Academic literature on the topic 'Optimisation hit-To-Lead'
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Journal articles on the topic "Optimisation hit-To-Lead":
Padalino, Gilda, Nelly El-Sakkary, Lawrence J. Liu, Chenxi Liu, Danielle S. G. Harte, Rachel E. Barnes, Edward Sayers, et al. "Anti-schistosomal activities of quinoxaline-containing compounds: From hit identification to lead optimisation." European Journal of Medicinal Chemistry 226 (December 2021): 113823. http://dx.doi.org/10.1016/j.ejmech.2021.113823.
El Bakali, Jamal, Lucie Maingot, Julie Dumont, Helene Host, Akila Hocine, Nicolas Cousaert, Sandrine Dassonneville, Florence Leroux, Benoit Deprez, and Rebecca Deprez-Poulain. "Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation." MedChemComm 3, no. 4 (2012): 469. http://dx.doi.org/10.1039/c2md00287f.
Zaidi, Norburhanuddin Johari, Adib Afandi Abdullah, Choon Han Heh, Chun-Hung Lin, Rozana Othman, and Abdullah Al Hadi Ahmad Fuaad. "Hit-to-Lead Short Peptides against Dengue Type 2 Envelope Protein: Computational and Experimental Investigations." Molecules 27, no. 10 (May 18, 2022): 3233. http://dx.doi.org/10.3390/molecules27103233.
Bobrovs, Raitis, Jekaterina Bolsakova, Jhon Alexander Rodriguez Buitrago, Larisa Varaceva, Marija Skvorcova, Iveta Kanepe, Anastasija Rudnickiha, Emilio Parisini, and Aigars Jirgensons. "Structure-based identification of salicylic acid derivatives as malarial threonyl tRNA-synthetase inhibitors." PLOS ONE 19, no. 4 (April 1, 2024): e0296995. http://dx.doi.org/10.1371/journal.pone.0296995.
Mostarda, Serena, Tugçe Gür Maz, Alessandro Piccinno, Bruno Cerra, and Erden Banoglu. "Optimisation by Design of Experiment of Benzimidazol-2-One Synthesis under Flow Conditions." Molecules 24, no. 13 (July 3, 2019): 2447. http://dx.doi.org/10.3390/molecules24132447.
Taki, Aya C., Joseph J. Byrne, Tao Wang, Brad E. Sleebs, Nghi Nguyen, Ross S. Hall, Pasi K. Korhonen, et al. "High-Throughput Phenotypic Assay to Screen for Anthelmintic Activity on Haemonchus contortus." Pharmaceuticals 14, no. 7 (June 26, 2021): 616. http://dx.doi.org/10.3390/ph14070616.
Osborne, James, Stanislava Panova, Magdalini Rapti, Tatsuya Urushima, and Harren Jhoti. "Fragments: where are we now?" Biochemical Society Transactions 48, no. 1 (January 27, 2020): 271–80. http://dx.doi.org/10.1042/bst20190694.
Kandil, Sahar B., Samuel R. Jones, Sonia Smith, Stephen E. Hiscox, and Andrew D. Westwell. "Structure-Based Virtual Screening, Synthesis and Biological Evaluation of Potential FAK-FAT Domain Inhibitors for Treatment of Metastatic Cancer." Molecules 25, no. 15 (July 31, 2020): 3488. http://dx.doi.org/10.3390/molecules25153488.
Richardson, Caroline J., Mladen Vincovic, Charlotte East, Nicola Wallis, George Ward, and Andrew Woodhead. "Abstract A142: Fragment based discovery of inhibitors of the eIF4E:eIF4G interaction." Molecular Cancer Therapeutics 22, no. 12_Supplement (December 1, 2023): A142. http://dx.doi.org/10.1158/1535-7163.targ-23-a142.
Workman, Paul. "Abstract IA014: From targeted phenotypic screen to NXP800: A clinical stage activator of the integrated stress response for the treatment of ARID1A-mutated ovarian carcinoma." Molecular Cancer Therapeutics 22, no. 12_Supplement (December 1, 2023): IA014. http://dx.doi.org/10.1158/1535-7163.targ-23-ia014.
Dissertations / Theses on the topic "Optimisation hit-To-Lead":
Quevedo, Camilo E. "Design and synthesis of Quinazolinone-based libraries for inhibitation of Kinase activity and hit-to-lead optimisation of Wnt pathway inhibitors." Thesis, Institute of Cancer Research (University Of London), 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.510367.
Borzakian, Sibyline. "Identification et développement chimique d'inducteurs de protéines immunorégulatrices (SLPI et IL-10) à visée thérapeutique." Electronic Thesis or Diss., université Paris-Saclay, 2024. http://www.theses.fr/2024UPASF012.
The work carried out during this thesis has been divided into three distincts parts, all relating to the developpement of compounds for therapeutic use. The first part of this manuscript is devoted to the identification of inducers of Secretory Leucocyte Protease Inhibitor (SLPI), a protein mainly produced by immune and epithelial cells, with numerous promising biological properties. A phenotypic screening was conducted using two academic chemical libraries, leading to the identification of 5 hits able of inducing SLPI production by B cells. This work paved the way for potential therapeutic applications of these compounds, particularly in the development of antibiotic or anti-inflammatory treatments. The second part of this manuscript is dedicated to identifying a pharmacophore for inducers of Interleukin-10 (IL-10), a cytokine produced by immune cells, whose main role is the regulation of immunity. Prior to this thesis, a phenotypic screening was conducted to identifiy inducers of IL-10 production by B cells for use in cell therapy to reduce symptoms of multiple sclerosis. This thesis work involved hit-to-lead optimization of the most promising compound to identify a pharmacophore for IL-10 inducers through the establishment of robust structure-activity relationships. During this phase, 240 analogs were synthetized. Finally, the third part of this manuscript focuses on the development of a photochemical synthesis methology for accessing original heterocylic compounds. This methology, requiring neither heating nor metallic catalysts, aligns with the development of greener chemistry
Voitovich, Iuliia. "Les inhibiteurs d'interaction protéine-protéine, une stratégie innovante en cancérologie." Thesis, Aix-Marseille, 2018. http://www.theses.fr/2018AIXM0701.
BET-proteins, acting as epigenetic readers, play an essential role in cancer development. To date, numerous potent inhibitors disrupting BET functions have been discovered, including several of them that are undergoing clinical trials for the treatment of different types of cancer. The common drawback limiting their use in clinical practice is an inability to distinguish between BET-members that may cause side effects and resistances. The selective targeting of individual BET and the discrimination between BD1 and BD2 present an opportunity to achieve more selective transcriptional effect. A midthroughput screening of previously designed chemical library allowed identification of two molecules with unique profiles of selectivity that have never been observed. An undertaken structure-based program revealed a minimum scaffolds necessary for binding. Taking together with resolved X-Ray structures it allowed the development of more potent and selective BET inhibitors by DOTS (diversity oriented target focused synthesis) strategy, combining virtual screening and diversity oriented library design. This optimization led to a potent inhibitor with up to 100-fold improvement of affinity to the target and up to 300-fold selectivity toward BD1. Dose-response downregulation of c-Myc levels in low micromolar range in cell assays allowed the validation of the identified molecule as a chemical probe. Further comprehensive in vitro and in vivo evaluations of this compound will enable elucidating the biological role of each bromodomain and a validation of the interest toward the development of selective inhibitors in clinic
Book chapters on the topic "Optimisation hit-To-Lead":
Narjes, Frank, Garry Pairaudeau, and Dušan Petrović. "Lead Generation." In The Handbook of Medicinal Chemistry, 682–719. The Royal Society of Chemistry, 2023. http://dx.doi.org/10.1039/9781788018982-00682.
Ward, Simon E., and Andrew M. Davis. "Lead Optimisation: What You Should Know!" In The Handbook of Medicinal Chemistry, 720–68. The Royal Society of Chemistry, 2023. http://dx.doi.org/10.1039/9781788018982-00720.