6-Heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)

    Bioorg. Med. Chem. Lett

  • CCR2: Characterization of the Antagonist Binding Site a Combined Receptor Modeling/Mutagenesis Approach

    J. Med. Chem.

  • Enantioselective alkylative double ring opening of epoxides: Synthesis of enantioenriched unsaturated diols and amino alcohols

    Angewandte Chemie, International Edition

  • Unsaturated 1,2-amino alcohols dihydropyrrole epoxides and organolithiums

    Synlett

  • Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

    Bioorg. Med. Chem. Lett.

  • Cyclic Ketone Inhibitors of the Cysteine Protease Cathepsin K

    J. Med. Chem.

  • Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K

    Bioorg. Med. Chem. Lett

  • Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K

    Bioorg. Med. Chem. Lett.

  • Orally bioavailable inhibitors of the cysteine protease cathepsin K

    218th ACS National Meeting

  • Isomerizations of cycloalkene- and bicycloalkene-derived achiral epoxides enantioselective deprotonation

    Journal of the Chemical Society, Perkin Transactions 1: Org. & Bioorg. Chem

  • Investigations of an Antibody Ligase

    J. Am. Chem. Soc

  • Phosphonate Diester and Phosphonamide Synthesis. Reaction Coordinate Analysis 31P NMR Spectroscopy: Identification of Pyrophosphonate Anhydrides and Highly Reactive Phosphonylammonium Salts

    J. Am. Chem. Soc

  • Pd/Cu Co-catalyzed cross-coupling reactions of methyl (Z)-2-tributylstannyl-3-methoxypropenoate: a method for direct introduction of the agrochemically important beta-methoxyacrylate toxophore

    Synlett

  • Phosphonyltriethylammonium Salts: Novel Reactive Species for the Synthesis of Phosphonate Esters and Phosphonamides

    J. Am. Chem. Soc.

  • Concise racemic and highly enantioselective approaches to key intermediates for the syntheses of carbocyclic nucleosides and pseudo-ribofuranoses: formal syntheses of carbovir

    J. Chem. Soc., Perkin Transactions 1: Org. and Bio-Org. Chem

  • Regio- and stereospecific synthesis of cis-(±)-1-acetoxy-4-(acetoxymethyl)cyclopent-2-ene: a key intermediate in the synthesis of carbocyclic nucleosides and pseudo-ribofuranoses

    Org. and Bio-Org. Chem

  • Human-​relevant near-​organ neuromodulation of the immune system via the splenic nerve

    Proceedings of the National Academy of Sciences of the United States of America

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