Research Publications
PUBLICATIONS
PUBLICATIONS
- Firdous F, Riaz S, Furqan M, Fozail S, Fatima K, Pohl OG, Doleschall NJ, Myant KB, Kahfi J, Emwas AH, Jaremko M, Chotana, GA, Saleem RSZ, Faisal A (2023) Design, Synthesis, and Biological Evaluation of SSE1806, a Microtubule Destabilizer That Overcomes Multidrug Resistance ACS Med. Chem. Lett. https://doi.org/10.1021/acsmedchemlett.3c00258
- Saleem, HN, Kousar S, Jiskani H, Sohail I, Faisal A, Saeed M (2023) Repurposing of investigational cancer drugs: Early phase discovery of dengue virus NS2B/NS3 protease inhibitors. Arch Pharm 15 August 2023 https://doi.org/10.1002/ardp.202300292
Farhan A, Hassan G, Ali SHL, Yousaf Z, Shafique K, Faisal A, Younis BB, Mirza S (2023) Spontaneous NETosis in diabetes: A role of hyperglycemia mediated ROS and autophagy Frontiers in Medicine 2023; 10: 1076690.
Ashraf N, Asari A, Yousaf N, Ahmad M, Ahmed M, Faisal A, Saleem M and Muddassar M (2022) Combined 3D-QSAR, molecular docking and dynamics simulations studies to model and design TTK inhibitors. Front. Chem., 02 November 2022 Sec. Medicinal and Pharmaceutical Chemistry
Firdous F, Raza HG, Chotana GA, Choudhary MI, Faisal A, Saleem RSZ (2022) Centrosome Clustering & Chemotherapy. Mini-Reviews in Medicinal Chemistry 19 September, 2022
Ahmed K, Chotana GA, Faisal A, Saleem RZS (2022) Chemical Synthesis of Selenium-containing Peptides. Mini-Reviews in Medicinal Chemistry 26 Aug 2022
Furqan M, Fayyaz A, Firdous , Raza H, Bilal A, Saleem RSZ, Hussan SS,Wang D, Youssef FS, Al Musayeib NM, Ashour ML, Hussain H and Faisal A. (2022) Identification and Characterization of Natural and Semisynthetic Quinones as Aurora Kinase Inhibitors. Journal of Natural Products 2022, 85, 6, 1503–1513
Farrukh UB, Bilal A, Zahid H, Iqbal M, Manzoor S, Firdous F, Furqan M, Azeem M, Emwas AH, Alazmi M, Gao X, Saleem RSZ, Faisal A (2022) Synthesis and Evaluation of Novel Carboxamides Capable of Causing Centrosome Declustering and Apoptosis in Breast Cancer Cells. ChemistrySelect 2022, 7, e202104218 (1 of 7)
Ahmed K, Ashraf D, Chotana GA, Faisal A, Khan KM, Saleem RSZ (2022) Selenium-containing Peptides and their Biological Applications Current Medicinal Chemistry https://doi.org/10.2174/0929867329666220214104010
- Tariq MU, Furqan M, Parveen H, Ullah R, Muddassar M, Saleem RSZ, Bavetsias V, Linardopoulos S and Faisal A* (2021) CCT245718, a dual FLT3/Aurora A inhibitor overcomes D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells. British Journal of Cancer 125, pages 966–974 (2021)
Gondal MN, Butt RN, Shah OS, Sultan MU, Mustafa G, Nasir Z, Hussain R, Khawar H, Qazi R, Tariq M, Faisal A and Chaudhary SU. (2021) A personalized therapeutics approach using an in silico Drosophila Patient Model reveals optimal chemo-and targeted therapy combinations for colorectal cancer. Frontiers in Oncology. 2021; 11: 692592.
Amina SJ, Iqbal M, Faisal A, Shoaib Z, Niazi MBK, Ahmed NM, Khalid N, Janjua HA (2021) Synthesis of Diosgenin conjugated gold nanoparticles using algal extract of Dictyosphaerium sp. and in-vitro Application of their antiproliferative activities. Materials Today Communications Volume 27, June 2021, 102360
Rai N, Madni A, Faisal A, Jamshaid T, Khan MI, Khan MM, Parveen F (2021) Glyceryl Monostearate Based Solid Lipid Nanoparticles for Controlled Delivery of Docetaxel. Current Drug Delivery, 03 Feb 2021
Malik HS, Bilal A, Ullah R, Iqbal M, Khan S, Ahmed I, Krohn K, Saleem RSZ, Hussain H, Faisal A (2020) Natural and Semisynthetic Chalcones as Dual FLT3 and Microtubule Polymerization Inhibitors J. Nat. Prod. September 25, 2020
Ullah R, Naz A, Akram HS, Ullah Z, Tariq M, Mithani A and Faisal A (2020) Transcriptomic analysis reveals differential gene expression, alternative splicing and novel exons during mouse trophoblast stem cell differentiation. Stem Cell Research and Therapy. 11, Article number: 342 (2020)
M Abid, M Naveed, I Azeem, A Faisal, MF Nazar, B Yameen (2020) Colon Specific Enzyme Responsive Oligoester Crosslinked Dextran Nanoparticles for Controlled Release of 5-Fluorouracil. International Journal of Pharmaceutics https://doi.org/10.1016/j.ijpharm.2020.119605
Zahra R, Furqan M, Ullah R, Mithani A, Saleem RSZ and Faisal A (2020) A cell-based high-throughput screen identifies inhibitors that overcome P-glycoprotein (Pgp)-mediated multidrug resistance. PLOS One. doi.org/10.1371/journal.pone.0233993
Moore A, Faisal A, Mak G, Miraki-Moud F, Bavetsis V, Valenti M, Box G, Hallworth A, Brandon AH, Xavier C, Stronge R, Pearson A, Blagg J, Raynaud F, Chopra R, Eccles S, Taussig D ad Linaropoulos S (2020) Quizartinib-resistant FLT3-ITD acute myeloid leukaemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736. Blood Advances Blood Adv (2020) 4 (7): 1478–1491.
- Furqan M, Huma Z, Ashfaq Z, Nasir A, Ullah R, Bilal A, Iqbal M, Khalid MH, Hussain I, Faisal A. (2019) Identification and evaluation of novel drug combinations of Aurora kinase inhibitor CCT137690 for enhanced efficacy in oral cancer cells. Cell Cycle 2019 Sep;18(18):2281-2292
- Anderhub SJ*, Mak GWY*, Gurden MD*, Faisal A*, Drosopoulos K*, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, van Montfort RL, Raynaud FI, Blagg J, Hoelder S, Eccles SA and Linardopoulos S. (2019) High proliferation rate and a compromised spindle assembly checkpoint confers sensitivity to the MPS1 inhibitor BOS172722 in triple negative breast cancers. Molecular Cancer Therapeutics; 2019;18:1696–707 * = equal contribution
- Sohail M, Ashfaq B, Azeem I, Faisal A, Doğan SY, Wang J, Duran H and Yameen B (2019) A facile and versatile route to functional poly(propylene) surfaces via UV-curable coatings Reactive and Functional Polymers Volume 144, November 2019, 104366.
- Amjad M, Iqbal M, Faisal A, Junjua AM, Hussain I, Hussain SZ, Ghramhe HA, Khan HA and Janjua Ha. (2019) Hydrothermal synthesis of carbon nanodots from bovine gelatin and PHM3 microalgae strain for anticancer and bioimaging applications. Nanoscale Adv 2019 DOI: 10.1039/C9NA00164F
- Wood F, Shepherd S, Hayes A, Liu M, Grira K, Mok Y, Linardopoulos S, Bavetsias V, Atrash B, Faisal A, Blagg J, Raynaud FI. (2019) Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species. Eur J Pharm Sci. 2019 Apr 3. pii: S0928-0987(19)30142-3. doi: 10.1016/j.ejps.2019.04.004. PubMed PMID: 30953752.
- Riaz S, Iqbal M, Ullah R, Zahra R, Chotana GA, Faisal A*, Saleem RSZ*. (2019) Synthesis and evaluation of novel α-substituted chalcones with potent anti-cancer activities and ability to overcome multidrug resistance. Bioorganic Chemistry Volume 87, June 2019, Pages 123-135 * Corresponding Authors
- Batool S, Ullah S, Tabassum S, Bilal A, Faisal A, Saleem RSZ, Ahmad MS. Effect of Extraction Methodologies on Antioxidant Potential and Synergistic Anticancer Behavior of Leaf Extract of Polygonum amplexicaule Against HCT-116 Cells (2019) Iranian Journal of Science and Technology, Transactions A: Science June 2019, Volume 43, Issue 3, pp 709–714
- Riaz M, Altaf M, Faisal A, Shekheli MA, Miana GA, Khan MQ, Shah MA, Ilyas SZ, Khan AA. (2018) Biogenic Synthesis of AgNPs with Saussurea lappa C.B. Clarke and Studies on Their Biochemical Properties. J Nanosci Nanotechnol. 2018 Dec 1;18(12):8392-8398.
- Woodward H, Innocenti P, Cheung K, Hayes A, Roberts J, Henley A, Faisal A, Mak G, Box G, Westwood I, Cronin N, Carter M, Valenti M, De Haven Brandon A, O’Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort R, Raynaud F, Eccles S, Linardopoulos S, Blagg J, Hoelder S. (2018) Introduction of a methyl group curbs metabolism of pyrido[3,4-d]pyrimidine monopolar spindle 1 (MPS1) inhibitors and enables the discovery of the Phase 1 clinical candidate N2-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722). J Med Chem. 2018 Sep 10. doi: 10.1021/acs.jmedchem.8b00690. [Epub ahead of print]
- Ullah R, Dar S, Ahmad T, de Renty C, Usman M, DePamphilis ML, Faisal A, Hussan SS, Ullah Z. (2018). CDK1 inhibition facilitates formation of syncytiotrophoblasts and expression of human Chorionic Gonadotropin. Placenta 2018 2018 Jun;66:57-64. doi: 10.1016/j.placenta.2018.05.003.
- Shah OS, Chaudhary FA, Awan HA, Fatima F, Arshad A, Bibi A, Ahmed M, Hameed H, Furqan F, Khalid S, Faisal A, Ullah Chaudhary SU. (2018) ATLANTIS – Attractor Landscape Analysis Toolbox for Cell Fate Discovery and Reprogramming. Scientific Reports 2018 Feb 23;8(1):3554.
- Manzoor S, Bilal A, Khan S, Ullah R Iftikhar S, Emwas A, Alazmi M, Gao, X, Jawaid A, Saleem RS* and Faisal A* (2018) Identification and characterization of SSE15206, a microtubule depolymerizing agent that overcomes multidrug resistance. Scientific Reports 2018 Feb 19;8(1):3305. *Corresponding Authors
- Arany I, Hall S, Faisal A, and Dixit M (2017) Nicotine Exposure Augments Renal Toxicity of 5-aza-cytidine through p66shc: Prevention by Resveratrol. Anticancer Research 37: 4075-4079 (2017)
- Iftikhar S, Khan S, Bilal A, Manzoor S, Abdullah M, Emwas A, Sioud S, Gao X, Chotana GA, Faisal A*, Saleem RS* (2017) Synthesis and evaluation of modified chalcone based p53 stabilizing agents. Bioorganic & Medicinal Chemistry Letters 2017 Sep 1;27(17):4101-4106 * Corresponding Authors
- Faisal A, Mak G, Gurden M, Xavier C, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box B, Valenti M, Brandon A, O’Fee L, Schmitt J, Woodward H, Burke R, vanMontfort R, Blagg J, Raynaud F, Eccles S, Hoelder S and Linardopoulos S. (2017) Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition versus therapeutic efficacy. British Journal of Cancer Mar 23. 2017 doi: 10.1038/bjc.2017.75. [Epub ahead of print] IF: 5.569
- Riaz M, Bilal A, Ali MS, Fatima I, Faisal A, Sherkheli MA, Asghar A. Natural products from Cuscuta reflexa Roxb. with antiproliferation activities in HCT116 colorectal cell lines. Nat Prod Res. 2016 Jul 22:1-5. [Epub ahead of print] PubMed PMID: 27450325.
- Gurden MD, Anderhub SJ, Faisal A, Linardopoulos S. Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis. Oncotarget. 2016 Jul 18. doi: 10.18632/oncotarget.10657. [Epub ahead of print] PubMed PMID: 27437774.
- Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak G4W, Box G, Valenti M, De Haven Brandon A, O’Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S. Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7. PubMed PMID: 27055065.
- Bavetsias V, Pérez-Fuertes Y, McIntyre PJ, Atrash B, Kosmopoulou M, O’Fee L, Burke R, Sun C, Faisal A, Bush K, Avery S, Henley A, Raynaud FI, Linardopoulos S, Bayliss R, Blagg J. 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4203-9. doi: 10.1016/j.bmcl.2015.08.003. Epub 2015 Aug 6. PubMed PMID: 26296477; PubMed Central PMCID: PMC4577729.Free full text
- Gurden MD, Westwood IM, Faisal A, Naud S, Cheung KM, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Van Montfort RL, Linardopoulos S. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54. doi: 10.1158/0008-5472.CAN-14-3272. Epub 2015 Jul 22. PubMed PMID: 26202014.
- Cheeseman MD, Faisal A, Rayter S, Barbeau OR, Kalusa A, Westlake M, Burke R, Swan M, van Montfort R, Linardopoulos S, Jones K. Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3469-74. doi: 10.1016/j.bmcl.2014.05.067. Epub 2014 May 29. PubMed PMID: 24953599.
- Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, Valenti M, de Haven Brandon A, Henley A, Baker R, McAndrew C, Matijssen B, Burke R, Hoelder S, Eccles SA, Raynaud FI, Linardopoulos S, van Montfort RL, Blagg J. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65. doi: 10.1021/jm401395s. Epub 2013 Dec 2. PubMed PMID: 24256217; PubMed Central PMCID: PMC3873811.Free full text
- Bavetsias V, Faisal A, Crumpler S, Brown N, Kosmopoulou M, Joshi A, Atrash B, Pérez-Fuertes Y, Schmitt JA, Boxall KJ, Burke R, Sun C, Avery S, Bush K, Henley A, Raynaud FI, Workman P, Bayliss R, Linardopoulos S, Blagg J. Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells. J Med Chem. 2013 Nov 27;56(22):9122-35. doi: 10.1021/jm401115g. Epub 2013 Nov 6. PubMed PMID: 24195668; PubMed Central PMCID: PMC3848336.Free full text
- Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, Raynaud FI, Workman P, Eccles SA, Bayliss R, Linardopoulos S, Blagg J.Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34. doi: 10.1021/jm300952s. Epub 2012 Oct 8. PubMed PMID: 23043539; PubMed Central PMCID: PMC3483018. Free full text
- Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S. Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52. Epub 2012 Feb 22. PubMed PMID: 22354205; PubMed Central PMCID: PMC3523391.Free full text
- Faisal A, Vaughan L, Bavetsias V, Sun C, Atrash B, Avery S, Jamin Y, Robinson SP, Workman P, Blagg J, Raynaud FI, Eccles SA, Chesler L, Linardopoulos S. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23. doi: 10.1158/1535-7163.MCT-11-0333. Epub 2011 Sep 1. PubMed PMID: 21885865; PubMed Central PMCID: PMC4298164. Free full text
- Clark JS, Faisal A, Baliga R, Nagamine Y, Arany I. Cisplatin induces apoptosis through the ERK-p66shc pathway in renal proximal tubule cells. Cancer Lett. 2010 Nov 28;297(2):165-70. doi: 10.1016/j.canlet.2010.05.007. Epub 2010 Jun 12. PubMed PMID: 20547441.
- Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V. Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells. Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21. PubMed PMID: 20833547.
- Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j. PubMed PMID: 20565112.
- Arany I, Faisal A, Clark JS, Vera T, Baliga R, Nagamine Y. p66SHC-mediated mitochondrial dysfunction in renal proximal tubule cells during oxidative injury. Am J Physiol Renal Physiol. 2010 May;298(5):F1214-21. doi: 10.1152/ajprenal.00639.2009. Epub 2010 Jan 6. PubMed PMID: 20053790.
- Bibby RA, Tang C, Faisal A, Drosopoulos K, Lubbe S, Houlston R, Bayliss R, Linardopoulos S. A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2. J Biol Chem. 2009 Nov 27;284(48):33177-84. doi: 10.1074/jbc.M109.032722. Epub 2009 Oct 2. PubMed PMID: 19801554; PubMed Central PMCID: PMC2785160.Free full text
- Saurin AT, Durgan J, Cameron AJ, Faisal A, Marber MS, Parker PJ. The regulated assembly of a PKCepsilon complex controls the completion of cytokinesis. Nat Cell Biol. 2008 Aug;10(8):891-901. doi: 10.1038/ncb1749. Epub 2008 Jul 6. PubMed PMID: 18604201.
- Faisal A, Saurin A, Gregory B, Foxwell B, Parker PJ. The scaffold MyD88 acts to couple protein kinase Cepsilon to Toll-like receptors. J Biol Chem. 2008 Jul 4;283(27):18591-600. doi: 10.1074/jbc.M710330200. Epub 2008 May 5. PubMed PMID: 18458086.
- Arany I, Faisal A, Nagamine Y, Safirstein RL. p66shc inhibits pro-survival epidermal growth factor receptor/ERK signaling during severe oxidative stress in mouse renal proximal tubule cells. J Biol Chem. 2008 Mar 7;283(10):6110-7. doi: 10.1074/jbc.M708799200. Epub 2008 Jan 3. PubMed PMID: 18174162.
- Cameron AJ, De Rycker M, Calleja V, Alcor D, Kjaer S, Kostelecky B, Saurin A, Faisal A, Laguerre M, Hemmings BA, McDonald N, Larijani B, Parker PJ. Protein kinases, from B to C. Biochem Soc Trans. 2007 Nov;35(Pt 5):1013-7. Review. PubMed PMID: 17956266.
- Kleiner S, Faisal A, Nagamine Y. Induction of uPA gene expression by the blockage of E-cadherin via Src- and Shc-dependent Erk signaling. FEBS J. 2007 Jan;274(1):227-40. PubMed PMID: 17222183.
- Tiberi L, Faisal A, Rossi M, Di Tella L, Franceschi C, Salvioli S. p66(Shc) gene has a pro-apoptotic role in human cell lines and it is activated by a p53-independent pathway. Biochem Biophys Res Commun. 2006 Apr 7;342(2):503-8. Epub 2006 Feb 9. PubMed PMID: 16487929.
- Faisal A, Kleiner S, Nagamine Y. Non-redundant role of Shc in Erk activation by cytoskeletal reorganization. J Biol Chem. 2004 Jan 30;279(5):3202-11. Epub 2003 Oct 23. PubMed PMID: 14576154.
- Faisal A, el-Shemerly M, Hess D, Nagamine Y. Serine/threonine phosphorylation of ShcA. Regulation of protein-tyrosine phosphatase-pest binding and involvement in insulin signaling. J Biol Chem. 2002 Aug 16;277(33):30144-52. Epub 2002 Jun 6. PubMed PMID: 12052829.
- 28. Kisielow M, Kleiner S, Nagasawa M, Faisal A, Nagamine Y. Isoform-specific knockdown and expression of adaptor protein ShcA using small interfering RNA. Biochem J. 2002 Apr 1;363(Pt 1):1-5. PubMed PMID: 11903040; PubMed Central PMCID: PMC1222444.Free full text