新鲜出炉的Octet®文献统计来啦，快来看看是否有您的文章吧！截至五月底，陈老师共搜集到国内Octet®文章近140篇，去除预印版和综述，在这里归纳了近120篇文章的单位和应用，如下表所示：

 

文献列表见文末

可见，有至少70个单位用到了Octet®，其中，中国药科大学、上海生化所和上海药物所是前五个月发表数量TOP3（>5篇），另外复旦大学、西湖大学、澳门科技大学、中国海洋大学等也发表了多篇文章。其中不乏优质文章，仅CNS就达到5篇！(5篇CNS | Octet®第一季度国内研究成果鉴赏)

 

从应用方向来看，依然涉及到了多个应用，而小分子应用文献数量超过了1/3，是前五个月文章中最多的应用，这个与一年前的统计比较类似（畅享小分子互作分析！）。足以说明Octet®不仅可以灵敏地测试小分子，而且简单易用，可以在更短时间内获得准确的动力学数据。今天陈老师就带大家继续畅游最近的优秀国内小分子文章。

 

➤ 中国医学科学院医药生物技术研究所/岑山研究员
微生物天然产物PROTAC分子[1]

该研究发现了第一个来源于微生物天然产物的PROTAC分子（蛋白降解靶向联合体）APL-16-5，同时结合 E3 泛素连接酶 TRIM25 和流感病毒 PA 亚基，基于 PROTAC 机制，诱导TRIM25依赖的PA泛素化及其降解，阻断病毒RNA复制，具有良好的体内抗甲型流感病毒活性。表明微生物代谢产物可成为发现天然PROTAC分子的重要来源。Octet®用来检测APL-16-5与TRIM25和PA的结合。

 

传感器固化PA与TRIM25不结合，但是与TRIM25/小分子的复合物结合（红色），并且结合的信号比单独小分子结合信号高（蓝色），说明形成了PA/小分子/TRIM25复合物

 

➤ 上海药物所/柳红
进入临床的降脂药[2]

小分子 DC371739在多种动物模型中能够同时显著降低血浆中总胆固醇、低密度脂蛋白胆固醇和甘油三酯水平，并且在1期临床试验（NCT04927221）中显示出初步阳性效果和良好的耐受性。从机制上来说，DC371739与其他已知的降血脂药物不同，它是通过直接与 HNF-1α 结合来阻止 PCSK9 和 ANGPTL3 的转录，从而发挥降血脂作用。Octet®检测HNF-1α与药物的结合。

 

Octet® BLI检测结果显示，HNF-1α与药物的亲和力在μM级别

 

➤ 广州健康院/许永
高亲和力小分子抑制剂[3]

BET（Bromodomain and Extra-Terminal Domain）家族成员包括BRD2、BRD3、BRD4和BRDT，每个家族成员都具有两个N端串联的溴结构域（BD1和BD2）。BET蛋白作为转录调控的阅读器，与癌症、炎症等多种疾病的发生发展密切相关。第一代BET抑制剂（Pan BET）对BD1和BD2溴结构域不具备选择性，导致在临床试验中出现血小板减少、腹泻、恶心呕吐等毒副作用。本研究采用基于结构的药物设计策略，结合结构生物学研究开展了深入的构效关系讨论，最终获得了成药性良好的化合物XY153（8l）。XY153对BRD4 BD2表现出强结合活性，用Octet®检测可以达到nM级别的亲和力，IC50达到0.79 nM，BD2选择性倍数为354倍。该研究为开发针对急性髓性白血病的药物提供了新的候选分子。

 

Octet®检测XY153对不同家族BET蛋白的不同结构域的亲和力检测

 

➤ 浙江大学药学院/侯廷军
抗肿瘤拮抗剂[4]

雄激素受体（AR）是前列腺癌药物研发的重要靶标。靶向AR AF2位点的小分子可以直接阻断共激活因子与AR的结合。该研究通过分子对接联合MM/GBSA重打分双层筛选策略开发了一系列具有N-(4-(苄氧基)-苯基)-磺酰胺骨架的AR AF2拮抗剂。其中，化合物T1-12显示出优异的AR拮抗活性。随后，Octet®小分子蛋白互作分析系统分别测试了小分子T1-12、恩杂鲁胺和SRC2-3多肽分别与AR LBD蛋白和AR LBD-DHT复合物的亲和力，根据体系间亲和力和作用模式差异验证小分子T1-12作用于AR AF2位点。

 

BLI结果显示，Octet®与AR LBD的AF2位点结合

 

为什么越来越多的文章用Octet®检测互作呢？
- 非标记Direct Binding是趋势，它的结果更准确
- 快速测定亲和力，更加定量化对互作进行表征
- 无洗涤步骤，可测弱亲和力（解离快）
- 测试时间短，一般10分钟，更快拿到结果！
- 实验形式多样化：定性，两者结合，协同/竞争实验，垂钓
- 写入了美国药典，文章多，认可度广
- 万金油技术，可以用与检测DNA、小分子、蛋白等各种生物分子
- 使用方便，成本相对低
 

Octet® 分子互作分析系统

想要一锤定音的分子互作分析结果，就用Octet®吧！

 

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-2022前五个月国内文献列表 -

 

    Galactofuranose side chains in galactomannans from Penicillium spp. modulate galectin-8-mediated bioactivity.Carbohydrate Polymers Volume 292, 15 September 2022, 119677

    Repurposing of berbamine hydrochloride to inhibit Ebola virus by targeting viral glycoprotein.Acta Pharmaceutica Sinica B Available online 25 May 2022

    Discovery of non-substrate, environmentally sensitive turn-on fluorescent probes for imaging HDAC8 in tumor cells and tissue slices.Bioorganic & Medicinal Chemistry Volume 68, 15 August 2022, 116821

    Discovery of honokiol thioethers containing 1,3,4-oxadiazole moieties as potential α-glucosidase and SARS-CoV-2 entry inhibitors.Bioorganic & Medicinal Chemistry Volume 67, 1 August 2022, 116838

    Tereticornate A suppresses RANKL-induced osteoclastogenesis via the downregulation of c-Src and TRAF6 and the inhibition of RANK signaling pathways.Biomedicine & Pharmacotherapy Volume 151, July 2022, 113140

    Functional, structural and molecular characterizations of leukemogenic driver MEF2D-HNRNPUL1 fusion.blood

    The truncated MyD88s negatively regulates TLR2 signal on expression of IL17-1 in oyster Crassostrea gigas.Developmental & Comparative Immunology Volume 133, August 2022, 104446

    Development of a colorimetric aptasensor fabricated with a group-specific aptamer and AuNPs@Fe2+ nanozyme for simultaneous detection of multiple diarrheic shellfish poisons.Talanta Volume 246, 15 August 2022, 123534

    Epigenetic regulation of the DNMT1/MT1G/KLF4/CA9 axis synergises the anticancer effects of sorafenib in hepatocellular carcinoma.Pharmacological Research Volume 180, June 2022, 106244

    Development and characterization of a novel mouse anti-canine oncostatin M receptor beta monoclonal antibody.Biochemical and Biophysical Research Communications Volume 614, 23 July 2022, Pages 114-119

    Gasdermin D mediates doxorubicin-induced cardiomyocyte pyroptosis and cardiotoxicity via directly binding to doxorubicin and changes in mitochondrial damage.Translational Research Available online 8 May 2022

    Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.European Journal of Medicinal Chemistry Volume 238, 5 August 2022, 114423

    Ginkgolide B targets and inhibits creatine kinase B to regulate the CCT/TRiC-SK1 axis and exerts pro-angiogenic activity in middle cerebral artery occlusion mice.Pharmacological Research, Volume 180, June 2022, 106240

    Design, synthesis and antitumor evaluation of novel 1H-indole-2-carboxylic acid derivatives targeting 14-3-3η protein.European Journal of Medicinal Chemistry Volume 238, 5 August 2022, 114402

    A highly stable human single-domain antibody-drug conjugate exhibits superior penetration and treatment of solid tumors.Molecular Therapy, Available online 22 April 2022

    Agrimonolide inhibits cancer progression and induces ferroptosis and apoptosis by targeting SCD1 in ovarian cancer cells.Phytomedicine, Volume 101, July 2022, 154102

    Isolation, characterization, and structure-based engineering of a neutralizing nanobody against SARS-CoV-2.International Journal of Biological Macromolecules, Volume 209, Part A, 1 June 2022, Pages 1379-1388

    Structures of Omicron spike complexes and implications for neutralizing antibody development.Cell Reports, Volume 39, Issue 5, 3 May 2022, 110770

    Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial.Cell Metabolism, Volume 34, Issue 5, 3 May 2022, Pages 667-680.e6

    The mouse nicotinamide mononucleotide adenylyltransferase chaperones diverse pathological amyloid client proteins.JBC,Volume 298, Issue 5, May 2022, 101912

    Identification of putative binding interface of PI(3,5)P2 lipid on rice black-streaked dwarf virus (RBSDV) P10 protein.Virology, Volume 570, May 2022, Pages 81-95

    Construction of a high affinity aptamer and an aptasensor with chitosan oligosaccharide-AuNPs@Fe2+ nanozyme for highly sensitive detection of phosphatidylserine.Sensors and Actuators B: Chemical, Volume 362, 1 July 2022, 131800

    Niloticin inhibits osteoclastogenesis by blocking RANKL–RANK interaction and suppressing the AKT, MAPK, and NF-κB signaling pathways.Biomedicine & Pharmacotherapy, Volume 149, May 2022, 112902

    Interfering effects on the bioactivities of several key proteins of COVID-19/variants in diabetes by compounds from Lianqiao leaves: In silico and in vitro analyses.International Journal of Biological Macromolecules, Volume 207, 15 May 2022, Pages 715-729

    Higher affinity of polyphenol to zein than to amyloid fibrils leading to nanoparticle-embed network wall scaffold to construct amyloid fibril-zein-EGCG hydrogels for coating of beef.Food Research International, Volume 156, June 2022, 111187

    Half-Life Extension Enhances Drug Efficacy in Adeno-Associated Virus Delivered Gene Therapy.Engineering, Available online 22 March 2022

    A novel inhibitor of monooxygenase reversed the activity of tetracyclines against tet(X3)/tet(X4)-positive bacteria.eBioMedicine, Volume 78, April 2022, 103943

    TFPI is a colonic crypt receptor for TcdB from hypervirulent clade 2 C. difficile.cell

    RBD trimer mRNA vaccine elicits broad and protective immune responses against SARS-CoV-2 variants.iScience, Volume 25, Issue 4, 15 April 2022, 104043

    Broad neutralization of SARS-CoV-2 variants by an inhalable bispecific single-domain antibody.CELL

    Structural basis of nanobodies neutralizing SARS-CoV-2 variants.Structure, Volume 30, Issue 5, 5 May 2022, Pages 707-720.e5

    Kappa-RBD produced by glycoengineered Pichia pastoris elicited high neutralizing antibody titers against pseudoviruses of SARS-CoV-2 variants.Virology, Volume 569, April 2022, Pages 56-63

    Atomic zinc sites with hierarchical porous carbon for high-throughput chemical screening with high loading capacity and stability.Pharmacological Research, Volume 178, April 2022, 106154

    CgATP synthase β subunit involved in the regulation of haemocytes proliferation as a CgAstakine receptor in Crassostrea gigas.Fish & Shellfish Immunology, Volume 123, April 2022, Pages 85-93

    A highly immunogenic live-attenuated vaccine candidate prevents SARS-CoV-2 infection and transmission in hamsters.The Innovation, Volume 3, Issue 2, 29 March 2022, 100221

    Small-molecule albumin ligand modification to enhance the anti-diabetic ability of GLP-1 derivatives.Biomedicine & Pharmacotherapy, Volume 148, April 2022, 112722

    Biomimetic ion nanochannels for sensing umami substances.Biomaterials, Volume 282, March 2022, 121418

    Motif-dependent immune co-receptor interactome profiling by photoaffinity chemical proteomics.Cell Chemical Biology

    Double amplification upon immuno-gold nanoparticles promoted trace measurement of ricin by biolayer interferometry.Sensors and Actuators B: Chemical, Volume 358, 1 May 2022, 131472

    Esculentoside A alleviates cognitive deficits and amyloid pathology through peroxisome proliferator-activated receptor γ-dependent mechanism in an Alzheimer's disease model.Phytomedicine, Volume 98, April 2022, 153956

    Dual-functional significance of ATM-mediated phosphorylation of spindle assembly checkpoint component Bub3 in mitosis and the DNA damage response.Journal of Biological Chemistry, Volume 298, Issue 3, March 2022, 101632

    Aptamer truncation strategy assisted by molecular docking and sensitive detection of T-2 toxin using SYBR Green I as a signal amplifier.Food Chemistry, Volume 381, 1 July 2022, 132171

    ERF4 affects fruit ripening by acting as a JAZ interactor between ethylene and jasmonic acid hormone signaling pathways.Horticultural Plant Journal, Available online 13 January 2022

    Enrichment of IgG and HRP glycoprotein by dipeptide-based polymeric material.Talanta, Volume 241, 1 May 2022, 123223

    Multiple functionalities of functional nucleic acids for developing high-performance lateral flow assays.TrAC Trends in Analytical Chemistry, Volume 148, March 2022, 116529

    Deoxyhypusine hydroxylase as a novel pharmacological target for ischemic stroke via inducing a unique post-translational hypusination modification.Pharmacological Research, Volume 176, February 2022, 106046

    Organic NIR-II dyes with ultralong circulation persistence for image-guided delivery and therapy.Journal of Controlled Release, Volume 342, February 2022, Pages 157-169

    Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer.European Journal of Medicinal Chemistry, Volume 229, 5 February 2022, 114082

    Structural and biochemical mechanism for increased infectivity and immune evasion of Omicron BA.2 variant compared to BA.1 and their possible mouse origins.Cell Research (2022)

    A genetic engineering strategy for editing near-infrared-II fluorophores.Nature Communications volume 13

    Insights into the client protein release mechanism of the ATP-independent chaperone Spy.Nature Communications volume 13

    Structure-guided affinity maturation of a novel human antibody targeting the SARS-CoV-2 nucleocapsid protein.Scientific Reports volume 12,

    Quadrivalent mosaic HexaPro-bearing nanoparticle vaccine protects against infection of SARS-CoV-2 variants.Nature Communications volume 13

    Unique binding pattern for a lineage of human antibodies with broad reactivity against influenza A virus.Nature Communications volume 13

    Novel sarbecovirus bispecific neutralizing antibodies with exceptional breadth and potency against currently circulating SARS-CoV-2 variants and sarbecoviruses.Cell Discovery volume 8

    An anti-influenza A virus microbial metabolite acts by degrading viral endonuclease PA.Nature Communications volume 13

    T cells expressing CD5/CD7 bispecific chimeric antigen receptors with fully human heavy-chain-only domains mitigate tumor antigen escape.Signal Transduction and Targeted Therapy volume 7

    RNA G-quadruplex in TMPRSS2 reduces SARS-CoV-2 infection.Nature Communications volume 13

    Molecular basis of receptor binding and antibody neutralization of Omicron.NATURE

    Structural basis for SARS-CoV-2 Delta variant recognition of ACE2 receptor and broadly neutralizing antibodies.Nature Communications volume 13

    ACE2-Targeting antibody suppresses SARS-CoV-2 Omicron and Delta variants.Signal Transduction and Targeted Therapy volume 7

    Parallel profiling of antigenicity alteration and immune escape of SARS-CoV-2 Omicron and other variant.Signal Transduction and Targeted Therapy volume 7

    Memory B cell repertoire from triple vaccinees against diverse SARS-CoV-2 variants.NATURE

    Microbial-Catalyzed Baeyer–Villiger Oxidation for 3,4-seco-Triterpenoids as Potential HMGB1 Inhibitors.ACS Omega 2022

    Antibiotic-Like Activity of Atomic Layer Boron Nitride for Combating Resistant Bacteria.ACS Nano 2022, 16, 5, 7674–7688

    Structure-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.J. Med. Chem. 2022, 65, 7, 5760–5799

    Heterogeneous Iron Oxide/Dysprosium Oxide Nanoparticles Target Liver for Precise Magnetic Resonance Imaging of Liver Fibrosis.ACS Nano 2022, 16, 4, 5647–5659

    Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome.J. Med. Chem. 2022, 65, 6, 5029–5043

    Covalently Engineered Protein Minibinders with Enhanced Neutralization Efficacy against Escaping SARS-CoV-2 Variants.J. Am. Chem. Soc. 2022, 144, 13, 5702–5707

    Identification of Adenylate Kinase 5 as a Protein Target of Ginsenosides in Brain Tissues Using Mass Spectrometry-Based Drug Affinity Responsive Target Stability (DARTS) and Cellular Thermal Shift Assay (CETSA) Techniques.J. Agric. Food Chem. 2022, 70, 8, 2741–2751

    Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.J. Med. Chem. 2022, 65, 3, 2507–2521

    PD-L1/TIGIT bispecific antibody showed survival advantage in animal model.https://doi.org/10.1002/ctm2.754

    Blockade of mIL-6R alleviated lipopolysaccharide-induced systemic inflammatory response syndrome by suppressing NF-κB-mediated Ccl2 expression and inflammasome activation. https://doi.org/10.1002/mco2.132

    Generation and characterization of humanized synergistic neutralizing antibodies against SARS-CoV-2. https://doi.org/10.1002/jmv.27801

    Analgesic effects of nerve growth factor-directed monoclonal antibody on diabetic neuralgia in an animal model.https://doi.org/10.1002/2211-5463.13410

    Potent Anti-SARS-CoV-2 Efficacy of COVID-19 Hyperimmune Globulin from Vaccine-Immunized Plasma. https://doi.org/10.1002/advs.202104333

    A Hybrid Supramolecular Polymeric Nanomedicine for Cascade-Amplified Synergetic Cancer Therapy.https://doi.org/10.1002/ange.202203786

    HER2/PD1 bispecific antibody in IgG4 subclass with superior anti-tumour activities.https://doi.org/10.1002/ctm2.791

    Identification of Ziyuglycoside II from a Natural Products Library as a STING Agonist. https://doi.org/10.1002/cmdc.202100719

    Acridinium-conjugated aromatic heterocycles as highly potent FtsZ inhibitors: Design, synthesis, and biological evaluation.https://doi.org/10.1002/ardp.202100400

    A novel transcriptional activation mechanism of inulinase gene in Kluyveromyces marxianus involving a glycolysis regulator KmGcr1p with unique and functional Q-rich repeats.https://doi.org/10.1111/mmi.14889

    Synthesis and identification of lithocholic acid 3-sulfate as RORγt ligand to inhibit Th17 cell differentiation.https://doi.org/10.1002/JLB.1MA0122-513R

    Structural characteristics of Heparan sulfate required for the binding with the virus processing Enzyme Furin.Glycoconjugate Journal volume 39, pages315–325 (2022)

    Novel contact–kinin inhibitor sylvestin targets thromboinflammation and ameliorates ischemic stroke.Cellular and Molecular Life Sciences volume 79

    Development of a Label-Free Colorimetric Aptasensor with Rationally Utilized Aptamer for Rapid Detection of Okadaic Acid.Journal of Ocean University of China volume 21, pages400–408 (2022)

    A novel insight into mechanism of derangement of coagulation balance: interactions of quantum dots with coagulation-related proteins.Particle and Fibre Toxicology volume 19, Article number: 17 (2022)

    Discovery of a Natural Product with Potent Efficacy Against SARS-CoV-2 by Drug Screening.Interdisciplinary Sciences: Computational Life Sciences volume 14, pages55–63 (2022)

    LAP2α preserves genome integrity through assisting RPA deposition on damaged chromatin.Genome Biology volume 23, Article number: 64 (2022)

    Combined strategies for effective cancer immunotherapy with a novel anti-CD47 monoclonal antibody.Cancer Immunology, Immunotherapy volume 71, pages353–363 (2022)

    A novel tumor-homing TRAIL variant eradicates tumor xenografts of refractory colorectal cancer cells in combination with tumor cell-targeted photodynamic therapy.Drug Delivery, Volume 29, 2022 - Issue 1

    Methylparaben as a preservative in the development of a multi-dose HPV-2 vaccine.Human Vaccines & Immunotherapeutics

    5,2′-Dibromo-2,4′,5′-trihydroxydiphenylmethanone Inhibits LPS-Induced Vascular Inflammation by Targeting the Cav1 Protein.Molecules 2022, 27(9), 2884

    PD‐L1/TIGIT bispecific antibody showed survival advantage in animal model.Clin Transl Med. 2022 May; 12(5): e754.

    An automated, rapid fluorescent immunoassay to quantify serum soluble programmed death-1 (PD-1) protein using testing-on-a-probe biosensors. Clinical Chemistry and Laboratory Medicine (CCLM)

    Ultrapotent neutralizing antibodies against SARS-CoV-2 with a high degree of mutation resistance.JCI

    High Mannose-Specific Aptamers for Broad-Spectrum Virus Inhibition and Cancer Targeting.https://doi.org/10.31635/ccschem.022.202101747

    Selection, Characterization, and Optimization of DNA Aptamers against Challenging Marine Biotoxin Gymnodimine-A for Biosensing Application.Toxins 2022, 14(3), 195

    Flotillin 2 Facilitates the Infection of a Plant Virus in the Gut of Insect Vector.DOI:https://doi.org/10.1128/jvi.02140-21

    A Five-Helix-Based SARS-CoV-2 Fusion Inhibitor Targeting Heptad Repeat 2 Domain against SARS-CoV-2 and Its Variants of Concern.Viruses 2022, 14(3), 597

    Elucidating the Novel Mechanism of Ligustrazine in Preventing Postoperative Peritoneal Adhesion Formation.https://doi.org/10.1155/2022/9226022

    Structural Characterization of RC28-E, a Recombinant Fusion Protein With Dual Targets on VEGF and FGF2.https://doi.org/10.1177/1934578X221086989

    Mucoadhesive Nucleoside-Based Hydrogel Delays Oral Leukoplakia Canceration.https://doi.org/10.1177/00220345221085192

    TIM-1 Augments Cellular Entry of Ebola Virus Species and Mutants, Which Is Blocked by Recombinant TIM-1 Protein.DOI:https://doi.org/10.1128/spectrum.02212-21

    An Innovative Site-Specific Anti-HER2 Antibody-Drug Conjugate with High Homogeneity and Improved Therapeutic Index.Onco Targets Ther. 2022; 15: 331–343.

    ROS1 promotes low temperature-induced anthocyanin accumulation in apple by demethylating the promoter of anthocyanin-associated genes.Horticulture Research, Volume 9, 2022

    Extracellular Vesicle Delivery of Neferine for the Attenuation of Neurodegenerative Disease Proteins and Motor Deficit in an Alzheimer’s Disease Mouse Model.Pharmaceuticals 2022, 15(1)

    A prototype protein nanocage minimized from carboxysomes with gated oxygen permeability.PNAS

    Preclinical characterization of the novel anti-SIRPα antibody BR105 that targets the myeloid immune checkpoint.J Immunother Cancer. 2022; 10(3): e004054.

    Rapid Optical Biosensing of SARS-CoV-2 Spike Proteins in Artificial Samples.Sensors 2022, 22(10), 3768

    Neutralizing SARS-CoV-2 by dimeric side chain-to-side chain cross-linked ACE2 peptide mimetics.Chemical Communications


-参考文献-

    An anti-influenza A virus microbial metabolite acts by degrading viral endonuclease PA. Nature Communications volume 13

    Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial. Cell Metabolism Volume 34, Issue 5, 3 May 2022, Pages 667-680.e6

    Structure-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors. J. Med. Chem. 2022, 65, 7, 5760–5799

    Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.J. Med. Chem. 2022, 65, 3, 2507–2521