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researcher

Professor Robert Falconer

Professor of Medicinal Chemistry

Faculty/Dept/School School of Pharmacy and Medical Sciences
(Faculty of Life Sciences)
Emailr.a.falconer1@bradford.ac.uk
Telephone +441274 235842

Biography

Robert Falconer is a Pharmacist, having obtained his pharmacy degree from The School of Pharmacy, University of London (now UCL School of Pharmacy). He undertook his pre-registration pharmacy training year at Joyce Green Hospital, Dartford, Kent. He then returned to academia in London, where he undertook a PhD in medicinal chemistry (2000). He was subsequently appointed Research & Teaching Fellow, and then Lecturer in Pharmaceutical Sciences.

A move to the new Institute of Cancer Therapeutics (ICT), University of Bradford followed (2005) followed, to establish a new medicinal chemistry team there. He is an academic responsible primarily for research, but also research-informed teaching (primarily the ICT’s post-graduate MSc courses) and the training of research students. His major interests include the cancer cell glycocalyx, and in the development of protease-activated anticancer prodrugs.

He has served as Deputy Director of the ICT since Feb 2017, overseeing medicinal chemistry and drug discovery, and was promoted to Professor of Medicinal Chemistry in 2019. He is a founder of University spin-out company Incanthera plc, leads the ICT's £2m Doctoral Training Centre. He is a member of several professional and learned societies, notably the Royal Pharmaceutical Society and is a registered pharmacist with the General Pharmaceutical Council. As a Fellow of the Royal Society of Chemistry, he has previously served as Honorary Treasurer for the RSC Central Yorkshire Local Section Trust (2012-18).

Research

The Falconer group is primarily focused on the tumour glycocalyx as a therapeutic target, and glycosyltransferases in particular, and in tumour protease-activated drug delivery. He is an experienced principal investigator and has secured funding from research councils and medical charities. He currently holds grants from Breast Cancer Now, Bone Cancer Research Trust, and Incanthera plc. He also leads the newly created Institute of Cancer Therapeutics Doctoral Training Centre (ICT DTC), established in 2019 following a major 10-year investment by Incanthera plc (£2m).  
He has a keen interest and track record in knowledge transfer and cancer drug development. As lead medicinal chemist, he is co-founder and technology co-inventor of the ‘crocus smart-bomb’ (MMP-targeted anti-vascular agent ICT2588), which is being progressed to the clinic by Ellipses Pharma/Incanthera Ltd. Incanthera is an ICT/University of Bradford spin-out company (www.incanthera.com). He is co-inventor on four patents associated with this technology.  

Current Research Projects 

1. Anti-cancer agents targeting the tumour glycocalyx
This research is focused on the design, synthesis and biological evaluation of inhibitors of polysialyltransferase (and prodrugs thereof) as a means by which to modulate tumour cell migration, invasion and metastasis. 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 (see Carbohydrate Polymers, 2021, 259, 117741 and Analyst, 2020, 145. 4512-4521, ), cell-surface polySia decoration (see review: Carbohydrate Polymers2019224, 11545), and effects on cell-cell and cell-matrix adhesion, cell migration and invasion (see PLoS ONE20138, e73366; Scientific Reports, 2016, 6, 33026; ChemBioChem, 2017, 18, 1332-1337). This work is currently supported by a PhD studentship in the ICT Doctoral Training Centre. 

2. Endoprotease-activated therapeutics
This 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, and other endoporteases overexpressed in tumours. We are employing both solution and solid phase chemistry to synthesise peptide-based therapeutics with potent but selective cytotoxicity in vivo. Compounds are assessed for in vitro cytotoxicity, successful cleavage in tumour tissue, stability in normal tissues (liver, kidney, lung) and plasma (key collaboration Prof Paul Loadman, Dr Huw Jones, ICT), before being evaluated in vivo (key collaboration with Dr Steve Shnyder, ICT). We are additionally pursuing prodrugs of DNA repair targets in collaboration with Prof Sherif El-Khamisy (ICT & University of Sheffield). Our lead compound ICT2588 was commercialised through Incanthera plc (see Cancer Research, 2010, 70, 6902-6912; Molecular Pharmaceutics, 2014, 11, 1294−1300). 

We have a particular interest in osteosarcoma, and in developing kinder treatments for this deadly disease that mainly affects children and young adults. Funded by the Bone Cancer Research Trust (BCRT) through a PhD studentship (2018-22), and a project grant (2023-26), our aim is to achieve preclinical proof-of-concept for an MMP-activated tumour-targeted prodrug of methotrexate. We will evaluate our lead molecules in clinically-relevant orthotopic models of the disease in collaboration with Prof Allie Gartland (University of Sheffield). 

A new project focused on neuroblastoma, and targeted delivery of an inhibitor of DNA repair, funded by Worldwide Cancer Research (2023-25) commenced in April 2023.

We continue our long-standing collaboratiion with the Daldrup-Link group (Standford University, USA) to further develop a novel theranostics, which have shown efficacy in breast cancer (see Small, 2014, 10, 566-575) and glioblastoma (see Molecular Cancer Therapeutics, 2017, 16, 1909-1921 and Nanotheranostics, 2019, 3, 299-310).

Current projects are additionally focused on development of treatments for breast cancer, prostate cancer and neuroblastoma. Our research is currently funded by Breast Cancer Now, Bone Cancer Research Trust, Worldwide Cancer Research, the ICT Doctoral Training Centre, and the Masonic Charitable Foundation.

Current Team members

PhD students

Gabriel Nwokolo (Masonic Charitable Foundation 2024-28)

Zubeda Khatoon (ICT DTC 2022-26)

Louise Stevenson (DiMeN/University of Sheffield with Prof Sherif El-Khamisy 2021-24)

Post-Doctoral Researchers 

Dr Goreti Ribeiro Morais (ICT DTC)

Dr Hannah Spencer (BCRT 2023-26)

Dr April Baral (Worldwide Cancer Research 2023-25)

Date Role Title / Description Funder Award
01-OCT-18 - 30-APR-23PIBone Cancer Research Trust - PhD studentship
116626
01-OCT-18 - 30-SEP-28PIIncanthera plc - ICT Doctoral Training Centre
2000000
01-JAN-19 - 28-JAN-24PIBreast Cancer Now - project grant
191037
01-OCT-19 - 30-SEP-23Co-IKidscan - PhD studentship
63675
09-JAN-23 - 08-JAN-26PIBone Cancer Research Trust - project grant
249760
01-APR-23 - 31-DEC-25PIWorldwide Cancer Research - project grant
194381

Teaching

Teaching interests

Robert's teaching activities are primarily focused on the application of medicinal chemistry to cancer drug discovery, with contributions to several modules across the ICT's MSc and MRes post-graduate courses in Cancer Drug Discovery, Cancer Pharmacology, and Drug Toxicology and Safety Pharmacology. He leads the Principles of Drug Discovery module (INC7014-B), which provides an overview of the various elements of the drug discovery process, from designing molecules, through in vitro screening, drug metabolism and ultimately clinical trials. He contributes to some modules in the MPharm Pharmacy and BSc Clinical Sciences degrees.

He regularly supervises research projects and dissertations for MSc/MRes and undergraduate students, including ERASMUS placement students from overseas partners, and is also a personal academic tutor for students undertaking the Foundation in Clinical Sciences course.

Professional activities

  • 01-JAN-97: Dartford & Gravesham NHS Trust - MRPharmS
  • 01-JAN-96: University of London, School of Pharmacy - BPharm (Hons)
  • 01-JAN-00: University of London, School of Pharmacy - PhD

  • 16-DEC-19: University of Bradford - Professor of Medicinal Chemistry
  • 01-SEP-13: University of Bradford - Reader in Medicinal Chemistry
  • 01-SEP-05: University of Bradford - Lecturer in Medicinal Chemistry
  • 01-JUN-03: UCL School of Pharmacy - Lecturer in Pharmaceutical Sciences
  • 01-OCT-00: UCL School of Pharmacy - Research & Teaching Fellow

  • Royal Society of Chemistry, Fellow
  • British Association for Cancer Research, Member
  • European Association for Cancer Research, Member
  • Amercian Association for Cancer Research, Member
  • Royal Pharmaceutical Society / General Pharmaceutical Council, Member

  • 01-JAN-17: Vice-Chancellor's Award for Excellence
  • 01-JAN-19: Fellow, Royal Society of Chemistry
  • 01-JAN-22: Commendation - Outstanding Achievement Award (PhD student supervision)

  • Deputy Director, ICT

  • Research Group Leadership: School of Pharmacy and Medical Sciences Team Leadership Group Member
  • Programme & Module Management: Teaching Module Leadership: INC7014-B (Principles of Drug Discovery)

  • External Examiner: MPharm Pharmacy, BSc Pharmaceutical Sciences, BSc Pharmaceutical Biotechnology School of Pharmacy, Queen’s University Belfast (2020-24)
  • Scientific Advisory Board Member: Health Research Charities Ireland/ Health Research Board Ireland Joint Funding Scheme (2020)
  • External Examiner: MRes Drug Sciences, UCL School of Pharmacy Joint Postgraduate Board (2018-22)
  • Scientific Advisory Board Member: Medical Research Charity Group/ Health Research Board Ireland Joint Funding Committee (2018)
  • Scientific Committee Member: Kidscan Children’s Cancer Research (2016-)
  • Scientific Advisory Board Member: Neuroblastoma UK (2016)
  • Editorial Board Member: Scientific Reports (Nature publishing group) (2016-)
  • Co-Founder, Member of Scientific Advisory Board: Incanthera plc (www.incanthera.com)
  • Committee Member: RSC Central Yorkshire Local Section Member Network (2008-10; 2012-18)
  • Honorary Treasurer: RSC Central Yorkshire Local Section Member Network (2012-18; 3 terms)
  • Elected Member: EPSRC Peer Review College (2006-)

Publications

TitleCancer-specific glycosylation of CD13 impacts its detection and activity in preclinical cancer tissues. (2023)
AuthorsBarnieh FM;Galuska SP;Loadman PM;Ward S;Falconer RA;El-Khamisy SF;
JournalIscience
DOI10.1016/j.isci.2023.108219
 
TitleAzodicarboxylate-mediated peptide cyclisation: application to disulfide bond formation in solution and solid phase. (2023)
AuthorsSerre, A.R.E.; Nwokolo, G.C.; Spencer, H.L.M.; Bell, T.J.; Barnieh, F.M.; Hughes, L.; Falconer, R.A.; Ribeiro Morais, G.
JournalEuropean Journal of Organic Chemistry
DOIDOI:10.1002/ejoc.202300789
 
TitleThe role of MT1-MMP in the progression and metastasis of osteosarcoma (2022)
AuthorsSpencer, H.L.M.; Shnyder, S.D.; Loadman, P.M.; Falconer, R.A.
JournalJournal of Cancer Metastasis and Treatment
DOIDOI:10.20517/2394-4722.2021.174
 
TitleChemoselective Solution- and Solid-Phase Synthesis of Disulfide-Linked Glycopeptides. (2022)
AuthorsBanisalman KAF;Polykandritou A;Barnieh FM;Ribeiro Morais G;Falconer RA;
JournalJournal of Organic Chemistry
DOI10.1021/acs.joc.2c01651
 
TitleTargeted delivery of a colchicine analogue provides synergy with ATR inhibition in cancer cells. (2022)
AuthorsBarnieh FM;Ribeiro Morais G;Garland H;Loadman PM;Falconer RA;
JournalBiochemical Pharmacology
DOI10.1016/j.bcp.2022.115095
 
TitleIs tumour-expressed aminopeptidase N (APN/CD13) structurally and functionally unique? (2021)
AuthorsBarnieh FM;Loadman PM;Falconer RA;
JournalBiochimica et Biophysica Acta - Reviews on Cancer
DOI10.1016/j.bbcan.2021.188641
 
TitleProgress towards a clinically-successful ATR inhibitor for cancer therapy (2021)
AuthorsBarnieh, F.M.; Loadman, P.M.; Falconer, R.A.
JournalCurrent Research in Pharmacology and Drug Discovery
DOI10.1016/j.crphar.2021.100017
 
TitleGlycosyl disulfides: importance, synthesis and application to chemical and biological systems (2021)
AuthorsRibeiro Morais, G.; Falconer, R.A.
JournalOrganic and Biomolecular Chemistry
DOI10.1039/D0OB02079F
 
TitleAn assay for quantitative analysis of polysialic acid expression in cancer cells (2021)
AuthorsGuo, X.; Elkashef, S.M.; Patel, A.; Ribeiro Morais, G.; Shnyder S.D.; Loadman, P.M.; Patterson, L.H.; Falconer, R.A.
JournalCarbohydrate Polymers
DOI10.1016/j.carbpol.2021.117741
 
TitleAn efficient assay for identification and quantitative evaluation of potential polysialyltransferase inhibitors. (2020)
AuthorsGuo X; Malcolm J.R.; Ali M.M.; Ribeiro Morais G; Shnyder S.D.; Loadman P.M.; Patterson L.H.; Falconer R.A.
JournalANALYST (PRINT)
DOI10.1039/d0an00721h
 
TitleRecent advances in the analysis of polysialic acid from complex biological systems (2019)
AuthorsXiaoxiao Guo, Sara M. Elkashef, Mark Sutherland, Paul M. Loadman and Robert A. Falconer
JournalCarbohydrate Polymers
DOI10.1016/j.carbpol.2019.115145
 
TitleNovel Ran-RCC1 inhibitory peptide-loaded nanoparticles have anti-cancer efficacy in vitro and in vivo (2019)
AuthorsHaggag, Y.A.; Matchett, K.B.; Falconer, R.A.; Isreb, M.; Jones, J.; Faheem, A.; McCarron, P.; El-Tanani, Mohamed
JournalCancers
DOI10.3390/cancers11020222
 
TitleTheranostic nanoparticles enhance the response of glioblastomas to radiation (2019)
AuthorsWu, W.; Klockow, J.L.; Mohanty, S.; Ku, K.S.; Aghighi, M.; Melemenidis, S.; Chen, Z.; Li, K.; Ribeiro Morais, Goreti; Zhao, N.; Schlegel, J.; Graves, E.E.; Rao, J.; Loadman, Paul M.; Falconer, R.A.; Mukherjee, S.; Chin, F.T.; Daldrup-Link, H.E.
JournalNanotheranostics
DOI10.7150/ntno.35342
 
TitleMembrane-type matrix metalloproteinases: expression, roles in metastatic prostate cancer progression and opportunities for drug targeting (2017)
AuthorsFalconer, R.A.; Loadman, P.M.
JournalJournal of Cancer Metastasis and Treatment
DOI10.20517/2394-4722.2017.40
 
TitleA novel theranostic strategy for MMP-14 expressing glioblastomas impacts survival (2017)
AuthorsMohanty, S.; Chen, Z.; Li, K.; Ribeiro Morais, G.; Klockow, J.; Yerneni, K.; Pasani, 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.
JournalMolecular Cancer Therapeutics
DOI10.1158/1535-7163.MCT-17-0022
 
TitleRationalized Computer-Aided Design of Matrix-Metalloprotease-Selective Prodrugs (2017)
AuthorsJain, M.; Harburn, J.J.; Gill, J.H.; Loadman, P.M.; Falconer, R.A.; Mooney, C.A.; Cobb, S.L.; Berry, David J.
JournalJournal of Medicinal Chemistry
DOI10.1021/acs.jmedchem.6b01472
 
TitleExploring and Exploiting Acceptor Preferences of the Human Polysialyltransferases as a Basis for an Inhibitor Screen (2017)
AuthorsEhrit, J.; Keys, T.G.; Sutherland, Mark H.; Wolf, S.; Meier, C.; Falconer, R.A.; Gerardy-Schahn, R.
JournalChemBioChem
DOI10.1002/cbic.201700157
 
TitleThe use of thermographic imaging to evaluate therapeutic response in human tumour xenograft models (2016)
AuthorsHussain, Nosheen; Connah, David; Ugail, Hassan; Cooper, Patricia A.; Falconer, Robert A.; Patterson, Laurence H.; Shnyder, Steven D.
JournalScientific Reports
DOI10.1038/srep31136
 
TitlePolysialic acid sustains cancer cell survival and migratory capacity in a hypoxic environment (2016)
AuthorsElkashef, Sara M.; Allison, Simon J.; Sadiq, Maria; Basheer, Haneen A.; Ribeiro Morais, Goreti; Loadman, Paul M.; Pors, Klaus; Falconer, Robert A.
JournalScientific Reports
DOI10.1038/srep33026
 
TitleThe Effect of Polysialic Acid Expression on Glioma Cell Nano-mechanics (2016)
AuthorsGrant, Colin A.; Twigg, Peter C.; Saeed, Rida F.; Lawson, G.; Falconer, Robert A.; Shnyder, Steven D.
JournalBioNanoScience
DOI10.1007/s12668-016-0192-2
 
TitleAn optimised assay for quantitative, high-throughput analysis of polysialyltransferase activity (2016)
AuthorsElkashef, Sara M.; Sutherland, Mark H.; Patterson, Laurence H.; Loadman, Paul M.; Falconer, Robert A.
JournalANALYST (PRINT)
DOI10.1039/c6an01073c
 
TitleNovel strategies for the synthesis of unsymmetrical glycosyl disulfides (2016)
AuthorsRibeiro Morais, Goreti; Springett, Bradley R.; Pauze, Martin; Schröder, Lisa; Northrop, Matthew; Falconer, Robert A.
JournalOrganic and Biomolecular Chemistry
DOI10.1039/c6ob00230g
 
TitleDevelopment of Novel Tumor-Targeted Theranostic Nanoparticles Activated by Membrane-Type Matrix Metalloproteinases for Combined Cancer Magnetic Resonance Imaging and Therapy (2014)
AuthorsAnsari, C.; Tikhomirov, G.A.; Hong, S.H.; Falconer, Robert A.; Loadman, Paul M.; Gill, Jason H.; Castaneda, R.; Hazard, F.K.; Tong, L.; Lenkov, O.D.; Felsher, D.W.; Rao, J.; Daldrup-Link, H.E.
JournalSmall
DOI10.1002/smll.201301456
 
TitleTumor-Targeted Prodrug ICT2588 Demonstrates Therapeutic Activity Against Solid Tumors and Reduced Potential For Cardiovascular Toxicity (2014)
AuthorsGill, Jason H.; Loadman, Paul M.; Shnyder, Steven D.; Cooper, Patricia A.; Atkinson, Jennifer M.; Ribeiro Morais, Goreti; Patterson, Laurence H.; Falconer, Robert A.
JournalMolecular Cancer Therapeutics
DOI10.1021/mp400760b
 
TitlePharmacological Inhibition of polysialyltransferase ST8SiaII Modulates Tumour Cell Migration (2013)
AuthorsAl-Saraireh, Yousef M.J.; Sutherland, Mark H.; Springett, Bradley R.; Freiberger, F.; Ribeiro Morais, Goreti; Loadman, Paul M.; Errington, R.J.; Smith, P.J.; Fukuda, M.; Gerardy-Schahn, R.; Patterson, Laurence H.; Shnyder, Steven D.; Falconer, Robert A.
JournalPLoS ONE
DOI10.1371/journal.pone.0073366
 
TitleNCAM polysialylation during adherence transitions: Live cell monitoring using an antibody-mimetic EGFP-endosialidase and the viability dye DRAQ7 (2013)
AuthorsSmith P.;Furon E.;Wiltshire M.;Chappell S.;Patterson L.;Shnyder S.;Falconer R.;Errington R.
JournalCytometry Part A
DOI10.1002/cyto.a.22306
 
TitleCarbohydrate-based molecules for Molecular Imaging in Nuclear Medicine (2013)
AuthorsRibeiro Morais G.;Falconer R.;Santos I.
JournalEuropean Journal of Organic Chemistry
DOI10.1002/ejoc.201201457
 
TitleMicro-community cytometry: Sensing changes in cell health and glycoconjugate expression by imaging and flow cytometry (2013)
AuthorsSmith P.;Falconer R.;Errington R.
JournalJournal of Microscopy
DOI10.1111/jmi.12060
 
TitlePolysialyltransferase: A new target in metastatic cancer (2012)
AuthorsFalconer R.;Errington R.;Shnyder S.;Smith P.;Patterson L.
JournalCurrent Cancer Drug Targets
DOI10.2174/156800912803251225
 
TitleSynthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation (2012)
AuthorsFournier-Dit-Chabert J.;Vinader V.;Santos A.;Redondo-Horcajo M.;Dreneau A.;Basak R.;Cosentino L.;Marston G.;Abdel-Rahman H.;Loadman P.;Shnyder S.;Díaz J.;Barasoain I.;Falconer R.;Pors K.
JournalBioorganic and Medicinal Chemistry Letters
DOI10.1016/j.bmcl.2012.09.104
 
TitleAn optimized method for the synthesis of amino-functionalized phosphatidylcholine (2012)
AuthorsKong F.;Morais G.;Falconer R.;Sutton C.
JournalTetrahedron Letters
DOI10.1016/j.tetlet.2011.11.100
 
TitleIdentification of an acetyl disulfide derivative in the synthesis of thiosialosides (2010)
AuthorsMorais G.;Oliveira I.;Humphrey A.;Falconer R.
JournalCarbohydrate Research
DOI10.1016/j.carres.2009.10.017
 
TitleDevelopment of a novel tumor-targeted vascular disrupting agent activated by membrane-type matrix metalloproteinases (2010)
AuthorsAtkinson J.;Falconer R.;Edwards D.;Pennington C.;Siller C.;Shnyder S.;Bibby M.;Patterson L.;Loadman P.;Gill J.
JournalCancer Research
DOI10.1158/0008-5472.CAN-10-1440