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Professor Robert Falconer,
Professor of Medicinal Chemistry

Information about Professor Robert Falconer at the University of Bradford.

School of Pharmacy & Medical Sciences
(Faculty of Life Sciences)
Email:
r.a.falconer1@bradford.ac.uk
Telephone:
+44 1274 235842
Photo of Professor Robert Falconer

3

supervised researchers.

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 Polymers, 2019, 224, 11545), and effects on cell-cell and cell-matrix adhesion, cell migration and invasion (see PLoS ONE, 2013, 8, 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 therapeuticsThis 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 membersPhD studentsGabriel 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)

Research supervision

Professor Robert Falconer is responsible for the supervision of 3 postgraduate researchers at the University of Bradford.

Teaching

Details on teaching interests, highlights and modules are available for Professor Robert Falconer as follows:

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

Information about education, employment and areas of particular interest for Professor Robert Falconer is as follows:

Employment

  • University of Bradford - Reader in Medicinal Chemistry in the year 2013 (specified as 01/09/2013)
  • UCL School of Pharmacy - Research & Teaching Fellow in the year 2000 (specified as 01/10/2000)
  • UCL School of Pharmacy - Lecturer in Pharmaceutical Sciences in the year 2003 (specified as 01/06/2003)
  • University of Bradford - Lecturer in Medicinal Chemistry in the year 2005 (specified as 01/09/2005)
  • University of Bradford - Professor of Medicinal Chemistry in the year 2019 (specified as 16/12/2019)

Education

  • University of London, School of Pharmacy - PhD
  • University of London, School of Pharmacy - BPharm (Hons)
  • Dartford & Gravesham NHS Trust - MRPharmS

Publications

There are 13 publications involving or that are attributed to Professor Robert Falconer.

Peer Reviewed Journal

Professor Robert Falconer has 13 publication(s) listed under peer reviewed journal.
Title Year Publication name Journal Volume Pages Authors Editors ISSN Publisher DOI Location
Recent advances in the analysis of polysialic acid from complex biological systems 2019 Carbohydrate Polymers 16 Xiaoxiao Guo, Sara M. Elkashef, Mark Sutherland, Paul M. Loadman and Robert A. Falconer 10.1016/j.carbpol.2019.115145
Dess–Martin periodinane-mediated oxidation of the primary alcohol of cytidine into a carboxylic acid 2024 Organic and Biomolecular Chemistry 22 Serre, A.R.E;Jha, V.;Rivault, A.;Eriksson, L.A.;Ribeiro Morais, G.;Falconer, R.A. Royal Society of Chemistry 10.1039/d4ob00240g
Cancer-specific glycosylation of CD13 impacts its detection and activity in preclinical cancer tissues. 2023 Iscience 26 Barnieh FM;Galuska SP;Loadman PM;Ward S;Falconer RA;El-Khamisy SF; 2589-0042 10.1016/j.isci.2023.108219
Chemoselective Solution- and Solid-Phase Synthesis of Disulfide-Linked Glycopeptides. 2022 Journal of Organic Chemistry 87 Banisalman KAF;Polykandritou A;Barnieh FM;Ribeiro Morais G;Falconer RA; 1520-6904 10.1021/acs.joc.2c01651
Azodicarboxylate-mediated peptide cyclisation: application to disulfide bond formation in solution and solid phase. 2023 European Journal of Organic Chemistry 26 Serre, A.R.E.; Nwokolo, G.C.; Spencer, H.L.M.; Bell, T.J.; Barnieh, F.M.; Hughes, L.; Falconer, R.A.; Ribeiro Morais, G. DOI:10.1002/ejoc.202300789
Is tumour-expressed aminopeptidase N (APN/CD13) structurally and functionally unique? 2021 Biochimica et Biophysica Acta - Reviews on Cancer 1876 Barnieh FM;Loadman PM;Falconer RA; 1879-2561 10.1016/j.bbcan.2021.188641
The role of MT1-MMP in the progression and metastasis of osteosarcoma 2022 Journal of Cancer Metastasis and Treatment 9 Spencer, H.L.M.; Shnyder, S.D.; Loadman, P.M.; Falconer, R.A. DOI:10.20517/2394-4722.2021.174
Progress towards a clinically-successful ATR inhibitor for cancer therapy 2021 Current Research in Pharmacology and Drug Discovery 2 100017 Barnieh, F.M.; Loadman, P.M.; Falconer, R.A. 10.1016/j.crphar.2021.100017
An assay for quantitative analysis of polysialic acid expression in cancer cells 2021 Carbohydrate Polymers 259 Guo, X.; Elkashef, S.M.; Patel, A.; Ribeiro Morais, G.; Shnyder S.D.; Loadman, P.M.; Patterson, L.H.; Falconer, R.A. 10.1016/j.carbpol.2021.117741
Glycosyl disulfides: importance, synthesis and application to chemical and biological systems 2021 Organic and Biomolecular Chemistry 19 Ribeiro Morais, G.; Falconer, R.A. 10.1039/D0OB02079F
An efficient assay for identification and quantitative evaluation of potential polysialyltransferase inhibitors. 2020 ANALYST (PRINT) 145 4512 - 4521 Guo X; Malcolm J.R.; Ali M.M.; Ribeiro Morais G; Shnyder S.D.; Loadman P.M.; Patterson L.H.; Falconer R.A. 1364-5528 10.1039/d0an00721h
Novel Ran-RCC1 inhibitory peptide-loaded nanoparticles have anti-cancer efficacy in vitro and in vivo 2019 Cancers 11 222 Haggag, Y.A.; Matchett, K.B.; Falconer, R.A.; Isreb, M.; Jones, J.; Faheem, A.; McCarron, P.; El-Tanani, Mohamed 10.3390/cancers11020222
Theranostic nanoparticles enhance the response of glioblastomas to radiation 2019 Nanotheranostics 3 299 - 310 Wu, 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. 10.7150/ntno.35342