• Room 03.011 - CCRCB

    United Kingdom

Accepting PhD Students

PhD projects

My lab is open to medicinal chemistry and biochemistry PhD studentships applications. Research fields of interest include: - small molecule inhibitors - protease chemical biology - cancer - respiratory diseases - cystic fibrosis Previous research experience is desirable although not essential.

20022020

Research output per year

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Research Output

  • 38 Article
  • 1 Conference contribution
  • 1 Review article
  • 1 Other contribution
2020

Development of a novel allograft model of prostate cancer: a new tool to inform clinical translation

Haughey, C. M., Mukherjee, D., Steele, R. E., Popple, A., Dura-Perez, L., Pickard, A., Jain, S., Mullan, P. B., Williams, R., Oliveira, P., Buckley, N. E., Honeychurch, J., Williams, R., McDade, S., Illidge, T., Mills, I. G. & Eddie, S. L., 2020

Research output: Other contribution

Open Access
2019

A Novel Role for Cathepsin S as a Potential Biomarker in Triple Negative Breast Cancer

Wilkinson, R., Burden, R., McDowell, S., McArt, D., McQuaid, S., Bingham, V., Williams, R., Cox, O., O'Connor, R., McCabe, N., Kennedy, R., Buckley, N. E. & Scott, C., 28 Jun 2019, In : Journal of Oncology.

Research output: Contribution to journalArticle

Open Access
File
78 Downloads (Pure)

Application of nanotechnology to target and exploit tumour associated proteases

Cogo, F., Williams, R., Burden, R. E. & Scott, C. J., 01 Nov 2019, In : Biochimie. 166, p. 112-131

Research output: Contribution to journalReview article

Identification and SAR exploration of a novel series of Legumain inhibitors

Eddie, S. L., Gregson, A., Graham, E., Burton, S., Harrison, T., Burden, R., Scott, C. J., Mullan, P. B. & Williams, R., 15 Jun 2019, In : Bioorganic & Medicinal Chemistry Letters. 29, 12, p. 1546-1548 3 p.

Research output: Contribution to journalArticle

2018

Development of an advanced nanoformulation for the intracellular delivery of a caspase-3 selective activity-based probe

Cogo, F., Smyth, P., Burden, R., Longley, D. B., Williams, R., Johnston, M., Poreba, M., Rut, W., Groborz, K., Salvesen, G., Drag, M. & Scott, C. J., 13 Dec 2018, In : Nanoscale - Royal Society of Chemistry.

Research output: Contribution to journalArticle

Open Access
File
1 Citation (Scopus)
41 Downloads (Pure)
2016

A bioavailable cathepsin S nitrile inhibitor abrogates tumor development

Wilkinson, R. D. A., Young, A., Burden, R. E., Williams, R. & Scott, C. J., 21 Apr 2016, In : Molecular Cancer. 15, 29, 11 p.

Research output: Contribution to journalArticle

Open Access
File
12 Citations (Scopus)
258 Downloads (Pure)

ADAM17: a potential regulator of resistance to EGFR targeted therapies in RAS wild type colorectal cancer.

Weir, J-A., Gilliland, P., Fuchs, M-A., Williams, R., Murray, L., Johnston, P. & Van Schaeybroeck, S., Nov 2016, ADAM17: a potential regulator of resistance to EGFR targeted therapies in RAS wild type colorectal cancer.. National Cancer Research Institute

Research output: Chapter in Book/Report/Conference proceedingConference contribution

Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors

Ness, K. A., Eddie, S. L., Burton, S., Harrison, T., Mullan, P. & Williams, R., 15 Jan 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 2, p. 413-6 4 p.

Research output: Contribution to journalArticle

1 Citation (Scopus)

Neutrophilic Cathepsin C Is Maturated by a Multistep Proteolytic Process and Secreted by Activated Cells during Inflammatory Lung Diseases

Hamon, Y., Legowska, M., Hervé, V., Dallet-Choisy, S., Marchand-Adam, S., Vanderlynden, L., Demonte, M., Williams, R., Scott, C. J., Si-Tahar, M., Heuzé-Vourc'h, N., Lalmanach, G., Jenne, D. E., Lesner, A., Gauthier, F. & Korkmaz, B., 15 Apr 2016, In : The Journal of biological chemistry. 291, 16, p. 8486-99 14 p.

Research output: Contribution to journalArticle

20 Citations (Scopus)
2015

CCL2 is transcriptionally controlled by the lysosomal protease cathepsin S in a CD74-dependent manner

Wilkinson, R., Magorrian, S., Williams, R., Young, A., Small, D., Scott, C. & Burden, R., 22 Aug 2015, In : Oncotarget. p. 1-15 15 p.

Research output: Contribution to journalArticle

Open Access
File
16 Citations (Scopus)
197 Downloads (Pure)

Development of a potent and selective cell penetrant Legumain inhibitor

Ness, K. A., Eddie, S. L., Higgins, C. A., Templeman, A., D'Costa, Z., Gaddale, K. K. D., Bouzzaoui, S., Jordan, L., Janssen, D., Harrison, T., Burkamp, F., Young, A., Burden, R., Scott, C. J., Mullan, P. B. & Williams, R., 01 Dec 2015, In : Bioorganic and Medicinal Chemistry Letters. 25, 23, p. 5642-5645

Research output: Contribution to journalArticle

6 Citations (Scopus)
2014

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead

Jones, C. K., Sheffler, D. J., Williams, R., Jadhav, S. B., Felts, A. S., Morrison, R. D., Niswender, C. M., Daniels, J. S. & Conn, P. J., 15 Feb 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 5, p. 1067-1070 4 p.

Research output: Contribution to journalArticle

7 Citations (Scopus)

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres

Sheffler, D. J., Nedelovych, M. T., Williams, R., Turner, S. C., Duerk, B. B., Robbins, M. R., Jadhav, S. B., Niswender, C. M., Jones, C. K., Conn, P. J., Daniels, R. N. & Lindsley, C. W., 15 Feb 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 4, p. 1062-1066 5 p.

Research output: Contribution to journalArticle

3 Citations (Scopus)

P3 SAR exploration of biphenyl carbamate based Legumain inhibitors

Higgins, C., Bouazzaoui, S., Gaddale Devanna, K., D'Costa, Z., Templeman, A., O'Rourke, M., Young, A., Scott, C., Harrison, T., Mullan, P. & Williams, R., 01 Jun 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 11, p. 2521-2524

Research output: Contribution to journalArticle

4 Citations (Scopus)

TBX2 represses CST6 resulting in uncontrolled legumain activity to sustain breast cancer proliferation: a novel cancer-selective target pathway with therapeutic opportunities.

D'Costa, Z. C., Higgins, C., Ong, C. W., Irwin, G. W., Boyle, D., McArt, D. G., McCloskey, K., Buckley, N. E., Crawford, N. T., Thiagarajan, L., Murray, J. T., Kennedy, R. D., Mulligan, K. A., Harkin, D. P., Waugh, D. J. J., Scott, C. J., Salto-Tellez, M., Williams, R. & Mullan, P. B., 08 Feb 2014, In : Oncotarget. 5, 6, p. 1609-1620 12 p.

Research output: Contribution to journalArticle

Open Access
File
23 Citations (Scopus)
210 Downloads (Pure)
2013

Expanded iron uta spectra - Probing the thermal stability limits in AGN clouds

Ferland, G. J., Kisielius, R., Keenan, F. P., Van Hoof, P. A. M., Jonauskas, V., Lykins, M. L., Porter, R. L. & Williams, R. J. R., 20 Apr 2013, In : Astrophysical Journal. 767, p. 1-12 123.

Research output: Contribution to journalArticle

4 Citations (Scopus)
2012
11 Citations (Scopus)
2011

Allosteric Modulators of Metabotropic Glutamate Receptor 5 for Treatment of Schizophrenia

Stauffer, S. R., Manka, J., Williams, R., Noetzel, M. J., Jadhav, S., Menion, U., Vinson, P., Niswender, C. M., Rook, J. M., Lindsley, C. W., Weaver, C. D., Conn, P. J., Blatt, T. N. & Days, E. L., 2011, In : CURRENT NEUROPHARMACOLOGY. 9, p. 11-12 2 p.

Research output: Contribution to journalArticle

Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

Williams, R., Manka, J. T., Rodriguez, A. L., Vinson, P. N., Niswender, C. M., Weaver, C. D., Jones, C. K., Conn, P. J., Lindsley, C. W. & Stauffer, S. R., 01 Mar 2011, In : Bioorganic & Medicinal Chemistry Letters. 21, 5, p. 1350-1353 4 p.

Research output: Contribution to journalArticle

34 Citations (Scopus)
2010

Context-Dependent Pharmacology Exhibited by Negative Allosteric Modulators of Metabotropic Glutamate Receptor 7

Niswender, C. M., Johnson, K., Miller, R., Ayala, J. E., Luo, H-K., Williams, R., Saleh, S., Orton, S., Weaver, C. D. & Conn, L., Mar 2010, In : Molecular Pharmacology. 77, 3, p. 459-468 10 p.

Research output: Contribution to journalArticle

59 Citations (Scopus)

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable gamma-Secretase Inhibitor

Gillman, K. W., Starrett, J. E., Parker, M. F., Xie, K., Bronson, J. J., Marcin, L. R., McElhone, K. E., Bergstrom, C. P., Mate, R. A., Williams, R., Meredith, J. E., Burton, C. R., Barten, D. M., Toyn, J. H., Roberts, S. B., Lentz, K. A., Houston, J. G., Zaczek, R., Albright, C. F., Decicco, C. P. & 2 others, Macor, J. E. & Olson, R. E., 10 Jun 2010, In : ACS MEDICINAL CHEMISTRY LETTERS. 1, 3, p. 120-124 5 p.

Research output: Contribution to journalArticle

119 Citations (Scopus)

Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

Rodrigeuz, A. L., Grier, M. D., Jones, C. K., Herman, E. J., Kane, A. S., Smith, R. L., Williams, R., Zhou, Y., Days, E. L., Blatt, T. N., Jadhav, S., Menion, U., Vinson, P. N., Rook, J. M., Stauffer, S. R., Niswender, C. M., Lindsley, C. W., Weaver, C. D. & Conn, P. J., Dec 2010, In : Molecular Pharmacology. 78, 6, p. 1105-1123 19 p.

Research output: Contribution to journalArticle

143 Citations (Scopus)

Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4

Williams, R., Zhou, Y., Niswender, C. M., Luo, Q., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., 16 Jun 2010, In : ACS chemical neuroscience. 1, 6, p. 411-419 9 p.

Research output: Contribution to journalArticle

40 Citations (Scopus)

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Engers, D. W., Gentry, P. R., Williams, R., Bolinger, J. D., Weaver, C. D., Menon, A., Conn, L., Lindsley, C. W., Niswender, C. M. & Hopkins, F., 01 Sep 2010, In : Bioorganic & Medicinal Chemistry Letters. 20, 17, p. 5175-5178 4 p.

Research output: Contribution to journalArticle

20 Citations (Scopus)
2009

A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning

Sheffler, D. J., Williams, R., Bridges, J., Xiang, J-J., Kane, A., Byun, N. E., Jadhav, S., Mock, M. M., Zheng, X., Lewis, C., Jones, C., Niswender, C. M., Weaver, C. D., Lindsley, C. W. & Conn, L., Aug 2009, In : Molecular Pharmacology. 76, 2, p. 356-368 13 p.

Research output: Contribution to journalArticle

81 Citations (Scopus)

Discovery and Development of a Potent and Highly Selective Small Molecule Muscarinic Acetylcholine Receptor Subtype I (mAChR 1 or M-1) Antagonist In Vitro and In Vivo Probe

Weaver, C. D., Sheffler, D. J., Lewis, L. M., Bridges, T. M., Williams, R., Nalywajko, N. T., Kennedy, J. P., Mulder, M. M., Jadhav, S., Aldrich, L. A., Jones, C. K., Marlo, J., Niswender, C. M., Mock, M. M., Zheng, F., Conn, P. J. & Lindsley, C. W., 2009, In : Current Topics In Medicinal Chemistry. 9, 13, p. 1217-1226 10 p.

Research output: Contribution to journalArticle

8 Citations (Scopus)

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Zhou, Y., Rodriguez, A. L., Williams, R., Weaver, C. D., Conn, P. J. & Lindsley, C. W., 15 Jun 2009, In : Bioorganic & Medicinal Chemistry Letters. 19(12), 12, p. 3209-3213 5 p.

Research output: Contribution to journalArticle

31 Citations (Scopus)

mGluR5 Positive Allosteric Modulators Facilitate both Hippocampal LTP and LTD and Enhance Spatial Learning

Ayala, J. E., Chen, Y., Banko, J. L., Sheffler, D. J., Williams, R., Telk, A. N., Watson, N., Xiang, Z., Zhang, Y., Jones, C. K., Lindsley, C. W., Olive, M. F. & Conn, P. J., Aug 2009, In : Neuropsychopharmacology. 34, 9, p. 2057-2071 15 p.

Research output: Contribution to journalArticle

154 Citations (Scopus)

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

Williams, R., Niswender, C. M., Luo, Q., Le, U., Conn, P. J. & Lindsley, C. W., 01 Feb 2009, In : Bioorganic & Medicinal Chemistry Letters. 19, 3, p. 962-966 5 p.

Research output: Contribution to journalArticle

40 Citations (Scopus)

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273.

Engers, D. W., Rodriguez, A. L., Williams, R., Hammond, A. S., Venable, D., Oluwatola, O., Sulikowski, G. A., Conn, P. J. & Lindsley, C. W., 17 Apr 2009, In : ChemMedChem. 4, 4, p. 505-511 7 p.

Research output: Contribution to journalArticle

37 Citations (Scopus)

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

Williams, R., Johnson, K. A., Gentry, P. R., Niswender, C. M., Weaver, C. D., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., 01 Sep 2009, In : Bioorganic & Medicinal Chemistry Letters. 19, 17, p. 4967-4970 4 p.

Research output: Contribution to journalArticle

23 Citations (Scopus)

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

Rodriguez, A. L., Zhou, Y., Williams, R., Weaver, C. D., Conn, P. J. & Lindsley, C. W., 01 Dec 2009, In : Bioorganic & Medicinal Chemistry Letters. 19, 23, p. 6502-6506 5 p.

Research output: Contribution to journalArticle

16 Citations (Scopus)
2008

Allosteric modulators of metapotropic glutamate receptor subtype 5 as a novel approach for treatment of CNS disorders

Conn, P. J., Rodriguez, A. L., Ayala, J. E., Jones, C. K., Barrett, R., Niswender, C. M., Weaver, C. D., Jadhav, S., Sheffler, D. J., Hammond, A. S., Williams, R., Sharma, S. & Lindsley, C. W., Sep 2008, In : Neuropharmacology. 55, p. 593-593 1 p.

Research output: Contribution to journalArticle

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

Shirey, J. K., Xiang, Z., Orton, D., Brady, A. E., Johnson, K. A., Williams, R., Ayala, J. E., Rodriguez, A. L., Wess, J., Weaver, C. D., Niswender, C. M. & Conn, P. J., Jan 2008, In : Nature Chemical Biology. 4, 1, p. 42-50 9 p.

Research output: Contribution to journalArticle

123 Citations (Scopus)

Design of potent GlyT1 inhibitors: In vitro and in vivo profiles

Bridges, J., Williams, R. & Lindsley, C. W., Dec 2008, In : Current opinion in molecular therapeutics. 10, 6, p. 591-601 11 p.

Research output: Contribution to journalArticle

44 Citations (Scopus)

mGlur5 positive allosteric modulators facilitate both LTP and LTD induction in the rat hippocampal CA1 region

Ayalaa, J. E., Chen, Y., Banko, J. L., Sheffler, D. J., Williams, R. & Conn, P. J., Sep 2008, In : Neuropharmacology. 55, p. 586-586 1 p.

Research output: Contribution to journalArticle

Novel allosteric modulators of metabotropic glutamate receptors subtypes 2 and 5 for the treatment of schizophrenia

Jones, C. K., Xiang, F., Jones, A., Byun, N. E., Hackler, E. A., Rodriguez, A. L., Ayala, J. E., Niswender, C. M., Jadhav, S., Sheffler, D. J., Hammond, A. S., Barret, R., Thompson, A., Williams, R., Gore, E., Weaver, C. D., Lindsley, C. W. & Conn, P. J., Sep 2008, In : Neuropharmacology. 55, p. 603-603 1 p.

Research output: Contribution to journalArticle

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

Bridges, T. M., Williams, R. & Lindsley, C. W., 01 Feb 2008, In : Bioorganic & Medicinal Chemistry Letters. 18(3), 3, p. 885-890 6 p.

Research output: Contribution to journalArticle

14 Citations (Scopus)
2006

Permissive antagonism induced by novel allosteric antagonists of metabotropic glutamate receptor 7

Niswender, C. M., Myers, K. A., Williams, R., Ayala, J. E., Luo, Q., Saleh, S., Jones, C. K., Orton, D., Weaver, C. D. & Conn, P. J., Dec 2006, In : Neuropsychopharmacology. 31, p. S127-S128 2 p.

Research output: Contribution to journalArticle

2002
207 Citations (Scopus)