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1

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Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models

Digby, G. J. ; Noetzel, M. J. ; Bubser, M. ; [et al.]

Society for Neuroscience ; 2012

In: Journal of Neuroscience Vol. 32, No. 25 ( 2012-06-20), p. 8532-8544

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In: Journal of Neuroscience, Society for Neuroscience, Vol. 32, No. 25 ( 2012-06-20), p. 8532-8544

Type of Medium: Online Resource

ISSN: 0270-6474 , 1529-2401

URL: Article

DOI: 10.1523/JNEUROSCI.0337-12.2012

Language: English

Publisher: Society for Neuroscience

Publication Date: 2012

detail.hit.zdb_id: 1475274-8

SSG: 12

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2

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Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies

Davies, M A ; Setola, V ; Strachan, R T ; [et al.]

Springer Science and Business Media LLC ; 2006

In: The Pharmacogenomics Journal Vol. 6, No. 1 ( 2006-01-01), p. 42-51

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In: The Pharmacogenomics Journal, Springer Science and Business Media LLC, Vol. 6, No. 1 ( 2006-01-01), p. 42-51

Type of Medium: Online Resource

ISSN: 1470-269X , 1473-1150

URL: Article

DOI: 10.1038/sj.tpj.6500342

Language: English

Publisher: Springer Science and Business Media LLC

Publication Date: 2006

detail.hit.zdb_id: 2051501-7

SSG: 15,3

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3

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Computational design of mechanically coupled axle-rotor protein assemblies

Courbet, A. ; Hansen, J. ; Hsia, Y. ; [et al.]

American Association for the Advancement of Science (AAAS) ; 2022

In: Science Vol. 376, No. 6591 ( 2022-04-22), p. 383-390

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In: Science, American Association for the Advancement of Science (AAAS), Vol. 376, No. 6591 ( 2022-04-22), p. 383-390

Abstract: Computationally designed self-assembling axle-rotor protein systems populate multiple rotational states.

Type of Medium: Online Resource

ISSN: 0036-8075 , 1095-9203

URL: Article

DOI: 10.1126/science.abm1183

RVK:

TA 1000

RVK:

WA 15000

Language: English

Publisher: American Association for the Advancement of Science (AAAS)

Publication Date: 2022

detail.hit.zdb_id: 128410-1

detail.hit.zdb_id: 2066996-3

detail.hit.zdb_id: 2060783-0

SSG: 11

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4

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Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor

Melancon, Bruce J. ; Gogliotti, Rocco D. ; Tarr, James C. ; [et al.]

Elsevier BV ; 2012

In: Bioorganic & Medicinal Chemistry Letters Vol. 22, No. 10 ( 2012-5), p. 3467-3472

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In: Bioorganic & Medicinal Chemistry Letters, Elsevier BV, Vol. 22, No. 10 ( 2012-5), p. 3467-3472

Type of Medium: Online Resource

ISSN: 0960-894X

URL: Article

DOI: 10.1016/j.bmcl.2012.03.088

RVK:

VA 2620

Language: English

Publisher: Elsevier BV

Publication Date: 2012

detail.hit.zdb_id: 1501505-1

SSG: 15,3

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5

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Design, Synthesis and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer

Ren, Huiyu ; Bakas, Nicole A. ; Vamos, Mitchell ; [et al.]

American Chemical Society (ACS) ; 2020

In: Journal of Medicinal Chemistry Vol. 63, No. 23 ( 2020-12-10), p. 14609-14625

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In: Journal of Medicinal Chemistry, American Chemical Society (ACS), Vol. 63, No. 23 ( 2020-12-10), p. 14609-14625

Type of Medium: Online Resource

ISSN: 0022-2623 , 1520-4804

URL: Article

DOI: 10.1021/acs.jmedchem.0c00873

DOI: 10.1021/acs.jmedchem.0c00873.s001

Language: English

Publisher: American Chemical Society (ACS)

Publication Date: 2020

detail.hit.zdb_id: 1491411-6

SSG: 15,3

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6

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Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012

Melancon, Bruce J. ; Lamers, Alexander P. ; Bridges, Thomas M. ; [et al.]

Elsevier BV ; 2012

In: Bioorganic & Medicinal Chemistry Letters Vol. 22, No. 2 ( 2012-01), p. 1044-1048

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In: Bioorganic & Medicinal Chemistry Letters, Elsevier BV, Vol. 22, No. 2 ( 2012-01), p. 1044-1048

Type of Medium: Online Resource

ISSN: 0960-894X

URL: Article

DOI: 10.1016/j.bmcl.2011.11.110

RVK:

VA 2620

Language: English

Publisher: Elsevier BV

Publication Date: 2012

detail.hit.zdb_id: 1501505-1

SSG: 15,3

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7

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Enhancing and shaping the immunogenicity of native-like HIV-1 envelope trimers with a two-component protein nanoparticle

Brouwer, Philip J. M. ; Antanasijevic, Aleksandar ; Berndsen, Zachary ; [et al.]

Springer Science and Business Media LLC ; 2019

In: Nature Communications Vol. 10, No. 1 ( 2019-09-19)

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In: Nature Communications, Springer Science and Business Media LLC, Vol. 10, No. 1 ( 2019-09-19)

Abstract: The development of native-like HIV-1 envelope (Env) trimer antigens has enabled the induction of neutralizing antibody (NAb) responses against neutralization-resistant HIV-1 strains in animal models. However, NAb responses are relatively weak and narrow in specificity. Displaying antigens in a multivalent fashion on nanoparticles (NPs) is an established strategy to increase their immunogenicity. Here we present the design and characterization of two-component protein NPs displaying 20 stabilized SOSIP trimers from various HIV-1 strains. The two-component nature permits the incorporation of exclusively well-folded, native-like Env trimers into NPs that self-assemble in vitro with high efficiency. Immunization studies show that the NPs are particularly efficacious as priming immunogens, improve the quality of the Ab response over a conventional one-component nanoparticle system, and are most effective when SOSIP trimers with an apex-proximate neutralizing epitope are displayed. Their ability to enhance and shape the immunogenicity of SOSIP trimers make these NPs a promising immunogen platform.

Type of Medium: Online Resource

ISSN: 2041-1723

URL: Article

DOI: 10.1038/s41467-019-12080-1

Language: English

Publisher: Springer Science and Business Media LLC

Publication Date: 2019

detail.hit.zdb_id: 2553671-0

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8

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Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012

Melancon, Bruce J. ; Utley, Thomas J. ; Sevel, Christian ; [et al.]

Elsevier BV ; 2012

In: Bioorganic & Medicinal Chemistry Letters Vol. 22, No. 15 ( 2012-8), p. 5035-5040

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In: Bioorganic & Medicinal Chemistry Letters, Elsevier BV, Vol. 22, No. 15 ( 2012-8), p. 5035-5040

Type of Medium: Online Resource

ISSN: 0960-894X

URL: Article

DOI: 10.1016/j.bmcl.2012.06.018

RVK:

VA 2620

Language: English

Publisher: Elsevier BV

Publication Date: 2012

detail.hit.zdb_id: 1501505-1

SSG: 15,3

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9

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Targeting Selective Activation of M 1 for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M 1 Positive Allosteric Modulator ML169

Tarr, James C. ; Turlington, Mark L. ; Reid, Paul R. ; [et al.]

American Chemical Society (ACS) ; 2012

In: ACS Chemical Neuroscience Vol. 3, No. 11 ( 2012-11-21), p. 884-895

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In: ACS Chemical Neuroscience, American Chemical Society (ACS), Vol. 3, No. 11 ( 2012-11-21), p. 884-895

Type of Medium: Online Resource

ISSN: 1948-7193 , 1948-7193

URL: Article

DOI: 10.1021/cn300068s

Language: English

Publisher: American Chemical Society (ACS)

Publication Date: 2012

detail.hit.zdb_id: 2528493-9

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10

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Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM

Sheffler, Douglas J. ; Wenthur, Cody J. ; Bruner, Joshua A. ; [et al.]

Elsevier BV ; 2012

In: Bioorganic & Medicinal Chemistry Letters Vol. 22, No. 12 ( 2012-06), p. 3921-3925

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In: Bioorganic & Medicinal Chemistry Letters, Elsevier BV, Vol. 22, No. 12 ( 2012-06), p. 3921-3925

Type of Medium: Online Resource

ISSN: 0960-894X

URL: Article

DOI: 10.1016/j.bmcl.2012.04.112

RVK:

VA 2620

Language: English

Publisher: Elsevier BV

Publication Date: 2012

detail.hit.zdb_id: 1501505-1

SSG: 15,3

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