skip to content

Department of Pharmacology

 

 

Ion Channels 

Yuan Y, Jaślan D, Rahman T......Yule DI, Grimm C, Patel S. Segregated cation flux by TPC2 biases Ca2+ signaling through lysosomes. Nature Communications 2022 ;13(1):4481. 

Patel S, Yuan Y, Chen C-C, Dawid J, Gunaratne G, Grimm C, Rahman T, Marchant JS. Electrophysiology of Endolysosomal Two-Pore Channels: A Current Account. Cells 2022; 15:10.3390/cells11152368 

Rahman T, Patel S. Rendezvous with PI(3,5)P2 - A rapalog gets caught opening TRPML1. Cell Calcium. 2022;105:102597. 

Patel S, Yuan Y, Gunaratne GS, Rahman T, Marchant JS. Activation of endo-lysosomal two-pore channels by NAADP and PI(3,5)P2. Five things to know. Cell Calcium. 2022;103:102543. 

Gökçe Y, Erkan O, Savaş K, Rahman T, Yaraş N. Pharmacological blockade of angiotensin II receptor restores diabetes-associated reduction of store operated Ca2+ entry in adult cardiomyocytes. Biochemical Biophysical Research Communications. 2022;610:56-60

Rossi AM, Riley AM, Dupont G, Rahman T, Potter BVL & Taylor CW. Quantal Ca2+ release mediated by very few IP3 receptors that rapidly inactivate allows graded responses to IP3. Cell Reports 2021; 5:109932. 

Li Z, King T, Ayong L, Asady B, Cai X, Rahman T, Vella S, Coppens I, Patel S. & Moreno S. A plastid Two-Pore Channel essential for inter-organelle communication and growth of Toxoplasma gondii, Nature Communication 2021; 12(1): 5802. 

Patel S, Gunaratne GS, Marchant JS, Biggin PC, Rahman T. NAADP receptors: A one-two. Cell Calcium. 2021 ;100:102478. 

Rahman S, Rahman T. Unveiling some FDA-approved drugs as inhibitors of the store-operated Ca2+ entry pathway. Scientific Reports, 2017. doi:10.1038/s41598-017-13343-x.

Penny CJ, Rahman T, Sula A, Miles AJ, Wallace BA, Patel S. Isolated pores dissected from human two-pore channel 2 are functional. Scientific Report. 2016; 6 :38426

Patel S, Penny CJ, Rahman T. Two-pore Channels Enter the Atomic Era: Structure of Plant TPC Revealed. Trends in Biochemical Sciences. 2016. pii: S0968-0004(16)30025-1.

Penny CJ, Vassileva K, Jha A, Yuan Y, Chee X, Yates E, Mazzon M, Kilpatrick BS, Muallem S, Marsh M, Rahman T, Patel S. Mining of Ebola virus entry inhibitors identifies approved drugs as two-pore channel pore blockers. Biochimia Biophysica Acta Mol Cell Res. 2018. pii: S0167-4889(18)30499-3. 

Dulai JS., Smith ESJ & Rahman T. Acid-Sensing Ion Channel 3: An Analgesic Target Channels. Channels 2021, 15(1):94-127. 

Callejo G, Pattison LA, Greenhalgh JC, Chakrabarti S, Andreopoulou E, Hockley JRF, Smith ESJ, Rahman T. In silico screening of GMQ-like compounds reveals guanabenz and sephin1 as new allosteric modulators of acid-sensing ion channel 3. Biochemical Pharmacology. 2020, 3:113834. 

Journigan VB, Feng Z, Rahman S...Van Horn WD, Ferrer-Montiel A, Xie XQ, Rahman T. Structure-based design of novel biphenyl amide antagonists of human Transient Receptor Potential Cation Channel Subfamily M Member 8 channels (TRPM8) with potential implications in the treatment of sensory neuropathies. ACS Chemical Neuroscience 2020. 11(3):268-290. 

Chandran A., Chee X, Prole DL., Rahman T. Exploration of inositol 1,4,5-trisphosphate (IP3) regulated dynamics of N-terminal domain of IP3 receptor reveals early phase molecular events during receptor activation. Scientific Reports, 9:2454  

Churamani D, Hooper R, Rahman T, Brailoiu E, Patel S (2013) The N-terminal region of two-pore channel 1 regulates trafficking and activation by NAADP. Biochemical Journal 453: 147-151

Li C, Enomoto M, Rossi AM, Seo MD, Rahman T, Stathopulos PB, Taylor CW, Ikura M, Ames JB (2013) CaBP1, a neuronal Ca2+ sensor protein, inhibits inositol trisphosphate receptors by clamping intersubunit interactions. Proc Natl Acad Sci U S A 110: 8507-8512

Saleem H, Tovey SC, Rahman T, Riley AM, Potter BV, Taylor CW (2013) Stimulation of inositol 1,4,5-trisphosphate (IP3) receptor subtypes by analogues of IP3PLoS One 8: e54877

Sun Y, Rossi AM, Rahman T, Taylor CW (2013) Activation of IP3 receptors requires an endogenous 1-8-14 calmodulin-binding motif. Biochemical Journal 449: 39-49

Rahman T (2012) Dynamic clustering of IP3 receptors by IP3Biochem Soc Trans 40: 325-330

Rossi AM, Tovey SC, Rahman T, Prole DL, Taylor CW (2012) Analysis of IP3 receptors in and out of cells. Biochim Biophys Acta 1820: 1214-1227

Taylor CW, Tovey SC, Rossi AM, Lopez Sanjurjo CI, Prole DL, Rahman T (2014). Structural organization of signalling to and from IP3receptors. Biochemical Society Transduction 2014;42:63-70.

Rahman T, Cai X, Brailoiu GC, Abood ME, Brailoiu E, Patel S. Two-pore channels provide insight into the evolution of voltage-gated Ca2+ and Na+ channels. Science Signalling 2014; 7(352):ra109.

Rahman T, Smith ES (2014). In silico assessment of interaction of sea anemone toxin APETx2 and acid sensing ion channel 3. Biochem Biophys Res Commun. 2014; 450(1):384-9.

Patel S, Ramakrishnan L, Rahman T, Hamdoun A, Marchant JS, Taylor CW, Brailoiu E (2011) The endo-lysosomal system as an NAADP-sensitive acidic Ca2+ store: role for the two-pore channels. Cell Calcium 50: 157-167

Brailoiu E, Rahman T, Churamani D, Prole DL, Brailoiu GC, Hooper R, Taylor CW, Patel S (2010) An NAADP-gated two-pore channel targeted to the plasma membrane uncouples triggering from amplifying Ca2+ signals. J Biol Chem 285: 38511-38516

Rahman T & Taylor CW (2010) Nuclear patch-clamp recording from inositol 1,4,5-trisphosphate receptors. Methods Cell Biol 99: 199-224

Ding Z, Rossi AM, Riley AM, Rahman T, Potter BV, Taylor CW (2010) Binding of inositol 1,4,5-trisphosphate (IP3) and adenophostin A to the N-terminal region of the IP3 receptor: thermodynamic analysis using fluorescence polarization with a novel IP3 receptor ligand. Mol Pharmacol 77: 995-1004

Tovey SC, Dedos SG, Rahman T, Taylor EJ, Pantazaka E, Taylor CW (2010) Regulation of inositol 1,4,5-trisphosphate receptors by cAMP independent of cAMP-dependent protein kinase. J Biol Chem 285: 12979-12989

Taufiq-Ur-Rahman, Skupin A, Falcke M, Taylor CW (2009) Clustering of InsP3 receptors by InsP3 retunes their regulation by InsP3 and Ca2+Nature 458: 655-659

Rossi AM, Riley AM, Tovey SC, Rahman T, Dellis O, Taylor EJ, Veresov VG, Potter BV, Taylor CW (2009) Synthetic partial agonists reveal key steps in IP3 receptor activation. Nat Chem Biol 5: 631-639

Rahman T & Taylor CW (2009) Dynamic regulation of IP3 receptor clustering and activity by IP3Channels (Austin) 3: 226-232

Taylor CW, Prole DL, Rahman T (2009) Ca2+ channels on the move. Biochemistry 48: 12062-12080

Taylor CW, Rahman T, Tovey SC, Dedos SG, Taylor EJ, Velamakanni S (2009) IP3 receptors: some lessons from DT40 cells. Immunol Rev 231: 23-44

Taylor CW, Taufiq-Ur-Rahman, Pantazaka E (2009) Targeting and clustering of IP3 receptors: key determinants of spatially organized Ca2+ signals. Chaos 19: 037102

Dellis O, Dedos SG, Tovey SC, Taufiq-Ur-Rahman, Dubel SJ, Taylor CW (2006) Ca2+ entry through plasma membrane IP3 receptors. Science 313: 229-233

 

Signalling/Pharmacology related

Francis LRA, Millington-Burgess SL, Rahman T, Harper MT. Q94 is not a selective modulator of proteinase-activated receptor 1 (PAR1) in platelets. Platelets. 2022:1-6. 

Shakur R, Ochoa JP, Robinson AJ, Niroula A, Chandran A, Rahman T, Vihinen M, Monserrat L. Prognostic implications of troponin T variations in inherited cardiomyopathies using systems biology. NPJ Genome Medicine 2021; 6(1):47. 

R5421 is not a selective inhibitor of platelet phospholipid scramblase activity. Burgess S, Arkadiusz B, Rahman T, Harper M. British Journal of Pharmacology 2020 (doi: 10.1111/bph.15152)

Safitri D, Harris M, Potter H, Yan Yeung H, Winfield I, Kopanitsa L, Svensson F, Rahman T, Harper MT, Bailey D, Ladds G. Elevated intracellular cAMP concentration mediates growth suppression in glioma cells. Biochemical Pharmacology. 2020:113823. 

 

Rational/Computational Drug Design, Molecular Modelling related

Chee Wezen X, Chandran A, Eapen RS, Waters E, Bricio-Moreno L, Tosi T, Dolan S, Millership C, Kadioglu A, Gründling A, Itzhaki LS, Welch M, Rahman T. Structure-Based Discovery of Lipoteichoic Acid Synthase Inhibitors. Journal of Chemical Information and Modelling 2022; 62(10):2586-2599. 

Ha CHX, Lee NK, Rahman T, Hwang SS, Yam WK, Chee XW. Repurposing FDA-approved drugs as HIV-1 integrase inhibitors: an in silico investigation. Journal of Biomolecular Structure and Dynamics 2022:1-14. 

Gunasinghe J, Hwang SS, Yam WK, Rahman T, Wezen XC. In-silico discovery of inhibitors against human papillomavirus E1 protein. Journal of Biomolecular Structure and Dynamics. 2022, 1-14. 

Bayazeid O, Rahman T. Correlation Analysis of Target Selectivity and Side Effects of FDA-Approved Kinase Inhibitors. ChemistrySelect 2021. 

Ghislat G, Rahman T & Ballester PJ. Recent progress on the prospective application of machine learning to structure-based virtual screening. Current Opinion in Chemical Biology 2021;65:28-34. 

Hajbabaie R, Harper MT & Rahman T. Establishing an Analogue Based in Silico Pipeline in the Pursuit of Novel Inhibitory Scaffolds against the SARS Coronavirus 2 Papain-Like Protease. Molecules 2021, 26(4), 1134. 

Augustin TL, Hajbabaie R, Harper MT & Rahman T . Novel Small Molecule Scaffolds as Candidates Against the SARS Coronavirus 2 Main Protease: a Fragment-Guided In Silico Approach. Molecules 2020, 25(23), 5501. 

Ghislat G, Rahman T & Ballester PJ. Identification and validation of Carbonic Anhydrase II as the first target of the anti-inflammatory drug Actarit. Biomolecules, 10(11), 1570. 

Maunders EA., Triniman RC., Rahman T. & Welch M. Global reprogramming of virulence and antibiotic resistance in Pseudomonas aeruginosa by a single nucleotide polymorphism in the elongation factor-encoding gene, fusA1Journal of Biological Chemistry. 2020. 295(48):16411-16426

Greenhalgh JC, Chandran A, Harper MT, Ladds G and Rahman T. Proposed model of the Dictyostelium cAMP receptors bound to cAMP. Journal of Molecular Graphics and Modelling 2020 

Zarkan A, Matuszewska A.....Greenhalgh J, Duboff J, Rahman T, Summers D. Inhibition of Indole Production Increases the Activity of Quinolone Antibiotics against E. coli Persisters. Scientific Reports. 2020 (doi: 10.1038/s41598-020-68693-w)

Abdelhamid Y. Brear P., Greenhalgh J., Chee X., Rahman, T & Welch M. Evolutionary plasticity in the allosteric regulator binding site of pyruvate kinase isoform PykA from Pseudomonas aeruginosaJournal of Biological Chemistry. 2019;294(42):15505-15516. 

McVey AC, Medarametla P, Chee X, Bartlett S, Poso A, Spring DR, Rahman T, Welch M. Structural and Functional Characterization of Malate Synthase G from Opportunistic Pathogen Pseudomonas aeruginosaBiochemistry. 2017. 

Wang Y, Mowla R, Guo L, Ogunniyi AD, Rahman T, De Barros Lopes MA, Ma S, Venter H. Evaluation of a series of 2-napthamide derivatives as inhibitors of the drug efflux pump AcrB for the reversal of antimicrobial resistance. Bioorganic and Medicinal Chemistry Letters; 27(4):733-739

Chattopadhyay A, O'Connor CJ, Zhang F, Galvagnion C, Galloway WR, Tan YS, Stokes JE, Rahman T, Verma C, Spring DR, Itzhaki LS. Discovery of a small-molecule binder of the oncoprotein gankyrin that modulates gankyrin activity in the cell. Scientific Reports. 2016;6:23732.

Ohene-Agyei T, Mowla R, Rahman T, Venter H. Phytochemicals increase the antibacterial activity of antibiotics by acting on a drug efflux pump. Microbiologyopen. 2014

Musa MA, Cooperwood JS, Khan MO, Rahman T (2011) In-vitro antiproliferative activity of benzopyranone derivatives in comparison with standard chemotherapeutic drugs. Arch Pharm (Weinheim) 344: 102-110

Rahman T & Rahmatullah M (2010) Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases. Bioorg Med Chem Lett 20: 537-540