Steven J. Charlton
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View article: SUN-432 Optimizing Binding Kinetics to Develop Insurmountable MC2 Receptor Antagonists for the Treatment of Congenital Adrenal Hyperplasia
SUN-432 Optimizing Binding Kinetics to Develop Insurmountable MC2 Receptor Antagonists for the Treatment of Congenital Adrenal Hyperplasia Open
Disclosure: L. Malet Sanz: OMass Therapeutics. M. Soave: OMass Therapeutics. K. Sengmany: OMass Therapeutics. U.R. Wilcox: OMass Therapeutics. M. Musgaard: OMass Therapeutics. K. Gherbi: OMass Therapeutics. M. Silva: None. A. Jazayeri: OMa…
View article: Development of a BRET based chloride biosensor for high throughput screening of KCC2 modulators
Development of a BRET based chloride biosensor for high throughput screening of KCC2 modulators Open
The generation of action potentials in neuronal cells and many other physiological processes involve the transport of chloride ions. Whilst there have been advances in chloride imaging techniques utilizing FRET biosensors, there is a lack …
View article: Identification of a Lipid-Exposed Extrahelical Binding Site for Positive Allosteric Modulators of the Dopamine D<sub>2</sub> Receptor
Identification of a Lipid-Exposed Extrahelical Binding Site for Positive Allosteric Modulators of the Dopamine D<sub>2</sub> Receptor Open
Recently, the first small-molecule positive allosteric modulators (PAMs) of the dopamine D2 receptor (D2R) were identified. The more potent PAM potentiated the effects of D2R signaling in vitro and in an in…
View article: Multiple polylogarithms and the Steinberg module
Multiple polylogarithms and the Steinberg module Open
We establish a connection between multiple polylogarithms on a torus and the Steinberg module of $\mathbb{Q}$, and show that multiple polylogarithms of depth $d$ and weight $n$ can be expressed via a single function $\mathrm{Li}_{n-d+1,1,\…
View article: Symmetry results for multiple t-values
Symmetry results for multiple t-values Open
For a composition I whose last part exceeds 1, we can define the multiple t -value t ( I ) as the sum of all the terms in the series for the multiple zeta value $$\zeta (I)$$ whose denominators are odd. In this paper we show that if …
View article: Explicit linear dependence congruence relations for the partition function modulo 4
Explicit linear dependence congruence relations for the partition function modulo 4 Open
Almost nothing is known about the parity of the partition function $p(n)$, which is conjectured to be random. Despite this expectation, Ono surprisingly proved the existence of infinitely many linear dependence congruence relations modulo …
View article: The Hopf algebra of multiple polylogarithms
The Hopf algebra of multiple polylogarithms Open
We define a Hopf algebra of polylogarithms of an infinite field, which is a candidate for a conjectural Hopf algebra of framed mixed Tate motives. Our definition is elementary and mimics Goncharov's construction of higher Bloch groups. We …
View article: Symmetries of weight 6 multiple polylogarithms and Goncharov's Depth Conjecture
Symmetries of weight 6 multiple polylogarithms and Goncharov's Depth Conjecture Open
We prove that the weight 6, depth 3, multiple polylogarithm $ \mathrm{Li}_{4,1,1}((xyz)^{-1}, x, y) $, or rather its more natural `divergent' incarnation $ \mathrm{Li}_{3;1,1,1}(x,y,z) $, satisfies the 6-fold anharmonic symmetries of the d…
View article: On the Goncharov depth conjecture and polylogarithms of depth two
On the Goncharov depth conjecture and polylogarithms of depth two Open
4 pages
View article: Differential operators and a depth reduction for the alternating multiple zeta values $ζ(1, \ldots, 1, \overline{2m})$
Differential operators and a depth reduction for the alternating multiple zeta values $ζ(1, \ldots, 1, \overline{2m})$ Open
We establish an identity amongst certain differential operators applied to a formal power-series. As a corollary we obtain an explicit depth reduction result for alternating MZV's of the form $ζ(1,\ldots,1,\overline{2m})$, which resolves a…
View article: Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2
Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2 Open
The inhibition of CXC chemokine receptor 2 (CXCR2), a key inflammatory mediator, is a potential strategy in the treatment of several pulmonary diseases and cancers. The complexity of endogenous chemokine interaction with the orthosteric bi…
View article: CCDC 2248014: Experimental Crystal Structure Determination
CCDC 2248014: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor
Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor Open
View article: On the Goncharov Depth Conjecture and polylogarithms of depth two
On the Goncharov Depth Conjecture and polylogarithms of depth two Open
We prove the surjectivity part of Goncharov's depth conjecture. We also show that the depth conjecture implies that multiple polylogarithms of depth $d$ and weight $n$ can be expressed via a single function $\mathrm{Li}_{n-d+1,1,\dots,1}(a…
View article: On two conjectures of Sun concerning Apéry-like series
On two conjectures of Sun concerning Apéry-like series Open
In this paper, we shall prove two conjectures of Z.-W. Sun concerning Apéry-like series. One of the series is alternating whereas the other one is not. Our main strategy is to convert the series (resp.~the alternating series) to log-sine-c…
View article: Evaluation of the multiple zeta values $ζ(2,\ldots,2,4,2,\ldots,2)$ and period polynomial relations
Evaluation of the multiple zeta values $ζ(2,\ldots,2,4,2,\ldots,2)$ and period polynomial relations Open
In studying the depth filtration on multiple zeta values, difficulties quickly arise due to a disparity between it and the coradical filtration. In particular, there are additional relations in the depth graded algebra coming from period p…
View article: Exploring the kinetic selectivity of drugs targeting the β <sub>1</sub> ‐adrenoceptor
Exploring the kinetic selectivity of drugs targeting the β <sub>1</sub> ‐adrenoceptor Open
In this study, we report the β 1 ‐adrenoceptor binding kinetics of several clinically relevant β 1/2 ‐adrenoceptor (β 1/2 AR) agonists and antagonists. [ 3 H]‐DHA was used to label CHO‐β 1 AR for binding studies. The kinetics of ligand bin…
View article: Symmetry results for multiple $t$-values
Symmetry results for multiple $t$-values Open
For a composition $I$ whose first part exceeds 1, we can define the multiple $t$-value $t(I)$ as the sum of all the terms in the series for the multiple zeta value $ζ(I)$ whose denominators are odd. In this paper we show that if $I$ is com…
View article: Interaction With the Lipid Membrane Influences Fentanyl Pharmacology
Interaction With the Lipid Membrane Influences Fentanyl Pharmacology Open
Overdose deaths from fentanyl have reached epidemic proportions in the USA and are increasing worldwide. Fentanyl is a potent opioid agonist that is less well reversed by naloxone than morphine. Due to fentanyl’s high lipophilicity and elo…
View article: On the evaluation of the alternating multiple $t$ value $t(\{\overline{1}\}^a, 1, \{\overline{1}\}^b)$
On the evaluation of the alternating multiple $t$ value $t(\{\overline{1}\}^a, 1, \{\overline{1}\}^b)$ Open
We prove an evaluation for the stuffle-regularised multiple $t$ value $ t^{\ast,V}(\{\overline{1}\}^a, 1, \{\overline{1}\}^b) $ in terms of $ \log(2) $, $ ζ(k) $ and $ β(k) $. This arises by evaluating the corresponding generating series u…
View article: On motivic multiple $t$ values, Saha's basis conjecture, and generators of alternating MZV's
On motivic multiple $t$ values, Saha's basis conjecture, and generators of alternating MZV's Open
We give an evaluation for the stuffle-regularised $t^{\ast,V}(\{2\}^a,1,\{2\}^b)$ as a polynomial in single-zeta values, $\log(2)$ and $V$. We then apply this to establish some linear independence results of certain sets of motivic multipl…
View article: Exploring the kinetic selectivity of antipsychotics for dopamine D<sub>2</sub> and 5-HT<sub>2A</sub> receptors: implications for the prevalence of EPS and receptor occupancy
Exploring the kinetic selectivity of antipsychotics for dopamine D<sub>2</sub> and 5-HT<sub>2A</sub> receptors: implications for the prevalence of EPS and receptor occupancy Open
Certain atypical antipsychotic drugs (APDs) used in the treatment of schizophrenia have been hypothesized to show reduced extrapyramidal side effects (EPS), due to their ability to promote nigrostriatal dopamine release through 5-HT 2A rec…
View article: Exploring the kinetic selectivity of drugs targeting the β<sub>1</sub>-adrenoceptor
Exploring the kinetic selectivity of drugs targeting the β<sub>1</sub>-adrenoceptor Open
In this study, we report the β 1 -adrenoceptor binding kinetics of several clinically relevant β 1/2 -adrenoceptor (β 1/2 AR) agonists and antagonists. We demonstrate that the physicochemical properties of a molecule directly affect its ki…
View article: Inhibition of the Proliferation of Human Lung Fibroblasts by Prostacyclin Receptor Agonists is Linked to a Sustained cAMP Signal in the Nucleus
Inhibition of the Proliferation of Human Lung Fibroblasts by Prostacyclin Receptor Agonists is Linked to a Sustained cAMP Signal in the Nucleus Open
Idiopathic pulmonary fibrosis is a chronic and progressive fibrotic lung disease, and current treatments are limited by their side effects. Proliferation of human lung fibroblasts in the pulmonary interstitial tissue is a hallmark of this …
View article: Fentanyl binds to the μ-opioid receptor via the lipid membrane and transmembrane helices
Fentanyl binds to the μ-opioid receptor via the lipid membrane and transmembrane helices Open
Overdose deaths from synthetic opioids, such as fentanyl, have reached epidemic proportions in the USA and are increasing worldwide. Fentanyl is a potent opioid agonist, that is less well reversed by naloxone than morphine. Due to fentanyl…
View article: Functional equations of polygonal type for multiple polylogarithms in weights 5, 6 and 7
Functional equations of polygonal type for multiple polylogarithms in weights 5, 6 and 7 Open
We present new functional equations in weights 5, 6 and 7 and use them for explicit depth reduction of multiple polylogarithms. These identities generalize the crucial identity $\mathbf{Q}_4$ from the recent work of Goncharov and Rudenko t…
View article: Structure–Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D<sub>2</sub> Receptor
Structure–Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D<sub>2</sub> Receptor Open
Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side effects (EPSs) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D…
View article: Generalized Jacobi-Trudi determinants and evaluations of Schur multiple\n zeta values
Generalized Jacobi-Trudi determinants and evaluations of Schur multiple\n zeta values Open
We present new determinant expressions for regularized Schur multiple zeta\nvalues. These generalize the known Jacobi-Trudi formulae and can be used to\nquickly evaluate certain types of Schur multiple zeta values. Using these\nformulae we…
View article: Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds
Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds Open
View article: Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies
Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies Open
The anabolic effects of β 2-adrenoceptor (β 2-AR) agonists on skeletal muscle have been demonstrated in various species. However, the clinical use of β 2-AR agonists for skeletal muscle…