Affinage

VPS72

Vacuolar protein sorting-associated protein 72 homolog · UniProt Q15906

Length
364 aa
Mass
40.6 kDa
Annotated
2026-06-11
100 papers in source corpus 11 papers cited in narrative 11 extracted findings
Cross-family judge vs UniProt: tie faithfulness: 6/6 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

VPS72 (YL1) is a conserved histone chaperone that confers H2A.Z specificity to ATP-dependent chromatin remodeling, functioning as a shared subunit of the SRCAP remodeling complex and the TRRAP/TIP60 histone acetyltransferase complex (PMID:15647280, PMID:26974124). Through a whip-like H2A.Z-binding domain, VPS72 directly wraps over the H2A.Z-H2B dimer, recognizing the extended αC helix, the hyperacidic patch, and the DNA-binding surface that distinguish H2A.Z from canonical H2A; substitution of as few as four H2A residues is sufficient to create a VPS72-recognized interface (PMID:26974124, PMID:26974126). The chaperone enforces unidirectional exchange by exploiting the inherent instability of H2A-containing nucleosomes, with an N-terminal subdomain anchoring the H2A nucleosome to license SWR1/SRCAP-catalyzed replacement of nucleosomal H2A with H2A.Z (PMID:34038732). This activity was first defined in yeast, where the ortholog Swc2 binds H2A.Z directly and is essential for its transfer during nucleosomal histone exchange (PMID:16299513). Beyond canonical remodeling, VPS72 acts independently of SRCAP and EP400 to deposit H2A.Z during post-mitotic nuclear reassembly, and its depletion produces malformed, nonfunctional nuclei (PMID:32708675). In hepatocellular carcinoma, VPS72 interacts with MYC and ACTL6A to enhance MYC promoter binding and oncogenic transcription, with its stability governed by ACTL6A antagonism of TRIM21-mediated ubiquitination, and it binds KAT5/TIP60 to modulate PI3K/AKT signaling (PMID:36631007, PMID:35383533).

Mechanistic history

Synthesis pass · year-by-year structured walk · 8 steps
  1. 2005 High

    Established that the VPS72 ortholog is a direct H2A.Z-binding factor essential for histone exchange, defining the molecular basis for variant-specific nucleosome remodeling.

    Evidence Co-immunoprecipitation, in vitro binding, and subunit-mutant analysis of Swc2 in yeast SWR1

    PMID:16299513

    Open questions at the time
    • Structural basis of H2A.Z discrimination not yet resolved
    • Requirement for Swc6/Arp6 in association left mechanism of recruitment unclear
  2. 2005 High

    Defined VPS72 as a shared subunit bridging two distinct mammalian chromatin machines, placing it at the intersection of remodeling and acetylation.

    Evidence Mass spectrometry of affinity-purified complexes and reciprocal co-IP from HeLa cells

    PMID:15647280

    Open questions at the time
    • Functional division of labor between the two complexes not addressed
    • No structural detail of how VPS72 docks into either complex
  3. 2016 High

    Resolved at near-atomic resolution how VPS72 achieves H2A.Z selectivity, showing a whip-like domain that reads out H2A.Z-specific surfaces and is essential for deposition.

    Evidence X-ray crystallography of Drosophila and human YL1-H2A.Z-H2B complexes with in vitro exchange and in vivo ChIP validation

    PMID:26974124 PMID:26974126

    Open questions at the time
    • Structure of full-length VPS72 within the SRCAP holocomplex unresolved
    • Coupling of chaperone binding to ATP-dependent catalysis not visualized
  4. 2021 High

    Explained the directionality of exchange, showing VPS72 exploits intrinsic H2A nucleosome instability to drive unidirectional H2A-to-H2A.Z replacement.

    Evidence Single-molecule force spectroscopy, mutagenesis, and in vitro/in vivo SWR1 exchange assays in yeast

    PMID:34038732

    Open questions at the time
    • Generality of the three H2A α2 residues across species not established
    • Kinetics of the anchoring-to-eviction transition unresolved
  5. 2020 High

    Revealed a chromatin-remodeling-independent role, demonstrating VPS72 deposits H2A.Z for proper nuclear reformation after mitosis outside the SRCAP/EP400 complexes.

    Evidence siRNA knockdown with live-cell imaging plus cell-free nuclear assembly assay with immunodepletion in HeLa

    PMID:32708675

    Open questions at the time
    • Identity of the alternative complex (if any) delivering H2A.Z during reassembly unknown
    • Mechanism linking H2A.Z deposition to functional nuclear envelope formation not defined
  6. 2020 Medium

    Connected the ortholog to autophagy regulation via an acetyltransferase complex acting on the LC3 ortholog Atg8a.

    Evidence Co-IP, mass spectrometry, and genetic knockdown with autophagy assays in Drosophila

    PMID:32460019

    Open questions at the time
    • Direct enzymatic role of VPS72 in Atg8a acetylation not established
    • Conservation of this autophagy link in mammals untested
  7. 2022 Medium

    Linked VPS72 to oncogenic signaling, showing it binds KAT5/TIP60 to sustain PI3K/AKT activation in hepatocellular carcinoma.

    Evidence Co-IP, siRNA knockdown, and KAT5 overexpression rescue with phospho-PI3K/AKT readouts in HCC cells

    PMID:35383533

    Open questions at the time
    • Single Co-IP without reciprocal validation of the VPS72-KAT5 interaction
    • Mechanism connecting KAT5 binding to PI3K/AKT phosphorylation undefined
  8. 2023 Medium

    Defined an oncogenic transcriptional axis in which VPS72 cooperates with MYC and ACTL6A, with stability controlled by TRIM21 ubiquitination.

    Evidence Reciprocal Co-IP, shRNA knockdown, ChIP, and in vivo xenograft assays in HCC

    PMID:36631007

    Open questions at the time
    • Whether this axis depends on VPS72 chromatin-chaperone activity unclear
    • Direct TRIM21 ubiquitination sites on VPS72 not mapped

Open questions

Synthesis pass · forward-looking unresolved questions
  • How VPS72's biochemically defined H2A.Z chaperone activity mechanistically underlies its disparate cellular roles in nuclear reassembly, autophagy, and oncogenic transcription remains unresolved.
  • No integrated model linking H2A.Z deposition to MYC-driven transcription
  • Tissue-specific contributions of the SRCAP versus TIP60 complexes not dissected

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0042393 histone binding 4 GO:0140096 catalytic activity, acting on a protein 1
Localization
GO:0000228 nuclear chromosome 2 GO:0005634 nucleus 2
Pathway
R-HSA-4839726 Chromatin organization 4 R-HSA-74160 Gene expression (Transcription) 1
Partners
ACTL6AH2A.ZKAT5MYCTRIM21
Complex memberships
SRCAP complexSWR1 complexTRRAP/TIP60 (EP400) HAT complex

Evidence

Reading pass · 11 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2005 Swc2 (yeast ortholog of VPS72/YL1) binds directly to histone H2A.Z and is essential for its transfer during ATP-dependent nucleosomal histone exchange by the SWR1 complex. Swc6 and Arp6 are required for Swc2 association and nucleosome binding, while the C-terminal alpha-helix of H2A.Z is crucial for SWR1 recognition. Co-immunoprecipitation, in vitro binding assays, domain dissection, mutant analysis in yeast Nature structural & molecular biology High 16299513
2005 Mammalian YL1 (VPS72) is a shared subunit of two distinct chromatin-modifying complexes: the TRRAP/TIP60 histone acetyltransferase (HAT) complex and the SRCAP chromatin-remodeling complex (a mammalian equivalent of the yeast SWR1 complex). Mass spectrometry of affinity-purified complexes, co-immunoprecipitation from HeLa cells The Journal of biological chemistry High 15647280
2016 Crystal structure of the H2A.Z-binding domain of Drosophila YL1 (dYL1-Z) in complex with H2A.Z-H2B dimer at 1.9-Å resolution revealed a whip-like structure that wraps over H2A.Z-H2B. Preferential recognition of H2A.Z is conferred by three residues in loop 2, the hyperacidic patch, and the extended αC helix of H2A.Z. The YL1-Z domain is essential for H2A.Z deposition in vivo and SRCAP-catalyzed histone replacement in vitro. X-ray crystallography at 1.9-Å resolution, in vitro histone exchange assay, in vivo H2A.Z ChIP in yeast Nature structural & molecular biology High 26974124
2016 Crystal structure of the human YL1-H2A.Z-H2B complex at 2.7-Å resolution showed that YL1 acts as a specific H2A.Z-deposition chaperone. YL1 binding triggers extension of the H2A.Z αC helix (similar to the eviction chaperone ANP32E), but the interaction is more extensive and includes both the extended acidic patch and the entire DNA-binding surface of H2A.Z-H2B. Substitution of only four residues of H2A is sufficient to create an H2A.Z-like interface specifically recognized by YL1. X-ray crystallography at 2.7-Å resolution, mutagenesis, in vitro binding assays Nature structural & molecular biology High 26974126
2020 VPS72/YL1 is required for nuclear reassembly after mitosis. siRNA-mediated knockdown of VPS72 extends telophase in HeLa cells (live-cell imaging). In cell-free nuclear assembly assays, depletion of VPS72 or H2A.Z results in malformed and nonfunctional nuclei. Importantly, VPS72 functions outside of the SRCAP and EP400 remodeling complexes to deposit H2A.Z for nuclear reformation. siRNA knockdown, live-cell imaging, cell-free nuclear assembly assay, immunodepletion Cells High 32708675
2021 The N-terminal 1-135 residues of Swc2 (Swc2-Z) facilitate disassembly of nucleosomes containing H2A but not H2A.Z, enabling unidirectional exchange. This selectivity depends on inherent instability of the H2A nucleosome conferred by three H2A α2-helical residues (Gly47, Pro49, Ile63). The Swc2-ZN subdomain (residues 1-37) directly anchors to the H2A nucleosome and is required for SWR1-catalyzed H2A.Z replacement in vitro and H2A.Z deposition in vivo. Single-molecule force spectroscopy, mutagenesis, in vitro SWR1 histone exchange assay, in vivo ChIP in yeast Cell reports High 34038732
2023 VPS72 interacts with MYC and ACTL6A and promotes formation of the ACTL6A/MYC complex in HCC cells. ACTL6A regulates VPS72 protein stability by weakening the interaction between the E3 ubiquitin ligase TRIM21 and VPS72. The VPS72-ACTL6A interaction enhances MYC binding affinity to target gene promoters and promotes their transcription. Co-immunoprecipitation, shRNA knockdown, overexpression, in vivo xenograft, ChIP assays, AAV8-mediated shRNA delivery Hepatology (Baltimore, Md.) Medium 36631007
2022 VPS72 physically binds KAT5 (TIP60/KAT5 acetyltransferase) in hepatocellular carcinoma cells. KAT5 overexpression rescues the suppression of proliferation, invasion, and migration caused by VPS72 knockdown, and VPS72 silencing downregulates p-PI3K and p-AKT expression in a KAT5-dependent manner. Co-immunoprecipitation, siRNA knockdown, overexpression rescue, western blotting for PI3K/AKT phosphorylation Bioengineered Medium 35383533
2020 In Drosophila, YL-1 (VPS72 ortholog) is a component of a nuclear acetyltransferase complex and interacts with Atg8a (LC3 ortholog). Atg8a is acetylated in nutrient-rich conditions, and this acetylation is linked to YL-1 association, suggesting YL-1 participates in regulating autophagy gene expression through Atg8a acetylation status. Co-immunoprecipitation, mass spectrometry, genetic knockdown in Drosophila, autophagy assays Cell reports Medium 32460019
1995 Forced expression of YL-1 (VPS72) protein in Kirsten sarcoma virus-transformed NIH3T3 cells markedly suppressed anchorage-independent growth (colony formation in soft agar), identifying it as a transformation suppressor. Rare soft-agar colonies that escaped expressed reduced or no exogenous YL-1, sometimes with loss/rearrangement of the introduced cDNA. YL-1 did not affect adherent-culture transformed phenotypes or tumorigenicity in nude mice. Stable cDNA overexpression, soft agar colony formation assay, antisense control experiments Experimental cell research Medium 7664828
2001 YL-1 (VPS72) undergoes intergenic splicing into TMOD4 and also produces alternative transcripts via intraexonic splicing using non-canonical splice sites. YL-1 encodes six exons with the last exon 291 bp from a 5' UTR exon of TMOD4. 5' RACE, RT-PCR, genomic sequence analysis BMC genomics Low 11716785

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2005 Swc2 is a widely conserved H2AZ-binding module essential for ATP-dependent histone exchange. Nature structural & molecular biology 205 16299513
2005 The mammalian YL1 protein is a shared subunit of the TRRAP/TIP60 histone acetyltransferase and SRCAP complexes. The Journal of biological chemistry 184 15647280
2008 Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. Journal of medicinal chemistry 132 18800763
2012 Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. Journal of medicinal chemistry 120 23181587
2011 The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. Neuropharmacology 112 21619887
2008 Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). Journal of medicinal chemistry 93 18318463
2016 Structural basis of H2A.Z recognition by SRCAP chromatin-remodeling subunit YL1. Nature structural & molecular biology 82 26974124
1985 Evidence for N-(deoxyguanosin-8-yl)-1-aminopyrene as a major DNA adduct in female rats treated with 1-nitropyrene. Carcinogenesis 75 3838706
2007 Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition. The Journal of pharmacology and experimental therapeutics 72 17684118
2016 Molecular basis and specificity of H2A.Z-H2B recognition and deposition by the histone chaperone YL1. Nature structural & molecular biology 68 26974126
2005 Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists. Journal of medicinal chemistry 68 16220976
2007 Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. Journal of medicinal chemistry 63 17253678
2019 5-(3,4-Difluorophenyl)-3-(6-methylpyridin-3-yl)-1,2,4-oxadiazole (DDO-7263), a novel Nrf2 activator targeting brain tissue, protects against MPTP-induced subacute Parkinson's disease in mice by inhibiting the NLRP3 inflammasome and protects PC12 cells against oxidative stress. Free radical biology & medicine 61 30615919
1999 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists. Bioorganic & medicinal chemistry letters 59 10476866
2018 Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. Journal of medicinal chemistry 58 30359003
1998 Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane . European journal of pharmacology 55 9774240
2006 Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. Journal of medicinal chemistry 54 17149879
2018 Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. Journal of medicinal chemistry 51 30204441
2007 Mutagenicity of the 1-nitropyrene-DNA adduct N-(deoxyguanosin-8-yl)-1-aminopyrene in mammalian cells. Chemical research in toxicology 50 17907783
2018 Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. Journal of medicinal chemistry 41 30525599
2016 Seeking potent anti-tubercular agents: Design, synthesis, anti-tubercular activity and docking study of various ((triazoles/indole)-piperazin-1-yl/1,4-diazepan-1-yl)benzo[d]isoxazole derivatives. Bioorganic & medicinal chemistry letters 41 27020525
2014 Synthesis and antiproliferative activity of substituted 3[2-(1H-indol-3-yl)- 1,3-thiazol-4-yl]-1H-pyrrolo[3,2-b]pyridines, marine alkaloid nortopsentin analogues. Current medicinal chemistry 37 24180279
2014 Discovery of methyl 4'-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an improved small-molecule inhibitor of c-Myc-max dimerization. ChemMedChem 36 24976143
2009 3-(4-(Benzo[d]thiazol-2-yl)-1-phenyl-1H-pyrazol-3-yl) phenyl acetate induced Hep G2 cell apoptosis through a ROS-mediated pathway. Chemico-biological interactions 35 20018182
2024 Novel quinazolin-2-yl 1,2,3-triazole hybrids as promising multi-target anticancer agents: Design, synthesis, and molecular docking study. Bioorganic chemistry 34 38749114
1988 Enzymatic conjugation of hexachloro-1,3-butadiene with glutathione. Formation of 1-(glutathion-S-yl)-1,2,3,4,4-pentachlorobuta-1,3-diene and 1,4-bis(glutathion-S-yl)-1,2,3,4-tetrachlorobuta-1,3-diene. Drug metabolism and disposition: the biological fate of chemicals 34 2906593
2016 In vitro, molecular modeling and behavioral studies of 3-{[4-(5-methoxy-1H-indol-3-yl)-1,2,3,6-tetrahydropyridin-1-yl]methyl}-1,2-dihydroquinolin-2-one (D2AAK1) as a potential antipsychotic. Neurochemistry international 32 26964765
2015 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin analogues with antiproliferative activity. Marine drugs 32 25854642
2005 Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide. Journal of medicinal chemistry 29 16279795
2004 Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists. Journal of medicinal chemistry 29 14695840
2019 Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. Bioorganic & medicinal chemistry 28 30795991
2018 5-(Thiophen-2-yl)-1,3,4-thiadiazole derivatives: synthesis, molecular docking and in vitro cytotoxicity evaluation as potential anticancer agents. Drug design, development and therapy 28 29881258
2004 Ro 64-6198 [(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one] acts differently from nociceptin/orphanin FQ in rat periaqueductal gray slices. The Journal of pharmacology and experimental therapeutics 28 15254141
2020 Regulation of Expression of Autophagy Genes by Atg8a-Interacting Partners Sequoia, YL-1, and Sir2 in Drosophila. Cell reports 27 32460019
2015 Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Bioorganic & medicinal chemistry letters 27 26475521
2018 Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. Journal of medicinal chemistry 26 30130103
2023 Targeting VPS72 inhibits ACTL6A/MYC axis activity in HCC progression. Hepatology (Baltimore, Md.) 25 36631007
2019 Design, synthesis and biological evaluation of substituted 2-(thiophen-2-yl)-1,3,5-triazine derivatives as potential dual PI3Kα/mTOR inhibitors. Bioorganic chemistry 25 31887474
2013 Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase. Bioorganic & medicinal chemistry letters 25 24012121
2009 Analysis of pulmonary vasodilator responses to SB-772077-B [4-(7-((3-amino-1-pyrrolidinyl)carbonyl)-1-ethyl-1H-imidazo(4,5-c)pyridin-2-yl)-1,2,5-oxadiazol-3-amine], a novel aminofurazan-based Rho kinase inhibitor. The Journal of pharmacology and experimental therapeutics 23 19369577
2019 Synthesis and Anticancer Activity of New ((Furan-2-yl)-1,3,4-thiadiazolyl)-1,3,4-oxadiazole Acyclic Sugar Derivatives. Chemical & pharmaceutical bulletin 22 31366838
2014 One-pot, four-component synthesis of novel cytotoxic agents 1-(5-aryl-1,3,4-oxadiazol-2-yl)-1-(1H-pyrrol-2-yl)methanamines. European journal of medicinal chemistry 22 24681979
2013 Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorganic & medicinal chemistry 22 24369839
2012 Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives. European journal of medicinal chemistry 22 22321993
2020 VPS72/YL1-Mediated H2A.Z Deposition Is Required for Nuclear Reassembly after Mitosis. Cells 21 32708675
2007 Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor. Drug metabolism and disposition: the biological fate of chemicals 20 17344341
2021 Pyoverdines Are Essential for the Antibacterial Activity of Pseudomonas chlororaphis YL-1 under Low-Iron Conditions. Applied and environmental microbiology 19 33452032
2019 Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors. Journal of medicinal chemistry 19 31009559
1997 Neurochemical effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-b enzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, in rats. The Journal of pharmacology and experimental therapeutics 19 9067312
1996 Solution properties and computational analysis of an oligodeoxynucleotide containing N-(deoxyguanosin-8-yl)-1-aminopyrene. Carcinogenesis 19 8565123
2018 8-Hydroxy-2-(1H-1,2,3-triazol-1-yl)-1,4-naphtoquinone derivatives inhibited P2X7 Receptor-Induced dye uptake into murine Macrophages. Bioorganic & medicinal chemistry 18 30528164
2014 Synthesis and biological evaluation of some 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones: antibacterial, DNA photocleavage, and anticancer activities. European journal of medicinal chemistry 18 24849271
2007 Long-term reduction of brain-derived neurotrophic factor levels and signaling impairment following prenatal treatment with the cannabinoid receptor 1 receptor agonist (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinyl-methyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1- naphthalenylmethanone. The European journal of neuroscience 17 17552998
2022 Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as a σ2 Receptor Brain PET Tracer. Journal of medicinal chemistry 16 35404616
2017 Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder. The Journal of pharmacology and experimental therapeutics 16 28954811
2013 Copper(II/I) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline: synthesis, crystal structure, antitumor activity and DNA interaction. European journal of medicinal chemistry 16 24211640
2007 Pharmacological properties of a novel nociceptin/orphanin FQ receptor agonist, 2-(3,5-dimethylpiperazin-1-yl)-1-[1-(1-methylcyclooctyl)piperidin-4-yl]-1H-benzimidazole, with anxiolytic potential. European journal of pharmacology 16 18001707
1997 5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor. Journal of medicinal chemistry 16 9258356
2020 Antiproliferative Evaluation of Some 2-[2-(2-Phenylethenyl)-cyclopent-3-en-1-yl]-1,3-benzothiazoles: DFT and Molecular Docking Study. Chemistry & biodiversity 15 32141675
2015 Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198). ACS chemical neuroscience 15 26367173
2012 The in vivo antitumor effects on human COLO 205 cancer cells of the 4,7-dimethoxy-5-(2-propen-1-yl)-1,3-benzodioxole (apiole) derivative of 5-substituted 4,7-dimethoxy-5-methyl-l,3-benzodioxole (SY-1) isolated from the fruiting body of Antrodia camphorate. Journal of cancer research and therapeutics 15 23361270
2024 Discovery of 5-(Piperidin-4-yl)-1,2,4-oxadiazole Derivatives as a New Class of Human Caseinolytic Protease P Agonists for the Treatment of Hepatocellular Carcinoma. Journal of medicinal chemistry 14 38905539
2023 Discovery, Optimization, and Evaluation of Novel N-(Benzimidazol-5-yl)-1,3,4-thiadiazol-2-amine Analogues as Potent STAT3 Inhibitors for Cancer Treatment. Journal of medicinal chemistry 14 37594012
2021 Recognition of the inherently unstable H2A nucleosome by Swc2 is a major determinant for unidirectional H2A.Z exchange. Cell reports 14 34038732
2021 Chemical Modulation of the 1-(Piperidin-4-yl)-1,3-dihydro-2H-benzo[d]imidazole-2-one Scaffold as a Novel NLRP3 Inhibitor. Molecules (Basel, Switzerland) 14 34209843
2021 Design and Synthesis of (2-oxo-1,2-Dihydroquinolin-4-yl)-1,2,3-triazole Derivatives via Click Reaction: Potential Apoptotic Antiproliferative Agents. Molecules (Basel, Switzerland) 14 34833890
2020 Design and Optimization of 3'-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors. ACS medicinal chemistry letters 14 32184973
2020 Synthesis, characterization and biological activity of bromido[3-ethyl-4-aryl-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(i) complexes. Dalton transactions (Cambridge, England : 2003) 14 32255443
2020 Double mutation of two homologous genes YL1 and YL2 results in a leaf yellowing phenotype in soybean [Glycine max (L.) Merr]. Plant molecular biology 14 32323129
2012 Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors. Bioorganic & medicinal chemistry letters 14 23294702
2008 Pharmacological properties and discriminative stimulus effects of a novel and selective 5-HT2 receptor agonist AL-38022A [(S)-2-(8,9-dihydro-7H-pyrano[2,3-g]indazol-1-yl)-1-methylethylamine]. Pharmacology, biochemistry, and behavior 14 18718483
2020 Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine. Journal of medicinal chemistry 13 32558564
2020 N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms. Journal of medicinal chemistry 13 33256400
2017 Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone. Inflammopharmacology 13 28825161
2016 Radiosynthesis and preliminary PET evaluation of (18)F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors. Bioorganic & medicinal chemistry letters 13 27546294
2008 Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol. Bioorganic & medicinal chemistry letters 13 18774292
2001 Genomic organization of Tropomodulins 2 and 4 and unusual intergenic and intraexonic splicing of YL-1 and Tropomodulin 4. BMC genomics 13 11716785
2022 Vacuolar protein sorting-associated protein 72 homolog (VPS72) binding to lysine acetyltransferase 5 (KAT5) promotes the proliferation, invasion and migration of hepatocellular carcinoma through regulating phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) signaling pathway. Bioengineered 12 35383533
2022 3JC48-3 (methyl 4'-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate): a novel MYC/MAX dimerization inhibitor reduces prostate cancer growth. Cancer gene therapy 12 35440696
2019 Synthesis, Antimicrobial, and Anti-Proliferative Activities of Novel 4-(Adamantan-1-yl)-1-arylidene-3-thiosemicarbazides, 4-Arylmethyl N'-(Adamantan-1-yl)piperidine-1-carbothioimidates, and Related Derivatives. Molecules (Basel, Switzerland) 12 31779091
2011 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors. Bioorganic & medicinal chemistry letters 12 22154349
2010 {2-[1-(3-Methoxycarbonylmethyl-1H-indol-2-yl)-1-methyl-ethyl]-1H-indol-3-yl}-acetic acid methyl ester (MIAM): its anti-cancer efficacy and intercalation mechanism identified via multi-model systems. Molecular bioSystems 12 21116565
2006 1-(1-phenethylpiperidin-4-yl)-1-phenylethanols as potent and highly selective 5-HT2A antagonists. ChemMedChem 12 16892357
1995 Forced expression of YL-1 protein suppresses the anchorage-independent growth of Kirsten sarcoma virus-transformed NIH3T3 cells. Experimental cell research 12 7664828
2022 Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. Journal of medicinal chemistry 11 35584513
2022 Coumarin-4-yl-1,2,3-triazol-4-yl-methyl-thiazolidine-2,4-diones: Synthesis, glucose uptake activity and cytotoxic evaluation. Bioorganic chemistry 11 36375354
2020 Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors. European journal of medicinal chemistry 11 32171154
2017 Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives. Bioorganic & medicinal chemistry letters 11 28756024
2014 Synthesis and anti-HIV activity of 4-(naphthalen-1-yl)-1,2,5-thiadiazol-3-hydroxyl derivatives. Chemical biology & drug design 11 24674646
2000 Mutagenicity of the 1-nitropyrene-DNA adduct N-(deoxyguanosin-8-yl)-1-aminopyrene in Escherichia coli located in a nonrepetitive CGC sequence. Chemical research in toxicology 11 10858326
2023 Discovery of 1-(5-bromopyrazin-2-yl)-1-[3-(trifluoromethyl)benzyl]urea as a promising anticancer drug via synthesis, characterization, biological screening, and computational studies. Scientific reports 10 38129413
2021 Discovery of novel antituberculosis agents among 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazole derivatives targeting aminoacyl-tRNA synthetases. Scientific reports 10 33785838
2021 Use of Intramolecular 1,5-Sulfur-Oxygen and 1,5-Sulfur-Halogen Interactions in the Design of N-Methyl-5-aryl-N-(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators. Journal of medicinal chemistry 10 33822618
2017 The Analgesic Effects of (5R,6R)6-(3-Propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1] Octane on a Mouse Model of Neuropathic Pain. Anesthesia and analgesia 10 28002166
2016 Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor. European journal of medicinal chemistry 10 27814560
2004 Induction of nitric oxide production by the cytostatic macrolide apicularen A [2,4-heptadienamide, N-[(1E)-3-[(3S,5R,7R,9S)-3,4,5,6,7,8,9,10-octahydro-7,14 dihydroxy-1-oxo-5,9-epoxy-1H-2-benzoxacyclododecin-3-yl]-1 propenyl]-, (2Z,4Z)-(9CI)] and possible role of nitric oxide in apicularen A-induced apoptosis in RAW 264.7 cells. The Journal of pharmacology and experimental therapeutics 10 15561798
2022 GABAA receptor participation in anxiolytic and anticonvulsant effects of (E)-3-(furan-2-yl)-1-(2hydroxy-3,4,6-trimethoxyphenyl)prop-2-en-1-one in adult zebrafish. Neurochemistry international 9 35183661
2021 Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition. Bioorganic & medicinal chemistry letters 9 33887438
2021 Phenazine-1-carboxylic Acid Produced by Pseudomonas chlororaphis YL-1 Is Effective against Acidovorax citrulli. Microorganisms 9 34683333
2016 A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives. European journal of medicinal chemistry 9 27240274

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