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Dr Robert Falconer

PositionReader in Medicinal Chemistry & YCR Group Leader
DepartmentInstitute of Cancer Therapeutics
Telephone+44 (0) 1274 235842
Emailr.a.falconer1@bradford.ac.uk
LinkedInVisit my LinkedIn profile

Research Interests (key words only)

Cancer Drug Discovery; Medicinal Chemistry; the tumour cell glycocalyx as a therapeutic target; Endoprotease-activated anti-tumour agents

PhD Supervision

Current PhD students

  • Ms Marrwa Ali (PhD student; Scholarship from Ahfad University for Women, Sudan; joint supervision with Dr Steve Shnyder; 2016-20)
  • Mr Francis Mprah Barnieh (PhD student; Ghana Education Trust Scholarship; joint supervision with Prof Paul Loadman; 2016-20)
  • Mr Rene Ankrah (PhD student; Yorkshire Cancer Research; co-supervisor with Prof Paul Loadman and Dr Steve Shnyder; 2013-17)

Graduated MPhil/PhD students

  • Mr Jamal Elbakay; PhD awarded February 2017
  • Ms Sara Elkashef; PhD awarded April 2016
  • Ms Rida Saeed; PhD awarded March 2016
  • Mr. Ahmed Youssef. PhD awarded November 2014
  • Ms Inês Oliveira. MPhil awarded November 2013
  • Mr Bradley Springett. PhD awarded July 2013
  • Mr Yousef Al-Saraireh. PhD awarded September 2012
  • Ms Georgia Tsoukala. PhD awarded February 2009

Teaching and Supervisory Responsibilities

MPharm undergraduate degree

  • Lectures: Common Diseases and their Treatment (PH8312D), Infectious and Neoplastic Disease (PH4019D)

MChem undergraduate degree

  • Module Co-ordinator - Fundamentals of Drug Discovery (CR3002D)
  • Lectures: Fundamentals of Drug Discovery (CR3002D), Biological and Organic Chemistry (CT3007M), Case Studies in Drug Discovery (CR4013D)
  • Supervisor: Stage Four Research Project (CT4015B), Stage Three Research Project (CT3504T)

MSc Cancer Drug Discovery

  • Module Co-ordinator - Principles of Drug Discovery (CR4016D)
  • Lectures and workshops: Principles of Drug Discovery (CR4016D), Case Studies in Drug Discovery (CR4013D), Chemical Toolbox for Drug Discovery (CR4012D)
  • Supervisor: Critical Appraisal of a current topic in Drug Discovery (CR4014L), Research Project in Drug Discovery (CR4015Z)

MSc Safety Pharmacology and Drug Toxicology

  • Lectures: Toxicology and Safety Pharmacology (CR4006D), Molecular mechanisms of toxicity (CR4010D)
  • Supervisor: Critical Appraisal of a topic in Safety Pharmacology (CR4007L), Research Project in Drug Toxicology (CR4011Z)

MSc Cancer Pharmacology

  • Lectures: Molecular Basis of Cancer (CR4001D), Cancer Pharmacology (CR4003D)
  • Supervisor: Critical Appraisal of a topic in Cancer Pharmacology (CR4004L), Research Project in Cancer Pharmacology (CR4005Z)

Administrative Responsibilities

  • Deputy Director, Institute of Cancer Therapeutics
  • Drug Discovery and Medicinal Chemistry Lead, Institute of Cancer Therapeutics
  • School of Pharmacy and Medical Sciences Team Leadership Group member
  • Teaching module leadership: INC6001-B (Fundamentals of Drug Discovery)
  • Teaching module leadership: INC7014-B (Principles of Drug Discovery)

Study History

  • PhD, The School of Pharmacy, University of London (2000)
  • BPharm(Hons), The School of Pharmacy, University of London (1996)
  • MRPharmS, Pre-registration pharmacy training: Dartford & Gravesham NHS Trust (1997)

Professional History

  • Institute of Cancer Therapeutics, University of Bradford (2005-present)
  • Lecturer in Pharmaceutical Sciences; The School of Pharmacy, University of London (2003-2005)
  • Teaching and Research Fellow; The School of Pharmacy, University of London (2000-2003)
  • Locum Pharmacist; Dartford & Gravesham NHS Trust (1997-2000)
  • Staff Pharmacist; Dartford & Gravesham NHS Trust (1997)

Professional Activities

  • Registered Pharmacist with the General Pharmaceutical Council
  • Member of the Royal Pharmaceutical Society (MRPharmS)
  • Founder and Technology Co-inventor, Incanthera Ltd (www.incanthera.com), University of Bradford spin-out company
  • Member of the Royal Society of Chemistry (MRSC)
  • Honorary Treasurer, RSC Central Yorkshire Section Local Trust 2012-18 (three terms); Committee member 2009-11
  • Member of the American Association for Cancer Research (and Chemistry in Cancer Research and Paediatric Cancer working groups)
  • Member of the British Association for Cancer Research and European Association for Cancer Research
  • Elected member of the EPSRC peer review college 2006-2009 and 2010-
  • Grant reviewer for EPSRC, MRC and AICR
  • Scientific Advisory Board Member, Neuroblastoma UK
  • Scientific Committee Member, Kidscan
  • Editorial Board member, Scientific Reports
  • Regular peer reviewer for several journals, including: J.Med.Chem., MedChemComm., Bioorg. Med. Chem., Bioorg. Med.Chem.Lett., Carbohydr. Res., J.Org.Chem., Tetrahedron Lett., Tumour Biology, Neuropathology, Cell Biology & Function, PLoS ONE, Scientia Pharmaceutica, Cancer Biomarkers

Research Areas

Anti-cancer agents targeting the tumour cell glycocalyx

My research is focused on the design, synthesis and biological evaluation of inhibitors of polysialyltransferase as a means by which to modulate tumour cell dissemination. The polysialyltransferases are responsible for the tumour cell surface biosynthesis of polysialic acid (polySia), which plays a key role in the metastatic process in a number of cancers (see review: Curr. Cancer Drug Targets, 2012, 12, 925-939). We are employing computational methods to aid the inhibitor design process and have the capability to assess enzyme inhibition, cell-surface polySia decoration, and effects on cell-cell and cell-matrix adhesion, cell migration and invasion.

This work is currently supported by Yorkshire Cancer Research (programme grant) and the Wellcome Trust (Pathfinder award).

Endoprotease-activated therapeutics

My research is focused on the transformation of potent cytotoxic agents to inactive peptide-conjugates that are selectively activated within the tumour microenvironment. We are currently interested in the matrix metalloproteinases (MMPs) which are a family of endopeptidases overexpressed in tumours. We are employing both solution and solid phase chemistry to synthesise peptide-based therapeutics with potent but selective cytotoxicity in vivo. Our lead agent, ICT-2588 is now progressing towards clinical evaluation by Incanthera Ltd., a university spin-out company (www.incanthera.com), having recently secured funding from Yorkshire Cancer Research.  Compounds are assessed for in vitro cytotoxicity, successful cleavage in tumour tissue, stability in normal tissues (liver, kidney, lung) and plasma, before being evaluated in vivo. Current projects are focused on development of treatments for prostate cancer and osteosarcoma.

This project is a joint effort with Prof Paul Loadman at the Institute, where I oversee the medicinal chemistry aspects of the project. Our research is currently funded by Yorkshire Cancer Research (project).

Research Team:

  • Dr Anjana Patel (PDRA; Wellcome Trust 2016-17)
  • Dr Xiaoxiao Guo (PDRA; YCR programme 2015-17)
  • Dr Marcella Sini (PDRA; YCR programme 2015-17)
  • Dr Goreti Ribeiro Morais (PDRA; YCR programme 2014-17)  
  • Ms Marrwa Ali (PhD student; Ahfad University scholarship; 2016-20)
  • Mr Francis Mprah Barnieh (PhD student; Ghana Education Trust Scholarship; 2016-20)
  • Mr Rene Ankrah (PhD student; Yorkshire Cancer Research; 2013-17)
  • Mr Jamal Elbakay (PhD student; Libyan government scholarship; 2013-17)
  • Ms Angela Florin (Placement student; University of York; 2016-17)

Current Projects

  • Wellcome Trust (Pathfinder award; October 2015; 19 months; £198,338): "Development of novel polysialyltransferase inhibitors for the treatment of neuroblastoma."; Falconer, R.A. (P.I.); Shnyder, S.D.; Loadman, P.M.; Patterson, L.H.
  • Yorkshire Cancer Research (Programme grant; March 2014; 5 years; £1,566,036): "Cancer Medicines Discovery" Patterson, L.H. (P.I.), Falconer, R.A.; Pors, K.; Afarinkia, K.; Loadman, P.M.; Shnyder S.D.
  • Yorkshire Cancer Research (PhD studentship; October 2013; £68,292): "MT-MMP expression in Head and Neck Cancer for Prodrug Development." Loadman, P.M. (P.I.); Falconer, R.A.; Shnyder, S.D.

Research Collaborations

Polysialyltransferase project

  • Scientific partners

    • Prof Rita Gerardy-Schahn (Hannover Medical School, Germany)
    • Prof Minoru Fukuda (Sanford Burnham Prebys Medical Discovery Institute, USA)
    • Dr Daniel Bexell (Lund University, Sweden)
    • Prof Jukka Finne (University of Helsinki, Finland)
    • Prof Natalie Strynadka (University of British Columbia, Canada)
    • Prof Colin Fishwick (University of Leeds, UK)
    • Prof Paul Smith (Cardiff University, UK)
    • Prof Rachel Errington (Cardiff University, UK)
    • Dr Colin Grant, Dr Pete Twigg (Engineering & Informatics, University of Bradford) 
  • Clinical partners

    • Dr Guy Makin (Manchester Children’s Hospital, UK)
    • Prof Chris Twelves (St James's Hospital, Leeds, UK)
    • Dr Catherine Cullinane, Dr Jens Stahlschmidt (St James’ Hospital Leeds, UK)
  • Commercial partners

    • Discovery, Charles River

Endoprotease-activated therapeutics project (with Prof Paul Loadman, ICT):

  • Scientific partners
    • Prof Heike Daldrup-Link (Stanford University, USA)
    • Dr Jianghong Rao (Stanford University, USA)
    • Prof Dylan Edwards (University of East Anglia, UK)
    • Dr Anne Collins (University of York)
    • Dr Jason Gill (Durham University, UK)
  • Clinical partners

    • Prof Chris Twelves (St James’ Hospital Leeds, UK)
    • Prof John Chester (Cardiff University, UK)
    • Prof Malcolm Mason (Cardiff University, UK)
    • Dr Shet Biswas (Southampton Teaching Hospitals, UK)
  • Commercial partners

    • Incanthera Ltd

Publications

  • Mohanty, S.; Chen, Z.; Li, K.; Ribeiro Morais, G.; Klockow, J.; Yerneni, K.; Pisani, L.; Chin, F.T.; Mitra, S.; Cheshier, S.; Chang, E.; Gambhir, S.S.; Rao, J.; Loadman, P.M.; Falconer, R.A.; Daldrup-Link, H.E. “A novel theranostic strategy for MMP-14 expressing glioblastomas impacts survival.” Molecular Cancer Therapeutics, 2017, accepted.

  • Jain, M.; Harburn, J.; Gill, J.H.; Loadman, P.M.; Falconer, R.A.; Mooney, C.; Cobb, S.; Berry, D. “Rationalized Computer-Aided Design of Matrix Metalloprotease-Selective Prodrugs.” Journal of Medicinal Chemistry, 2017, accepted.
  • Ehrit, J.; Keys, T.G.; Sutherland, M.; Wolf, S.; Meier, C.; Falconer, R.A.; Gerardy-Schahn, R. “Exploring and Exploiting Acceptor Preferences of the Human Polysialyltransferases as a Basis for an Inhibitor Screen.” ChemBioChem, 2017, accepted.
  • Gill, J.H.; Loadman, P.M.; Shnyder, S.D.; Cooper, P.A.; Atkinson, J.M.; Ribeiro Morais, G.; Patterson, L.H.; Falconer, R.A. “The Tumor-Targeted Prodrug ICT2588 Demonstrates Therapeutic Activity Against Solid Tumors and Reduced Potential For Cardiovascular Toxicity.” Molecular Pharmaceutics, 2014, 11, 1294−1300
  • Ansari, C.; Tikhomirov, G.A.; Hong, S.H.; Falconer, R.A.; Loadman, P.M.; Gill, J.H.; Castaneda, R.; Hazard, F.K.; Tong, L.; Felsher, D.W.; Rao, J.; Daldrup-Link, H.E. “Development of Novel Tumor-Targeted Theranostic Nanoparticles Activated by Membrane-Type Matrix Metalloproteinases for Combined Cancer Magnetic Resonance Imaging and Therapy.” Small, 2014, 10, 566-575 (front cover p 474)

  • Al-Saraireh, Y.M.J.; Sutherland, M.; Springett, B.R.; Freiberger, F.; Ribeiro Morais, G.; Loadman, P.M.; Errington, R.J.; Smith, P.J.; Fukuda, M.; Gerardy-Schahn, R.; Patterson, L.H.; Shnyder, S.D.; Falconer, R.A. “Pharmacological inhibition of polysialyltransferase ST8SiaII modulates tumour cell migration.” PLoS ONE, 2013, 8, e73366 (open access: click here)

  • Smith, P.J.; Falconer R.A.; Errington, R.J. “Micro-community cytometry: sensing changes in cell health and glycoconjugate expression by imaging and flow cytometry.” Journal of Microscopy, 2013, 251, 113-122

  • Smith, P.J.; Wiltshire, M.; Chappell, S.; Patterson, L.H.; Shnyder, S.D.; Falconer, R.A.; Errington, R.J. “Profiling dynamic changes NCAM polysialylation during adherence transitions of live cells using an antibody-mimetic eGFP-endosialidase and the viability dye DRAQ7.” Cytometry Part A, 2013, 83, 659-671

  • Ribeiro Morais, G.; Falconer, R.A.; Santos, I. “Carbohydrate-based molecules for Molecular Imaging in Nuclear Medicine.” European Journal of Organic Chemistry, 2013, 8, 1401-14

  • Fournier Dit Chabert, J.; Vinader, V.; Santos, A.; Redondo-Horcajo, M.; Dreneau, A.; Basak, R.; Cosentino, L.; Gordon, A.; Abdel-Rahman, H.; Loadman, P.M.; Shnyder, S.D.; Fernando Díaz, F.; Barasoain, I.; Falconer, R.A.; Pors, K. “Synthesis and Biological Evaluation of Colchicine C-Ring Analogues Tethered with Aliphatic Linkers Suitable for Prodrug Derivatisation.” Bioorganic and Medicinal Chemistry Letters, 2012, 22, 7693-7696

  • Falconer, R.A.; Errington, R.J.; Shnyder, S.D.; Smith, P.J.; Patterson, L.H. “Polysialyltransferase: a new target in metastatic cancer.” Current Cancer Drug Targets, 2012, 12, 925-939

Impact

Patents

  • Loadman, P.M.; Falconer, R.A.; Gill, J.H. “Prodrugs” UK Patent Application; Ref: p127743GB00/ILF (Filed 1 December 2015)
  • Falconer, R.A.; Loadman, P.M.; Gill, J.H.; Daldrup-Link, H.; Rao, J. “Tumour-targeted Theranostics.” UK Patent Application; Ref: 1313900.1 (Filed 2 August 2013)
  • Falconer, R.A.; Atkinson, J., Gill, J.H.; Loadman, P.M.; Bibby M.; Patterson, L.H.  “MMP activated anti-vascular agents II” UK Patent Application; Ref: 0819287.4 (2008); PCT/GB2009/002484; WO/2010/046628 (2009)
  • Gill, J.H.; Loadman, P.M.; Falconer, R.A.; Patterson, L.H.; Atkinson, J.; Bibby M.  “MMP activated anti-vascular agents I” Ref 0459P/GB (2007); PCT/GB2008/001043; WO 2008/125800 (2008)
  • Toth, I.; Falconer, R.A. “Preparation of monosaccharide and oligosaccharide lipoamino acids as  pharmaceutical  agents used for oral administration as  delivery  systems.” UK Application. UK 0100115.5, PCT Int. Appl. (2002) WO 2002053572, WO 2002-AU5 20020103 US 2004176281

Selected Oral Presentations

  • “Exploiting the prostate tumour microenvironment for targeted drug delivery.” Prostate Cancer and the Tumour Microenvironment Workshop, 1 February 2017, School of Medicine, Cardiff University, U.K. (Keynote speaker)
  • “Targeting Polysialyltransferase as a Therapeutic Strategy for Cancer.” SialoGlyco 2016, 14-17 November 2016, Santa Barbara CA, USA.
  • “Polysialyltransferase: a novel target for inhibition of tumour dissemination.” YCR Annual Scientific Meeting, 2 July 2015, Harrogate, U.K. (invited speaker)
  • “Development of inhibitors of polysialyltransferases PST and STX: a novel strategy for the treatment of neuroblastoma.” The Neuroblastoma Society Spring Conference, 26 Apr 2014, London, U.K. (invited speaker)
  • Bitter-Sweet – Polysialic acid and metastasis in neuroblastoma” University of Leeds, Paediatric Oncology Research Seminar, 29 Nov 2013, Leeds, U.K
  • “Membrane Type Matrix Metalloproteinase (MT-MMP) targeted anti-tumour agents” YCR Annual Scientific Meeting, 14 June 2011, Harrogate, U.K. (selected speaker)
  • “Design and Synthesis of Membrane Type 1-Matrix Metalloproteinase (MT1-MMP) targeted anti-tumour agents” Spirogen Ltd., 5 August 2009, London, U.K
  • “Design and Synthesis of Membrane Type 1-Matrix Metalloproteinase (MT1-MMP) targeted anti-tumour agents” YCR Annual Scientific Meeting, 26 June 2008, Leeds, U.K
  • “Selective delivery of anti-tumour agents via matrix metalloproteinase (MMP)-cleavable peptides” 1st International Conference on Drug Design and Discovery, 4-7 Feb 2008, Dubai, U.A.E
  • “Strategies for the development of PST inhibitors” Polysialyltransferases as a therapeutic in cancer: Mini-symposium, 8 Aug 2007, Bradford, U.K. (Mini-symposium organiser: speakers from UoB, University of Leeds and Cardiff University)

In the News/Media

Winner of Vice Chancellor’s award for Outstanding achievement 2017 – Team award (PM Loadman; RA Falconer; LH Patterson) for contribution to development of ‘crocus smart bomb’ ICT2588

Flower power Drug crocuses help beat breast, bowel, lung cancers new research reveals - Daily Mail

Cancer charity invests £634,000 to fund trials of Bradford smart bomb drug - Telegraph and Argus

Can a spoon full of sugar treat cancer? - Science Daily

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