Antioxidant, Anti-Inflammatory, and Oral Bioavailability of Novel Sulfonamide Derivatives of Gallic Acid
D Alhyari;N A Qinna;H M Sheldrake;S Kantamneni;B Y Ghanem;K J Paluch (2025) Antioxidants. 14
Dr. Helen Sheldrake
Assistant Professor
- Area
- School of Pharmacy & Medical Sciences
- Faculty of Life Sciences
- Phone
Biography
Helen Sheldrake studied Natural Sciences followed by a PhD in natural product synthesis at the University of Cambridge. After postdoctoral work at The University of Manchester, she joined the Institute of Cancer Therapeutics, University of Bradford as a RCUK Academic Fellow in Medicinal Chemistry. She is now a Lecturer in the School of Pharmacy and Medical Sciences, and School Health and Safety Lead.
Research
New synthetic methods for biologically active/druglike molecules. Design and synthesis of integrin antagonists. Total synthesis.
The integrins are a family of transmembrane receptors which mediate cell-cell and cell-ECM adhesion, and signalling across the cell membrane involved in pathways controlling cell migration, proliferation, differentiation, cell survival and apoptosis. In cancers, their vital role in the cross-talk between the cell and extracellular matrix enhances the growth, migration, invasion and metastasis of cancer cells. The RGD-binding subfamily of integrins are of particular interest as anticancer targets, since there is strong evidence that their expression in cancers is correlated with tumour progression, treatment resistance, and a cancer stem cell phenotype. Research areas currently under investigation include:
- Investigation of combination therapies to combat integrin-mediated resistance to existing anticancer agents
- Targeted integrin degradation
- Synthesis and characterisation of new integrin targeting small molecules for the treatment of advanced cancers, particularly metastatic prostate cancer and malignant melanoma.
- Synthesis of biologically active natural products, and derivatives. Current targets include Nigramide Q and Scopariusicides A-C.
Postgraduate Supervision
Currently Dr Sheldrake is supervisor to the following postgraduate students:
Name: Reuben
McKay
Contact details: r.c.mckay@bradford.ac.uk
Project outline: Reuben’s current research uses enamine cyclisation reactions to explore analogues of natural products with potential antibacterial and anticancer activities.
Note list only includes students who have opted in.
Supervision Capacity and Current Project Availability
I currently have capacity to supervise new Self-funded Postgraduate Researchers. To see available projects, please visit https://www.findaphd.com/phds/faculty-of-life-sciences/?c0g71Ug0 To apply online, complete our application form Complete Postgraduate Enquiry Form HERE
Teaching
Current teaching activities:
Programme Leader: Clinical Sciences
Module Leader: CLS3006-C Chemistry, CLS5013-B Pharmacology and Therapeutics; INC7018-E Research Project
Professional activities
Education (3)
- Fellow of the Higher Education Academy
- University of Cambridge - PhD
- University of Cambridge - MSci
Employment (2)
- University of Bradford - RCUK Academic Fellow in Medicinal Chemistry (1 January 2007)
- The University of Manchester - Postdoctoral Research Associate (1 January 2004)
Publications
Peer reviewed journal (19)
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Sidechain structure-activity relationships of cyclobutane-based small molecule αvβ3 antagonists
Adam Throup;Manar Saleh Zraikat;Andrew Gordon;Shohreh Jafarinejad Soumehsaraei;Kathrin D Haase;Laurence H Patterson;Patricia A Cooper;Katherine Hanlon;Paul M Loadman;Mark Sutherland;Steven D Shnyder;Helen M Sheldrake (2024) Rsc Medicinal Chemistry.
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Overcoming Vemurafenib Resistance in Metastatic Melanoma: Targeting Integrins to Improve Treatment Efficacy
Asiye Busra Boz Er;Helen M Sheldrake;Mark Sutherland (2024) International Journal of Molecular Sciences. 25
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Synthesis and Biological Evaluation of Cyclobutane-Based β3 Integrin Antagonists: A Novel Approach to Targeting Integrins for Cancer Therapy
Mark Sutherland, Andrew Gordon, Fatemah OFO Al-Shammari, Adam Throup, Amy Cilia La Corte, Helen Philippou, Steven D Shnyder, Laurence H Patterson, Helen M Sheldrake (2023) Cancers. 15
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Probing cytochrome P450 (CYP) bioactivation with chloromethylindoline bioprecursors derived from the duocarmycin family of compounds.
Ortuzar N;Karu K;Presa D;Morais GR;Sheldrake HM;Shnyder SD;Barnieh FM;Loadman PM;Patterson LH;Pors K;Searcey M; (2021) Bioorganic and Medicinal Chemistry. 40
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Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo-keto reductase 1C3 target affinity
Santos A.;Sheldrake H.;Ibrahim A.;Danta C.;Bonanni D.;Daga M.;Oliaro-Bosso S.;Boschi D.;Lolli M.;Pors K. (2019) MedChemComm. 10, 1476-1480.
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RGD-Binding Integrins in Head and Neck Cancers
Ahmedah, H.T.; Patterson, Laurence H.; Shnyder, Steven D.; Sheldrake, Helen M. (2017)
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Intramolecular thermal stepwise [2 + 2] cycloadditions: investigation of a stereoselective synthesis of [n.2.0]-bicyclolactones
Throup, Adam; Patterson, Laurence H.; Sheldrake, Helen M. (2016)
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Solid-phase synthesis of duocarmycin analogues and the effect of C-terminal substitution on biological activity
Stephenson, M.J.; Howell, L.A.; O'Connell, M.A.; Fox, K.R.; Adcock, C.; Kingston, J.; Sheldrake, Helen M.; Pors, Klaus; Collingwood, S.P.; Searcey, M. (2015)
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Strategies to inhibit tumour associated integrin receptors: rationale for dual and multi-antagonists
Sheldrake, Helen M.; Patterson, Laurence H. (2014)
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Antitumor activity of a duocarmycin analogue rationalized to be metabolically activated by cytochrome P450 1A1 in human transitional cell carcinoma of the bladder
Sutherland, Mark H.; Gill, Jason H.; Loadman, Paul M.; Laye, Jonathan P.; Sheldrake, Helen M.; Illingworth, Nicola A.; Alandas, Mohammed N.; Cooper, Patricia A.; Searcey, M.; Pors, Klaus; Shnyder, Steven D.; Patterson, Laurence H. (2013)
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Re-engineering of the Duocarmycin Structural Architecture Enables Bioprecursor Development Targeting CYP1A1 and CYP2W1 for Biological Activity
Sheldrake, Helen M.; Travica, S.; Johansson, I.; Loadman, Paul M.; Sutherland, Mark H.; Elsalem, Lina M.I.; Illingworth, Nicola A.; Cresswell, Alexander J.; Reuillon, Tristan; Shnyder, Steven D.; Mkrtchian, S.; Searcey, M.; Ingelman-Sundberg, M.; Patterson, Laurence H.; Pors, Klaus (2013)
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Colon cancer-specific cytochrome P450 2W1 converts duocarmycin analogues into potent tumor cytotoxins
Travica, S.; Pors, Klaus; Loadman, Paul M.; Shnyder, Steven D.; Johansson, I.; Alandas, Mohammed N.; Sheldrake, Helen M.; Mkrtchian, S.; Patterson, Laurence H.; Ingelman-Sundberg, M. (2013)
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Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity
Pors, Klaus; Loadman, Paul M.; Shnyder, Steven D.; Sutherland, Mark H.; Sheldrake, Helen M.; Guino, M.; Kiakos, K.; Hartley, J.A.; Searcey, M.; Patterson, Laurence H. (2011)
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Function and Antagonism of beta3 integrins in the development of cancer therapy
Sheldrake, Helen M.; Patterson, Laurence H. (2009)
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Chemical and Biological Explorations of the Family of CC-1065 and the Duocarmycin Natural Products.
Ghosh, Nandita; Sheldrake, Helen M.; Searcey, M.; Pors, Klaus (2009)
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Synthesis of the originally proposed structure of elatenyne and an enyne from Laurencia majuscula
Sheldrake, Helen M.; Jamieson, C.; Pascu, S.I.; Burton, J.W. (2009)
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Rapid stereoselective access to the tetracyclic core of puupehenone and related sponge metabolites using metal-free radical cyclisations of cyclohexenyl-substituted 3-bromochroman-4-ones.
Pritchard, R.P.; Sheldrake, Helen M.; Taylor, I.Z.; Wallace, T.W. (2008)
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Reduction of Propargylic Sulfones to (Z)-Allylic Sulfones using Zinc and Ammonium Chloride.
Sheldrake, Helen M.; Wallace, T.W. (2007)
Reviews (5)
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RGD-binding integrins in head and neck cancers
Ahmedah H.;Patterson L.;Shnyder S.;Sheldrake H. (2017) Cancers.
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Strategies to inhibit tumor associated integrin receptors: Rationale for dual and multi-antagonists
Sheldrake H.;Patterson L. (2014) Journal of Medicinal Chemistry.
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RGD-binding integrins in prostate cancer: Expression patterns and therapeutic prospects against bone metastasis
Sutherland M.;Gordon A.;Shnyder S.;Patterson L.;Sheldrake H. (2012) Cancers.
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Chemical and biological explorations of the family of CC-1065 and the duocarmycin natural products
Ghosh N.;Sheldrake H.;Searcey M.;Pors K. (2009) Current Topics in Medicinal Chemistry.
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Function and antagonism of β
3 integrins in the development of cancer therapySheldrake H.;Patterson L. (2009) Current Cancer Drug Targets.