Medicinal Chemistry Approaches to Personalized Medicine

Acronyms

AChE(I) acetylcholine esterase (inhibitor) AD Alzheimer's disease ADC antibody drug conjugates ADME absorption, distribution, metabolism, and excretion AE adverse events AGC protein kinase A, G, and C families AHR airway hyperresponsiveness ALCL anaplastic large-cell lymphoma ALK anaplastic lymphoma kinase AP-1 activating protein 1 APC adenomatous polyposis coli gene APP amyloid precursor protein ATP adenosine triphosphate AUC area under the curve BBB blood–brain barrier BCC basal-cell carcinoma BCRP breast cancer resistance protein BER base excision repair BID bis in die (Latin) meaning twice a day BP binding protein CAD coronary artery disease CBD corticobasal degeneration CETP cholesteryl ester transfer protein CHMP Committee for Medicinal Products for Human Use CIA collagen-induced arthritis CI confidence interval CLR clearance rate CML chronic myelogenous leukemia CNS central nervous system CNV copy number variations COPD chronic obstructive pulmonary disorder CR complete response CRC colorectal cancer CSF cerebral spinal fluid CTC circulating tumor cells CUP carcinoma of unknown primary CDK cyclin-dependent kinase COMT catechol-O-methyl transferase DAG diacylglycerol DAT dopamine transporter DCR disease control rate DDR DNA damage response DECP diethyl cyanophosphonate DLB dementia with Lewy bodies DMF dimethylformamide DMSO dimethylsulfoxide DNA deoxyribonucleic acid DR direct repair DUPA (dicarboxypropyl)ureidopentanedioic acid ER estrogen receptor ErbB2 erythroblastic leukemia oncogene homolog 2, also known as HER2/Neu ERK extracellular regulating kinase FAM 6-carboxyfluorescein FBDD fragment-based drug discovery FBLD fragment-based ligand discovery FDA Food and Drug Administration FDG fluoro-deoxy-d-glucose FFPET formalin fixed paraffin embedded tissue FISH fluorescence in situ hybridization FRET fluorescence resonance energy transfer FTD frontotemporal dementia GEMM genetically engineered mouse model GIM genetic interaction mapping GIST gastrointestinal stromal tumors GLUT glucose transport proteins GSK glycogen synthase kinase GTPase guanine triphosphatase GWAS genome-wide association studies HDAC histone deacetylases HDM histone demethylases HER2 human epidermal growth factor receptor 2 hERG human ether-a-go-go related gene HGF(R) hepatocyte growth factor (receptor) Hh hedgehog HIF hypoxia inducible factor HR homologous recombinations HSP heat shock protein HTS high-throughput screening IC50 concentration at 50% inhibition ICGC International Cancer Genome Consortium ICS inhaled corticosteroids IGF(R) insulin growth factor (receptor) IHC immunohistochemistry IL-1 interleukin-1 IMT inflammatory myofibroblastic tumors INDEL insertions or deletions of a short coding region ITK interleukin-2-inducible T-cell kinase IV intravenous LABA long acting beta-2 agonists LE ligand efficiency LipE lipophilic efficiency LN lymph node MAO monoamine oxidase MAPK mitogen-activated protein kinase MBC metastatic breast cancer MBP microprecipitated bulk powder MCI mild cognitive impairment MCT methylcellulose Tween MGMT O-(6)-methylguanine-DNA methyltransferase MK midkine MLC myosin light chain MLK mixed lineage kinase MMR mismatch repair MMSE minimental state examination MOM methoxymethyl MP molecular profiling MPI myocardial perfusion imaging MRI magnetic resonance imaging MRT mean residence time MTD maximum tolerated dose MTEB metabotropic glutamate receptor type mTOR mammalian target of rapamycin NA not applicable NCI National Cancer Institute NER nucleotide excision repair NET norepinephrine transporter NFT neurofibrillary tangles NGS next-generation sequencers NHEJ nonhomologous end joining NHL non-Hodgkin lymphoma NIH National Institute of Health NK natural killer NME new molecular entity NMR nuclear magnetic resonance NOAEL no adverse effect level NPM nucleophosmin NRTK nonreceptor tyrosine kinase NSCLC non-small cell lung cancer OICR Ontario Institute for Cancer Research ORR overall response rate OS overall survival PARP poly-ADP-ribose polymerase PAS peripheral anionic...