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A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin.

Lee JB, Radhi M, Cipolla E, Gandhi RD, Sarmad S, Zgair A, Kim TH, Feng W, Qin C, Adrower C, Ortori CA, Barrett DA, Kagan L, Fischer PM, de Moor CH, Gershkovich P.

Sci Rep. 2019 Oct 31;9(1):15760. doi: 10.1038/s41598-019-52254-x.


Crystal structures of the recombinant β-factor XIIa protease with bound Thr-Arg and Pro-Arg substrate mimetics.

Pathak M, Manna R, Li C, Kaira BG, Hamad BK, Belviso BD, Bonturi CR, Dreveny I, Fischer PM, Dekker LV, Oliva MLV, Emsley J.

Acta Crystallogr D Struct Biol. 2019 Jun 1;75(Pt 6):578-591. doi: 10.1107/S2059798319006910. Epub 2019 Jun 4.


1-Hydroxy-xanthine derivatives inhibit the human Caf1 nuclease and Caf1-containing nuclease complexes via Mg2+-dependent binding.

Airhihen B, Pavanello L, Jadhav GP, Fischer PM, Winkler GS.

FEBS Open Bio. 2019 Mar 7;9(4):717-727. doi: 10.1002/2211-5463.12605. eCollection 2019 Apr.


The Meisenheimer Complex as a Paradigm in Drug Discovery: Reversible Covalent Inhibition through C67 of the ATP Binding Site of PLK1.

Pearson RJ, Blake DG, Mezna M, Fischer PM, Westwood NJ, McInnes C.

Cell Chem Biol. 2018 Sep 20;25(9):1107-1116.e4. doi: 10.1016/j.chembiol.2018.06.001. Epub 2018 Jul 12.


Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system.

Lee JB, Zgair A, Malec J, Kim TH, Kim MG, Ali J, Qin C, Feng W, Chiang M, Gao X, Voronin G, Garces AE, Lau CL, Chan TH, Hume A, McIntosh TM, Soukarieh F, Al-Hayali M, Cipolla E, Collins HM, Heery DM, Shin BS, Yoo SD, Kagan L, Stocks MJ, Bradshaw TD, Fischer PM, Gershkovich P.

J Control Release. 2018 Sep 28;286:10-19. doi: 10.1016/j.jconrel.2018.07.022. Epub 2018 Jul 18.


Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B.

Zyryanova AF, Weis F, Faille A, Alard AA, Crespillo-Casado A, Sekine Y, Harding HP, Allen F, Parts L, Fromont C, Fischer PM, Warren AJ, Ron D.

Science. 2018 Mar 30;359(6383):1533-1536. doi: 10.1126/science.aar5129.


Multiple Linear Regression Modeling To Predict the Stability of Polymer-Drug Solid Dispersions: Comparison of the Effects of Polymers and Manufacturing Methods on Solid Dispersion Stability.

Fridgeirsdottir GA, Harris RJ, Dryden IL, Fischer PM, Roberts CJ.

Mol Pharm. 2018 May 7;15(5):1826-1841. doi: 10.1021/acs.molpharmaceut.8b00021. Epub 2018 Mar 29.


Oral administration of cannabis with lipids leads to high levels of cannabinoids in the intestinal lymphatic system and prominent immunomodulation.

Zgair A, Lee JB, Wong JCM, Taha DA, Aram J, Di Virgilio D, McArthur JW, Cheng YK, Hennig IM, Barrett DA, Fischer PM, Constantinescu CS, Gershkovich P.

Sci Rep. 2017 Nov 6;7(1):14542. doi: 10.1038/s41598-017-15026-z.


Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.

Fischer PM.

J Med Chem. 2018 May 10;61(9):3799-3822. doi: 10.1021/acs.jmedchem.7b00772. Epub 2017 Nov 9. Review.


Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.

Whittaker SR, Barlow C, Martin MP, Mancusi C, Wagner S, Self A, Barrie E, Te Poele R, Sharp S, Brown N, Wilson S, Jackson W, Fischer PM, Clarke PA, Walton MI, McDonald E, Blagg J, Noble M, Garrett MD, Workman P.

Mol Oncol. 2018 Mar;12(3):287-304. doi: 10.1002/1878-0261.12148. Epub 2018 Jan 28.


Assessment of the protein interaction between coagulation factor XII and corn trypsin inhibitor by molecular docking and biochemical validation.

Hamad BK, Pathak M, Manna R, Fischer PM, Emsley J, Dekker LV.

J Thromb Haemost. 2017 Sep;15(9):1818-1828. doi: 10.1111/jth.13773. Epub 2017 Aug 9.


Development of Cordycepin Formulations for Preclinical and Clinical Studies.

Lee JB, Adrower C, Qin C, Fischer PM, de Moor CH, Gershkovich P.

AAPS PharmSciTech. 2017 Nov;18(8):3219-3226. doi: 10.1208/s12249-017-0795-0. Epub 2017 May 30.


PPP1R15A-mediated dephosphorylation of eIF2α is unaffected by Sephin1 or Guanabenz.

Crespillo-Casado A, Chambers JE, Fischer PM, Marciniak SJ, Ron D.

Elife. 2017 Apr 27;6. pii: e26109. doi: 10.7554/eLife.26109.


Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease.

Baker JG, Gardiner SM, Woolard J, Fromont C, Jadhav GP, Mistry SN, Thompson KSJ, Kellam B, Hill SJ, Fischer PM.

FASEB J. 2017 Jul;31(7):3150-3166. doi: 10.1096/fj.201601305R. Epub 2017 Apr 11.


Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays.

Lee JB, Zgair A, Taha DA, Zang X, Kagan L, Kim TH, Kim MG, Yun HY, Fischer PM, Gershkovich P.

Eur J Pharm Biopharm. 2017 May;114:38-42. doi: 10.1016/j.ejpb.2016.12.027. Epub 2017 Jan 12.


Simple and sensitive HPLC-UV method for determination of bexarotene in rat plasma.

Lee JB, Zgair A, Kim TH, Kim MG, Yoo SD, Fischer PM, Gershkovich P.

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Jan 1;1040:73-80. doi: 10.1016/j.jchromb.2016.11.024. Epub 2016 Nov 17.


Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview.

Fischer PM.

Med Res Rev. 2017 Mar;37(2):314-367. doi: 10.1002/med.21409. Epub 2016 Oct 24. Review.


Erratum to "Survival of the Fittest: Time-To-Event Modelling of Crystallisation of Amorphous Poorly Soluble Drugs".

Nurzyńska K, Austin RP, Fischer PM, Booth J, Gommer F.

J Pharm Sci. 2016 Nov;105(11):3464. doi: 10.1016/j.xphs.2016.09.012. No abstract available.


Dietary fats and pharmaceutical lipid excipients increase systemic exposure to orally administered cannabis and cannabis-based medicines.

Zgair A, Wong JC, Lee JB, Mistry J, Sivak O, Wasan KM, Hennig IM, Barrett DA, Constantinescu CS, Fischer PM, Gershkovich P.

Am J Transl Res. 2016 Aug 15;8(8):3448-59. eCollection 2016.


Design of nucleotide-mimetic and non-nucleotide inhibitors of the translation initiation factor eIF4E: Synthesis, structural and functional characterisation.

Soukarieh F, Nowicki MW, Bastide A, Pöyry T, Jones C, Dudek K, Patwardhan G, Meullenet F, Oldham NJ, Walkinshaw MD, Willis AE, Fischer PM.

Eur J Med Chem. 2016 Nov 29;124:200-217. doi: 10.1016/j.ejmech.2016.08.047. Epub 2016 Aug 24.


GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors.

Emtage AL, Mistry SN, Fischer PM, Kellam B, Laughton CA.

J Biomol Struct Dyn. 2017 Sep;35(12):2604-2619. doi: 10.1080/07391102.2016.1226197. Epub 2016 Sep 1.


Support Tools in Formulation Development for Poorly Soluble Drugs.

Fridgeirsdottir GA, Harris R, Fischer PM, Roberts CJ.

J Pharm Sci. 2016 Aug;105(8):2260-9. doi: 10.1016/j.xphs.2016.05.024. Epub 2016 Jun 29. Review.


Survival of the Fittest: Time-To-Event Modeling of Crystallization of Amorphous Poorly Soluble Drugs.

Nurzyńska K, Austin RP, Fischer PM, Booth J, Gommer F.

J Pharm Sci. 2016 Jun;105(6):1858-1866. doi: 10.1016/j.xphs.2016.03.014. Erratum in: J Pharm Sci. 2016 Nov;105(11):3464.


Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1.

Jadhav GP, Kaur I, Maryati M, Airhihen B, Fischer PM, Winkler GS.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4219-24. doi: 10.1016/j.bmcl.2015.07.095. Epub 2015 Aug 6.


Long-Term Amorphous Drug Stability Predictions Using Easily Calculated, Predicted, and Measured Parameters.

Nurzyńska K, Booth J, Roberts CJ, McCabe J, Dryden I, Fischer PM.

Mol Pharm. 2015 Sep 8;12(9):3389-98. doi: 10.1021/acs.molpharmaceut.5b00409. Epub 2015 Aug 12.


Development of a simple and sensitive HPLC-UV method for the simultaneous determination of cannabidiol and Δ(9)-tetrahydrocannabinol in rat plasma.

Zgair A, Wong JC, Sabri A, Fischer PM, Barrett DA, Constantinescu CS, Gershkovich P.

J Pharm Biomed Anal. 2015 Oct 10;114:145-51. doi: 10.1016/j.jpba.2015.05.019. Epub 2015 May 22.


Stress responses. Mutations in a translation initiation factor identify the target of a memory-enhancing compound.

Sekine Y, Zyryanova A, Crespillo-Casado A, Fischer PM, Harding HP, Ron D.

Science. 2015 May 29;348(6238):1027-30. doi: 10.1126/science.aaa6986. Epub 2015 Apr 9.


Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity.

Halliday M, Radford H, Sekine Y, Moreno J, Verity N, le Quesne J, Ortori CA, Barrett DA, Fromont C, Fischer PM, Harding HP, Ron D, Mallucci GR.

Cell Death Dis. 2015 Mar 5;6:e1672. doi: 10.1038/cddis.2015.49.


Coagulation factor XII protease domain crystal structure.

Pathak M, Wilmann P, Awford J, Li C, Hamad BK, Fischer PM, Dreveny I, Dekker LV, Emsley J.

J Thromb Haemost. 2015 Apr;13(4):580-91. doi: 10.1111/jth.12849. Epub 2015 Mar 11.


A facile approach to tryptophan derivatives for the total synthesis of argyrin analogues.

Chen CH, Genapathy S, Fischer PM, Chan WC.

Org Biomol Chem. 2014 Dec 28;12(48):9764-8. doi: 10.1039/c4ob02107j.


Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73.

Lam F, Abbas AY, Shao H, Teo T, Adams J, Li P, Bradshaw TD, Fischer PM, Walsby E, Pepper C, Chen Y, Ding J, Wang S.

Oncotarget. 2014 Sep 15;5(17):7691-704.


Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

Reddy TR, Li C, Guo X, Fischer PM, Dekker LV.

Bioorg Med Chem. 2014 Oct 1;22(19):5378-91. doi: 10.1016/j.bmc.2014.07.043. Epub 2014 Aug 7.


Investigation of the flexibility of protein kinases implicated in the pathology of Alzheimer's disease.

Mazanetz MP, Laughton CA, Fischer PM.

Molecules. 2014 Jun 30;19(7):9134-59. doi: 10.3390/molecules19079134.


A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine.

Walsby E, Pratt G, Shao H, Abbas AY, Fischer PM, Bradshaw TD, Brennan P, Fegan C, Wang S, Pepper C.

Oncotarget. 2014 Jan 30;5(2):375-85.


Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.

Shao H, Shi S, Foley DW, Lam F, Abbas AY, Liu X, Huang S, Jiang X, Baharin N, Fischer PM, Wang S.

Eur J Med Chem. 2013;70:447-55. doi: 10.1016/j.ejmech.2013.08.052. Epub 2013 Sep 15.


A fluorescence-based assay suitable for quantitative analysis of deadenylase enzyme activity.

Maryati M, Kaur I, Jadhav GP, Olotu-Umoren L, Oveh B, Hashmi L, Fischer PM, Winkler GS.

Nucleic Acids Res. 2014 Mar;42(5):e30. doi: 10.1093/nar/gkt972. Epub 2013 Oct 28.


5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

Dickens MP, Roxburgh P, Hock A, Mezna M, Kellam B, Vousden KH, Fischer PM.

Bioorg Med Chem. 2013 Nov 15;21(22):6868-77. doi: 10.1016/j.bmc.2013.09.038. Epub 2013 Sep 25.


Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice.

Moreno JA, Halliday M, Molloy C, Radford H, Verity N, Axten JM, Ortori CA, Willis AE, Fischer PM, Barrett DA, Mallucci GR.

Sci Transl Med. 2013 Oct 9;5(206):206ra138. doi: 10.1126/scitranslmed.3006767.


Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

Mistry SN, Baker JG, Fischer PM, Hill SJ, Gardiner SM, Kellam B.

J Med Chem. 2013 May 23;56(10):3852-65. doi: 10.1021/jm400348g. Epub 2013 May 10.


Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.

Shao H, Shi S, Huang S, Hole AJ, Abbas AY, Baumli S, Liu X, Lam F, Foley DW, Fischer PM, Noble M, Endicott JA, Pepper C, Wang S.

J Med Chem. 2013 Feb 14;56(3):640-59. doi: 10.1021/jm301475f. Epub 2013 Jan 25.


Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.

Hole AJ, Baumli S, Shao H, Shi S, Huang S, Pepper C, Fischer PM, Wang S, Endicott JA, Noble ME.

J Med Chem. 2013 Feb 14;56(3):660-70. doi: 10.1021/jm301495v. Epub 2013 Jan 29.


Three-dimensional pharmacophore design and biochemical screening identifies substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

Reddy TR, Li C, Fischer PM, Dekker LV.

ChemMedChem. 2012 Aug;7(8):1435-46. doi: 10.1002/cmdc.201200107. Epub 2012 May 29.


Synthetic lethal targeting of DNA double-strand break repair deficient cells by human apurinic/apyrimidinic endonuclease inhibitors.

Sultana R, McNeill DR, Abbotts R, Mohammed MZ, Zdzienicka MZ, Qutob H, Seedhouse C, Laughton CA, Fischer PM, Patel PM, Wilson DM 3rd, Madhusudan S.

Int J Cancer. 2012 Nov 15;131(10):2433-44. doi: 10.1002/ijc.27512. Epub 2012 Mar 28.


Small molecules that bind the Mdm2 RING stabilize and activate p53.

Roxburgh P, Hock AK, Dickens MP, Mezna M, Fischer PM, Vousden KH.

Carcinogenesis. 2012 Apr;33(4):791-8. doi: 10.1093/carcin/bgs092. Epub 2012 Feb 2.


Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.

Wilson SC, Atrash B, Barlow C, Eccles S, Fischer PM, Hayes A, Kelland L, Jackson W, Jarman M, Mirza A, Moreno J, Nutley BP, Raynaud FI, Sheldrake P, Walton M, Westwood R, Whittaker S, Workman P, McDonald E.

Bioorg Med Chem. 2011 Nov 15;19(22):6949-65. doi: 10.1016/j.bmc.2011.08.051. Epub 2011 Aug 31.


Phase 1 trial of everolimus plus sunitinib in patients with metastatic renal cell carcinoma.

Molina AM, Feldman DR, Voss MH, Ginsberg MS, Baum MS, Brocks DR, Fischer PM, Trinos MJ, Patil S, Motzer RJ.

Cancer. 2012 Apr 1;118(7):1868-76. doi: 10.1002/cncr.26429. Epub 2011 Sep 6.


Immunosuppressive but non-LasR-inducing analogues of the Pseudomonas aeruginosa quorum-sensing molecule N-(3-oxododecanoyl)-l-homoserine lactone.

Jadhav GP, Chhabra SR, Telford G, Hooi DS, Righetti K, Williams P, Kellam B, Pritchard DI, Fischer PM.

J Med Chem. 2011 May 12;54(9):3348-59. doi: 10.1021/jm2001019. Epub 2011 Apr 13.


CDKI-71, a novel CDK9 inhibitor, is preferentially cytotoxic to cancer cells compared to flavopiridol.

Liu X, Shi S, Lam F, Pepper C, Fischer PM, Wang S.

Int J Cancer. 2012 Mar 1;130(5):1216-26. doi: 10.1002/ijc.26127. Epub 2011 Jun 21.


In vitro antitumor mechanism of a novel cyclin-dependent kinase inhibitor CDKI-83.

Liu X, Lam F, Shi S, Fischer PM, Wang S.

Invest New Drugs. 2012 Jun;30(3):889-97. doi: 10.1007/s10637-011-9641-5. Epub 2011 Feb 18.


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