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Auteur : Grafiati
Publié le 11 mars 2023

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1

Fauceglia, Domenico. « Nullità e conformazione dei contratti di impresa ad opera delle autorità indipendenti = Nullity and conformation of business contracts by authorities ». CUADERNOS DE DERECHO TRANSNACIONAL 10, no 2 (5 octobre 2018) : 306. http://dx.doi.org/10.20318/cdt.2018.4379.

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Riassunto: Sin dall’avvento nel sistema istituzionale italiano delle c.d. Autorità indipendenti, al-le quali è attribuito il potere di regolare settori sensibili del mercato (domain sensibles), si è posta l’attenzione sulla particolare interferenza tra regolazione del mercato e di-sciplina dei contratti. In parti­colare, le Autorità indipendenti godono di un potere re-golamentare abbastanza variegato: la legge attri­buisce alle Authorities i poteri di defi-nire i procedimenti di formazione e conclusione, nonché la forma e il contenuto mi-nimo dei contratti. In relazione a questi ultimi poteri, si cercherà, con tale contributo, di esaminare le ipotesi di nullità negoziale derivanti dalla difformità dei contratti ri-spetto ai regolamenti delle Autorità Indipendenti, nonché le ipotesi di eteroregola-mentazione dei contratti ad opera dei rego­lamenti delle Autorità Indipendenti.Parole chiavi: contratto, mercato, autorità indipendenti, nullità dei contratti, integrazione contrat-tuale, contratti d’impresa, contratti bancari, contratti finanziari.Abstract: Since the inclusion in the Italian institutional system of the c.d. Independent authori-ties, which are given the power to regulate sensitive sectors of the market (domain sensibles), attention has been focused on the particular interference between market regulation and contract discipline. In particular, the Authorities have quite a varied regulatory power: the law gives the Authorities the power to define the starting and conclusion procedures, as well as the form and minimum content of the con­tracts. In relation to these last powers, we will try, with this contribution, to examine the hy-pothesis of negotiation nullity deriving from the non-conformity of the contracts with the regulations of the Inde­pendent Authorities, as well as the hypothesis of external regulation of the contracts by the regulations of Independent Authorities.Keywords: contract, market, independent authorities, nullity of contracts, contractual inte-gration, business contract, banking contracts, financial contracts.
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Hu, Wei-Gang, Junfei Yin, Damon Chau, Charles Chen Hu, Dustin Lillico, Justin Yu, Laurel M. Negrych et John W. Cherwonogrodzky. « Conformation-Dependent High-Affinity Potent Ricin-Neutralizing Monoclonal Antibodies ». BioMed Research International 2013 (2013) : 1–9. http://dx.doi.org/10.1155/2013/471346.

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Ricin is a potential biothreat agent with no approved antidote available for ricin poisoning. The aim of this study was to develop potent antibody-based antiricin antidotes. Four strong ricin resistant hybridoma clones secreting antiricin monoclonal antibodies (mAbs) were developed. All four mAbs are bound to conformational epitopes of ricin toxin B (RTB) with high affinity (KDvalues from 2.55 to 36.27 nM). RTB not only triggers cellular uptake of ricin, but also facilitates transport of the ricin toxin A (RTA) from the endoplasmic reticulum to the cytosol, where RTA exerts its toxic activity. The four mAbs were found to have potent ricin-neutralizing capacities and synergistic effects among them as determined by anin vitroneutralization assay.In vivoprotection assay demonstrated that all four mAbs had strong efficacy against ricin challenges. D9 was found to be exceptionally effective. Intraperitoneal (i.p.) administration of D9, at a dose of 5 μg, 6 weeks before or 6 hours after an i.p. challenge with 5 × LD50 of ricin was able to protect or rescue 100% of the mice, indicating that mAb D9 is an excellent candidate to be developed as a potent antidote against ricin poisoning for both prophylactic and therapeutic purposes.
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Pukin, Aliaksei V., Arwin J. Brouwer, Leonie Koomen, H. C. Quarles van Ufford, Johan Kemmink, Nico J. de Mol et Roland J. Pieters. « Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA ». Organic & ; Biomolecular Chemistry 13, no 44 (2015) : 10923–28. http://dx.doi.org/10.1039/c5ob01452b.

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GURRATH, Marion, Gerhard MULLER, Horst KESSLER, Monique AUMAILLEY et Rupert TIMPL. « Conformation/activity studies of rationally designed potent anti-adhesive RGD peptides ». European Journal of Biochemistry 210, no 3 (décembre 1992) : 911–21. http://dx.doi.org/10.1111/j.1432-1033.1992.tb17495.x.

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Houdai, Toshihiro, Shigeru Matsuoka, Nagy Morsy, Nobuaki Matsumori, Masayuki Satake et Michio Murata. « Hairpin conformation of amphidinols possibly accounting for potent membrane permeabilizing activities ». Tetrahedron 61, no 11 (mars 2005) : 2795–802. http://dx.doi.org/10.1016/j.tet.2005.01.069.

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Naveen, S., Sridhar M. Anandalwar, J. Shashidhara Prasad, Dinesh Manvar, Arun Mishra et Anamik Shah. « Synthesis and Structural Conformation Studies of a Potent Unsymmetrical 1,4-Dihydropyridine ». Journal of Chemical Crystallography 38, no 4 (29 janvier 2008) : 315–19. http://dx.doi.org/10.1007/s10870-008-9314-1.

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Rizo, Josep, R. Bryan Sutton, Joshua Breslau, Steven C. Koerber, John Porter, Arnold T. Hagler, Jean E. Rivier et Lila M. Gierasch. « A Novel Conformation in a Highly Potent, Constrained Gonadotropin-Releasing Hormone Antagonist ». Journal of the American Chemical Society 118, no 5 (janvier 1996) : 970–76. http://dx.doi.org/10.1021/ja953207e.

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Yamagat, Yuriko, Ken-ichi Tomita, Nobuhiro Marubayashi, Ikuhiko Ueda, Shinji Sakata, Akira Matsuda, Kenji Takenuki et Tohru Ueda. « Molecular Conformation of 2′-Deoxy-2′-methylidene-cytidine : A Potent Antineoplastic Nucleoside ». Nucleosides and Nucleotides 11, no 2-4 (février 1992) : 835–53. http://dx.doi.org/10.1080/07328319208021744.

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Maia, Angélica Faleiros da Silva, Felipe T. Martins, Leonardo da Silva Neto, Rosemeire Brondi Alves et Ângelo De Fátima. « Cocaethylene, the in vivo product of cocaine and ethanol, is a narcotic more potent than its precursors ». Acta Crystallographica Section C Structural Chemistry 73, no 10 (20 septembre 2017) : 780–83. http://dx.doi.org/10.1107/s2053229617012852.

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The molecular conformation and supramolecular architecture of cocaethylene [systematic name: ethyl (1R,2R,3S,5S)-3-benzoyloxy-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate], C18H23NO4, have been determined for the first time. Cocaethylene is a narcotic produced in vivo when cocaine and ethanol are administered concomitantly. The intra- and intermolecular features of cocaethylene and its less potent narcotic precursor cocaine are very similar. The only molecular difference is in the conformation of the methyl group of the ethoxycarbonyl group. Similar to cocaine, the carboxylate atoms and the α-C atom are coplanar in cocaethylene, but the methyl C atom of the ethyl group is bent by ca 90° away from this plane in the narcotic reported here. The main supramolecular motif is a one-dimensional chain stabilized by weak C—H...O contacts.
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Amorim-Carmo, Bruno, Alessandra Daniele-Silva, Adriana M. S. Parente, Allanny A. Furtado, Eneas Carvalho, Johny W. F. Oliveira, Elizabeth C. G. Santos et al. « Potent and Broad-Spectrum Antimicrobial Activity of Analogs from the Scorpion Peptide Stigmurin ». International Journal of Molecular Sciences 20, no 3 (31 janvier 2019) : 623. http://dx.doi.org/10.3390/ijms20030623.

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Scorpion venom constitutes a rich source of biologically active compounds with high potential for therapeutic and biotechnological applications that can be used as prototypes for the design of new drugs. The aim of this study was to characterize the structural conformation, evaluate the antimicrobial activity, and gain insight into the possible action mechanism underlying it, for two new analog peptides of the scorpion peptide Stigmurin, named StigA25 and StigA31. The amino acid substitutions in the native sequence for lysine residues resulted in peptides with higher positive net charge and hydrophobicity, with an increase in the theoretical helical content. StigA25 and StigA31 showed the capacity to modify their structural conformation according to the environment, and were stable to pH and temperature variation—results similar to the native peptide. Both analog peptides demonstrated broad-spectrum antimicrobial activity in vitro, showing an effect superior to that of the native peptide, being non-hemolytic at the biologically active concentrations. Therefore, this study demonstrates the therapeutic potential of the analog peptides from Stigmurin and the promising approach of rational drug design based on scorpion venom peptide to obtain new anti-infective agents.
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Glauser, Daniel L., Anne-Sophie Kratz, Laurent Gillet et Philip G. Stevenson. « A mechanistic basis for potent, glycoprotein B-directed gammaherpesvirus neutralization ». Journal of General Virology 92, no 9 (1 septembre 2011) : 2020–33. http://dx.doi.org/10.1099/vir.0.032177-0.

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Glycoprotein B (gB) is a conserved, essential component of gammaherpes virions and so potentially vulnerable to neutralization. However, few good gB-specific neutralizing antibodies have been identified. Here, we show that murid herpesvirus 4 is strongly neutralized by mAbs that recognize an epitope close to one of the gB fusion loops. Antibody binding did not stop gB interacting with its cellular ligands or initiating its fusion-associated conformation change, but did stop gB resolving stably to its post-fusion form, and so blocked membrane fusion to leave virions stranded in late endosomes. The conservation of gB makes this mechanism a possible general route to gammaherpesvirus neutralization.
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Ishida, Michiko, et Haruhiko Shinozaki. « Glutamate receptor subtypes and conformation of glutamate agonists : Discovery of new potent agonists ». Japanese Journal of Pharmacology 49 (1989) : 308. http://dx.doi.org/10.1016/s0021-5198(19)56761-0.

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Bacsa, John, Maurice Okello, Pankaj Singh et Vasu Nair. « Solid-state tautomeric structure and invariom refinement of a novel and potent HIV integrase inhibitor ». Acta Crystallographica Section C Crystal Structure Communications 69, no 3 (14 février 2013) : 285–88. http://dx.doi.org/10.1107/s0108270113003806.

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The conformation and tautomeric structure of (Z)-4-[5-(2,6-difluorobenzyl)-1-(2-fluorobenzyl)-2-oxo-1,2-dihydropyridin-3-yl]-4-hydroxy-2-oxo-N-(2-oxopyrrolidin-1-yl)but-3-enamide, C27H22F3N3O5, in the solid state has been resolved by single-crystal X-ray crystallography. The electron distribution in the molecule was evaluated by refinements with invarioms, aspherical scattering factors by the method of Dittrichet al.[Acta Cryst.(2005), A61, 314–320] that are based on the Hansen–Coppens multipole model [Hansen & Coppens (1978).Acta Cryst.A34, 909–921]. The β-diketo portion of the molecule exists in the enol form. The enol –OH hydrogen forms a strong asymmetric hydrogen bond with the carbonyl O atom on the β-C atom of the chain. Weak intramolecular hydrogen bonds exist between the weakly acidic α-CH hydrogen of the keto–enol group and the pyridinone carbonyl O atom, and also between the hydrazine N—H group and the carbonyl group in the β-position from the hydrazine N—H group. The electrostatic properties of the molecule were derived from the molecular charge density. The molecule is in a lengthened conformation and the rings of the two benzyl groups are nearly orthogonal. Results from a high-field1H and13C NMR correlation spectroscopy study confirm that the same tautomer exists in solution as in the solid state.
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Lee, Won-Gil, Albert H. Chan, Krasimir A. Spasov, Karen S. Anderson et William L. Jorgensen. « Design, Conformation, and Crystallography of 2-Naphthyl Phenyl Ethers as Potent Anti-HIV Agents ». ACS Medicinal Chemistry Letters 7, no 12 (novembre 2016) : 1156–60. http://dx.doi.org/10.1021/acsmedchemlett.6b00390.

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Miyahara, Seiji, Hitoshi Miyakoshi, Tatsushi Yokogawa, Khoon Tee Chong, Junko Taguchi, Toshiharu Muto, Kanji Endoh et al. « Discovery of Highly Potent Human Deoxyuridine Triphosphatase Inhibitors Based on the Conformation Restriction Strategy ». Journal of Medicinal Chemistry 55, no 11 (30 mai 2012) : 5483–96. http://dx.doi.org/10.1021/jm300416h.

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Xiong, Xiaoli, Davide Corti, Junfeng Liu, Debora Pinna, Mathilde Foglierini, Lesley J. Calder, Stephen R. Martin et al. « Structures of complexes formed by H5 influenza hemagglutinin with a potent broadly neutralizing human monoclonal antibody ». Proceedings of the National Academy of Sciences 112, no 30 (13 juillet 2015) : 9430–35. http://dx.doi.org/10.1073/pnas.1510816112.

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H5N1 avian influenza viruses remain a threat to public health mainly because they can cause severe infections in humans. These viruses are widespread in birds, and they vary in antigenicity forming three major clades and numerous antigenic variants. The most important features of the human monoclonal antibody FLD194 studied here are its broad specificity for all major clades of H5 influenza HAs, its high affinity, and its ability to block virus infection, in vitro and in vivo. As a consequence, this antibody may be suitable for anti-H5 therapy and as a component of stockpiles, together with other antiviral agents, for health authorities to use if an appropriate vaccine was not available. Our mutation and structural analyses indicate that the antibody recognizes a relatively conserved site near the membrane distal tip of HA, near to, but distinct from, the receptor-binding site. Our analyses also suggest that the mechanism of infectivity neutralization involves prevention of receptor recognition as a result of steric hindrance by the Fc part of the antibody. Structural analyses by EM indicate that three Fab fragments are bound to each HA trimer. The structure revealed by X-ray crystallography is of an HA monomer bound by one Fab. The monomer has some similarities to HA in the fusion pH conformation, and the monomer’s formation, which results from the presence of isopropanol in the crystallization solvent, contributes to considerations of the process of change in conformation required for membrane fusion.
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Reifenberger, Matthew S., Krista L. Arnett, Craig Gatto et Mark A. Milanick. « The reactive nitrogen species peroxynitrite is a potent inhibitor of renal Na-K-ATPase activity ». American Journal of Physiology-Renal Physiology 295, no 4 (octobre 2008) : F1191—F1198. http://dx.doi.org/10.1152/ajprenal.90296.2008.

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Peroxynitrite is a reactive nitrogen species produced when nitric oxide and superoxide react. In vivo studies suggest that reactive oxygen species and, perhaps, peroxynitrite can influence Na-K-ATPase function. However, the direct effects of peroxynitrite on Na-K-ATPase function remain unknown. We show that a single bolus addition of peroxynitrite inhibited purified renal Na-K-ATPase activity, with IC50 of 107 ± 9 μM. To mimic cellular/physiological production of peroxynitrite, a syringe pump was used to slowly release (∼0.85 μM/s) peroxynitrite. The inhibition of Na-K-ATPase activity induced by this treatment was similar to that induced by a single bolus addition of equal cumulative concentration. Peroxynitrite produced 3-nitrotyrosine residues on the α, β, and FXYD subunits of the Na pump. Interestingly, the flavonoid epicatechin, which prevented tyrosine nitration, was unable to blunt peroxynitrite-induced ATPase inhibition, suggesting that tyrosine nitration is not required for inhibition. Peroxynitrite led to a decrease in iodoacetamidofluorescein labeling, implying that cysteine modifications were induced. Glutathione was unable to reverse ATPase inhibition. The presence of Na+ and low MgATP during peroxynitrite treatment increased the IC50 to 145 ± 10 μM, while the presence of K+ and low MgATP increased the IC50 to 255 ± 13 μM. This result suggests that the EPNa conformation of the pump is slightly more sensitive to peroxynitrite than the E(K) conformation. Taken together, these results show that peroxynitrite is a potent inhibitor of Na-K-ATPase activity and that peroxynitrite can induce amino acid modifications to the pump.
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Kusakabe, Ken-ichi, Nobuyuki Ide, Yataro Daigo, Takeshi Itoh, Kenichi Higashino, Yousuke Okano, Genta Tadano et al. « Diaminopyridine-Based Potent and Selective Mps1 Kinase Inhibitors Binding to an Unusual Flipped-Peptide Conformation ». ACS Medicinal Chemistry Letters 3, no 7 (7 juin 2012) : 560–64. http://dx.doi.org/10.1021/ml3000879.

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Pulz, Robert, Daniela Angst, Janet Dawson, Francois Gessier, Sascha Gutmann, Rene Hersperger, Alexandra Hinniger et al. « Design of Potent and Selective Covalent Inhibitors of Bruton’s Tyrosine Kinase Targeting an Inactive Conformation ». ACS Medicinal Chemistry Letters 10, no 10 (6 septembre 2019) : 1467–72. http://dx.doi.org/10.1021/acsmedchemlett.9b00317.

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Chi, Seung-Wook, Kyu-Hwan Park, Jae-Eun Suk, Baldomero M. Olivera, J. Michael McIntosh et Kyou-Hoon Han. « Solution Conformation of αA-conotoxin EIVA, a Potent Neuromuscular Nicotinic Acetylcholine Receptor Antagonist fromConus ermineus ». Journal of Biological Chemistry 278, no 43 (4 août 2003) : 42208–13. http://dx.doi.org/10.1074/jbc.m303342200.

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CHI, Seung-Wook, Do-Hyoung KIM, Baldomero M. OLIVERA, J. Michael McINTOSH et Kyou-Hoon HAN. « Solution conformation of alpha-conotoxin GIC, a novel potent antagonist of alpha3beta2 nicotinic acetylcholine receptors ». Biochemical Journal 380, no 2 (1 juin 2004) : 347–52. http://dx.doi.org/10.1042/bj20031792.

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α-Conotoxin GIC is a 16-residue peptide isolated from the venom of the cone snail Conus geographus. α-Conotoxin GIC potently blocks the α3β2 subtype of human nicotinic acetylcholine receptor, showing a high selectivity for neuronal versus muscle subtype [McIntosh, Dowell, Watkins, Garrett, Yoshikami, and Olivera (2002) J. Biol. Chem. 277, 33610–33615]. We have now determined the three-dimensional solution structure of α-conotoxin GIC by NMR spectroscopy. The structure of α-conotoxin GIC is well defined with backbone and heavy atom root mean square deviations (residues 2–16) of 0.53 Å and 0.96 Å respectively. Structure and surface comparison of α-conotoxin GIC with the other α4/7 subfamily conotoxins reveals unique structural aspects of α-conotoxin GIC. In particular, the structural comparison between α-conotoxins GIC and MII indicates molecular features that may confer their similar receptor specificity profile, as well as those that provide the unique binding characteristics of α-conotoxin GIC.
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ARORA, S. K., et P. ARJUNAN. « Molecular structure and conformation of rifamycin S, a potent inhibitor of DNA-dependent RNA polymerase. » Journal of Antibiotics 45, no 3 (1992) : 428–31. http://dx.doi.org/10.7164/antibiotics.45.428.

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Kümmerle, Arthur E., Juliana M. Raimundo, Carla M. Leal, Givanildo S. da Silva, Tatiane L. Balliano, Mariano A. Pereira, Carlos A. de Simone, Roberto T. Sudo, Gisele Zapata-Sudo et Carlos A. M. Fraga. « Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives ». European Journal of Medicinal Chemistry 44, no 10 (octobre 2009) : 4004–9. http://dx.doi.org/10.1016/j.ejmech.2009.04.044.

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Bogusky, Michael J., Adel M. Naylor, Michael E. Mertzman, Steven M. Pitzenberger, Ruth F. Nutt, Stephen F. Brady, Christiane D. Colton et Daniel F. Veber. « The solution conformation Ac-Pen-Arg-Gly-Asp-Cys-OH, a potent fibrinogen receptor antagonist ». Biopolymers 33, no 8 (août 1993) : 1287–97. http://dx.doi.org/10.1002/bip.360330813.

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Theansungnoen, Tinnakorn, Santi Phosri, Sureewan Bumrungthai, Jureerut Daduang, Sompong Klaynongsruang et Sakda Daduang. « Novel non-cytotoxic antimicrobial peptides WSKK11 and WSRR11 with potent activity against Cutibacterium acnes ». Journal of Antimicrobial Chemotherapy 77, no 4 (28 janvier 2022) : 1012–19. http://dx.doi.org/10.1093/jac/dkac014.

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Abstract Objectives Cutibacterium acnes is one of the common multifactorial causes that play an important role in the pathophysiology of acne vulgaris. We aimed to develop novel antimicrobial peptides for reduction of the hypercolonization. Methods Six cationic peptides were derived by de novo designation. The antimicrobial and cytotoxic activities of peptides were investigated. The peptide conformation was determined by circular dichroism spectrometry. The antimicrobial effects of peptides were evaluated using scanning electron microscopy (SEM), transmission electron microscopy (TEM) and DNA-binding ability assay. Results Among designed peptides, WSKK11 and WSRR11 were effective antimicrobials against C. acnes at MICs of 128 and 64 mg/L, respectively. The MICs of WSKK11 against Staphylococcus epidermidis, Staphylococcus aureus and Candida albicans were 8, 8 and 32 mg/L, while those of WSRR11 were 64, 32 and 32 mg/L, respectively. WSKK11 and WSRR11 were less toxic to human erythrocytes (<2%) and not toxic to macrophages, keratinocytes and fibroblasts up to 512 mg/L. WSKK11 and WSRR11 mostly revealed the conformation of the undefined or random coil structures under mimicked environmental conditions. The peptides affected cell surfaces and cell membranes of C. acnes as well as possibly translocating through the cell membrane, observed by a combination of SEM and TEM, respectively. WSKK11 and WSRR11 had the ability to bind bacterial DNA. Conclusions The two novel antimicrobial peptides WSKK11 and WSRR11 are members of a new class of antimicrobial agents that could deal with acne problems. Therefore, the antimicrobial peptides may be promising novel active agents for dermatological, beauty and cosmeceutical applications.
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Jang, Yongwoo, Woori Kim, Pierre Leblanc, Chun-Hyung Kim et Kwang-Soo Kim. « Potent synthetic and endogenous ligands for the adopted orphan nuclear receptor Nurr1 ». Experimental & ; Molecular Medicine 53, no 1 (janvier 2021) : 19–29. http://dx.doi.org/10.1038/s12276-021-00555-5.

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AbstractUntil recently, Nurr1 (NR4A2) was known as an orphan nuclear receptor without a canonical ligand-binding domain, featuring instead a narrow and tight cavity for small molecular ligands to bind. In-depth characterization of its ligand-binding pocket revealed that it is highly dynamic, with its structural conformation changing more than twice on the microsecond-to-millisecond timescale. This observation suggests the possibility that certain ligands are able to squeeze into this narrow space, inducing a conformational change to create an accessible cavity. The cocrystallographic structure of Nurr1 bound to endogenous ligands such as prostaglandin E1/A1 and 5,6-dihydroxyindole contributed to clarifying the crucial roles of Nurr1 and opening new avenues for therapeutic interventions for neurodegenerative and/or inflammatory diseases related to Nurr1. This review introduces novel endogenous and synthetic Nurr1 agonists and discusses their potential effects in Nurr1-related diseases.
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Whitlow, Marc, Damain O. Arnaiz, Brad O. Buckman, David D. Davey, Brain Griedel, William J. Guilford, Sunil K. Koovakkat et al. « Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin ». Acta Crystallographica Section D Biological Crystallography 55, no 8 (1 août 1999) : 1395–404. http://dx.doi.org/10.1107/s0907444999007350.

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Factor Xa is a serine protease which activates thrombin (factor IIa) and plays a key regulatory role in the blood-coagulation cascade. Factor Xa is, therefore, an important target for the design of anti-thrombotics. Both factor Xa and thrombin share sequence and structural homology with trypsin. As part of a factor Xa inhibitor-design program, a number of factor Xa inhibitors were crystallographically studied complexed to bovine trypsin. The structures of one diaryl benzimidazole, one diaryl carbazole and three diaryloxypyridines are described. All five compounds bind to trypsin in an extended conformation, with an amidinoaryl group in the S1 pocket and a second basic/hydrophobic moiety bound in the S4 pocket. These binding modes all bear a resemblance to the reported binding mode of DX-9065a in bovine trypsin and human factor Xa.
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Gonnella, Nina C., Yu-Chin Li, Xiaolu Zhang et C. Gregory Paris. « Bioactive conformation of a potent stromelysin inhibitor determined by X-nucleus filtered and multidimensional NMR spectroscopy ». Bioorganic & ; Medicinal Chemistry 5, no 12 (décembre 1997) : 2193–201. http://dx.doi.org/10.1016/s0968-0896(97)00173-9.

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Chen, Li, Jefferson Tilley, Richard V. Trilles, Weiya Yun, David Fry, Charles Cook, Karen Rowan, Virginia Schwinge et Robert Campbell. « N-Acyl-l-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation ». Bioorganic & ; Medicinal Chemistry Letters 12, no 2 (janvier 2002) : 137–40. http://dx.doi.org/10.1016/s0960-894x(01)00711-9.

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Huang, Zhen, Yan Han, Congzhou Wang et Li Niu. « Potent and Selective Inhibition of the Open-Channel Conformation of AMPA Receptors by an RNA Aptamer ». Biochemistry 49, no 27 (13 juillet 2010) : 5790–98. http://dx.doi.org/10.1021/bi100690k.

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Ghosh, Basusree, Liberalis Debraj Boila, Susobhan Choudhury, Priya Mondal, Sayan Bhattacharjee, Samir Kumar Pal, Amitava Sengupta et Siddhartha Roy. « A Potent Conformation-Constrained Synthetic Peptide Mimic of a Homeodomain Selectively Regulates Target Genes in Cells ». ACS Chemical Biology 13, no 8 (2 juillet 2018) : 2003–9. http://dx.doi.org/10.1021/acschembio.8b00488.

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Huang, Zhen, Yan Han, Congzhou Wang et Li Niu. « Potent and Selective Inhibition of the Open-Channel Conformation of AMPA Receptors by an RNA Aptamer ». Biophysical Journal 100, no 3 (février 2011) : 269a. http://dx.doi.org/10.1016/j.bpj.2010.12.1678.

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Finnegan, C., V. Dettmer, M. Bramah-Lawani, T. Nitz, P. Bullock, I. Burimski, M. Reddick et al. « 211 Potent Orally Bioavailable HIV-1 Fusion Inhibitors Alter Env Conformation and Expose Conserved Neutralization Epitopes ». JAIDS Journal of Acquired Immune Deficiency Syndromes 51 (juin 2009) : 1. http://dx.doi.org/10.1097/01.qai.0000351167.10725.ca.

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Vanderslice, Peter, Darren G. Woodside, Amy R. Caivano, E. Radford Decker, Christy L. Munsch, Sidney J. Sherwood, Wanda S. LeJeune et al. « Potent in vivo suppression of inflammation by selectively targeting the high affinity conformation of integrin α4β1 ». Biochemical and Biophysical Research Communications 400, no 4 (octobre 2010) : 619–24. http://dx.doi.org/10.1016/j.bbrc.2010.08.114.

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White, Kris M., Paul De Jesus, Zhong Chen, Pablo Abreu, Elisa Barile, Puiying A. Mak, Paul Anderson et al. « A Potent Anti-influenza Compound Blocks Fusion through Stabilization of the Prefusion Conformation of the Hemagglutinin Protein ». ACS Infectious Diseases 1, no 2 (22 décembre 2014) : 98–109. http://dx.doi.org/10.1021/id500022h.

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Xiao, Dong, Anandan Palani, Xianhai Huang, Michael Sofolarides, Wei Zhou, Xiao Chen, Robert Aslanian et al. « Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors ». Bioorganic & ; Medicinal Chemistry Letters 23, no 11 (juin 2013) : 3262–66. http://dx.doi.org/10.1016/j.bmcl.2013.03.109.

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Hung, Tzu-Chieh, Tung-Ti Chang, Ming-Jen Fan, Cheng-Chun Lee et Calvin Yu-Chian Chen. « In SilicoInsight into Potent of Anthocyanin Regulation of FKBP52 to Prevent Alzheimer’s Disease ». Evidence-Based Complementary and Alternative Medicine 2014 (2014) : 1–20. http://dx.doi.org/10.1155/2014/450592.

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Alzheimer’s disease (AD) is caused by the hyperphosphorylation of Tau protein aggregation. FKBP52 (FK506 binding protein 52) has been found to inhibit Tau protein aggregation. This study found six different kinds of anthocyanins that have high binding potential. After analyzing the docking positions, hydrophobic interactions, and hydrogen bond interactions, several amino acids were identified that play important roles in protein and ligand interaction. The proteins’ variation is described using eigenvectors and the distance between the amino acids during a molecular dynamics simulation (MD). This study investigates the three loops based around Glu85, Tyr113, and Lys121—all of which are important in inducing FKBP52 activation. By performing a molecular dynamic simulation process between unbound proteins and the protein complex with FK506, it was found that ligand targets that docked onto the FK1 domain will decrease the distance between Glu85/Tyr113 and Glu85/Lys121. The FKBP52 structure variation may induce FKBP52 activation and inhibit Tau protein aggregation. The results indicate that anthocyanins might change the conformation of FKBP52 during binding. In addition, the purple anthocyanins, such as cyanidin-3-glucoside and malvidin-3-glucoside, might be better than FK506 in regulating FKBP52 and treating Alzheimer’s disease.
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Chen, Yan, Shasha Cai, Xue Qiao, Mali Wu, Zhilai Guo, Renping Wang, Yi-Qun Kuang, Haining Yu et Yipeng Wang. « As-CATH1–6, novel cathelicidins with potent antimicrobial and immunomodulatory properties from Alligator sinensis, play pivotal roles in host antimicrobial immune responses ». Biochemical Journal 474, no 16 (10 août 2017) : 2861–85. http://dx.doi.org/10.1042/bcj20170334.

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Crocodilians are regarded as possessing a powerful immune system. However, the composition and action of the crocodilian immune system have remained unclear until now. Cathelicidins, the principal family of host defense peptides, play pivotal roles in vertebrate immune defense against microbial invasions. However, cathelicidins from crocodilians have not been extensively studied to date. In the present study, six novel cathelicidins (As-CATH1–6) were identified and characterized from the endangered Chinese alligator (Alligator sinensis). As-CATH1–6 exhibit no sequence similarity with any of the known cathelicidins. Structure analysis indicated that As-CATH1–3 adopt a random coil secondary conformation, whereas As-CATH4–6 were predicted to mainly adopt an amphipathic α-helix conformation. Among them, As-CATH4–6 exhibited potent, broad-spectrum and rapid antimicrobial activity by inducing the disruption of cell membrane integrity. They also exhibited strong ability to prevent the formation of bacterial biofilms and eradicate preformed biofilms. Furthermore, As-CATH4–6 exhibited potent anti-inflammatory activity by inhibiting the lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and pro-inflammatory cytokines in mouse peritoneal macrophages. They directly neutralized LPS toxicity and therefore inhibited the binding of LPS to the TLR4 receptor and the subsequent activation of inflammatory response pathways. In a peritonitis mice model, As-CATH2–6 provided effective protection against bacterial infection through enhanced immune cell recruitment. In the host Chinese alligator, As-CATH1–6 are mainly expressed in immune organs and epithelial tissues. Bacterial infection significantly enhances their expression, which implies an important role in host anti-infective response. Taken together, the diversity and multiple functions of As-CATH1–6 partially reveal the powerful immune system of the Chinese alligator.
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Zuniga, Jorge E., James J. Schmidt, Timothy Fenn, James C. Burnett, Demet Araç, Rick Gussio, Robert G. Stafford, Shirin S. Badie, Sina Bavari et Axel T. Brunger. « A Potent Peptidomimetic Inhibitor of Botulinum Neurotoxin Serotype A Has a Very Different Conformation than SNAP-25 Substrate ». Structure 16, no 10 (octobre 2008) : 1588–97. http://dx.doi.org/10.1016/j.str.2008.07.011.

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Mosquna, A., F. C. Peterson, S. Y. Park, J. Lozano-Juste, B. F. Volkman et S. R. Cutler. « Potent and selective activation of abscisic acid receptors in vivo by mutational stabilization of their agonist-bound conformation ». Proceedings of the National Academy of Sciences 108, no 51 (2 décembre 2011) : 20838–43. http://dx.doi.org/10.1073/pnas.1112838108.

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Juncosa, Jose I., Martin Hansen, Lisa A. Bonner, Juan Pablo Cueva, Rebecca Maglathlin, John D. McCorvy, Danuta Marona-Lewicka, Markus A. Lill et David E. Nichols. « Extensive Rigid Analogue Design Maps the Binding Conformation of Potent N-Benzylphenethylamine 5-HT2A Serotonin Receptor Agonist Ligands ». ACS Chemical Neuroscience 4, no 1 (août 2012) : 96–109. http://dx.doi.org/10.1021/cn3000668.

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Chen, Li, Jefferson Tilley, Richard V. Trilles, Weiya Yun, David Fry, Charles Cook, Karen Rowan, Virginia Schwinge et Robert Campbell. « ChemInform Abstract : N-Acyl-L-phenylalanine Derivatives as Potent VLA-4 Antagonists that Mimic a Cyclic Peptide Conformation. » ChemInform 33, no 19 (21 mai 2010) : no. http://dx.doi.org/10.1002/chin.200219183.

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Fujii, Nobutaka, Shinya Oishi, Kenichi Hiramatsu, Takanobu Araki, Satoshi Ueda, Hirokazu Tamamura, Akira Otaka et al. « Molecular-Size Reduction of a Potent CXCR4-Chemokine Antagonist Using Orthogonal Combination of Conformation- and Sequence-Based Libraries ». Angewandte Chemie International Edition 42, no 28 (21 juillet 2003) : 3251–53. http://dx.doi.org/10.1002/anie.200351024.

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Pawlak, Danuta, Marta Oleszczuk, Jacek Wójcik, Maria Pachulska, Nga N. Chung, Peter W. Schiller et Jan Izdebski. « Highly potent side-chain to side-chain cyclized enkephalin analogues containing a carbonyl bridge : synthesis, biology and conformation ». Journal of Peptide Science 7, no 3 (mars 2001) : 128–40. http://dx.doi.org/10.1002/psc.303.

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Strokappe, Nika M., Miriam Hock, Lucy Rutten, Laura E. Mccoy, Jaap W. Back, Christophe Caillat, Matthias Haffke, Robin A. Weiss, Winfried Weissenhorn et Theo Verrips. « Super Potent Bispecific Llama VHH Antibodies Neutralize HIV via a Combination of gp41 and gp120 Epitopes ». Antibodies 8, no 2 (18 juin 2019) : 38. http://dx.doi.org/10.3390/antib8020038.

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Broad and potent neutralizing llama single domain antibodies (VHH) against HIV-1 targeting the CD4 binding site (CD4bs) have previously been isolated upon llama immunization. Here we describe the epitopes of three additional VHH groups selected from phage libraries. The 2E7 group binds to a new linear epitope in the first heptad repeat of gp41 that is only exposed in the fusion-intermediate conformation. The 1B5 group competes with co-receptor binding and the 1F10 group interacts with the crown of the gp120 V3 loop, occluded in native Env. We present biophysical and structural details on the 2E7 interaction with gp41. In order to further increase breadth and potency, we constructed bi-specific VHH. The combination of CD4bs VHH (J3/3E3) with 2E7 group VHH enhanced strain-specific neutralization with potencies up to 1400-fold higher than the mixture of the individual VHHs. Thus, these new bivalent VHH are potent new tools to develop therapeutic approaches or microbicide intervention.
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Kumar, Rajesh, Suprit Deshpande, Leigh M. Sewall, Gabriel Ozorowski, Christopher A. Cottrell, Wen-Hsin Lee, Lauren G. Holden et al. « Elicitation of potent serum neutralizing antibody responses in rabbits by immunization with an HIV-1 clade C trimeric Env derived from an Indian elite neutralizer ». PLOS Pathogens 17, no 4 (7 avril 2021) : e1008977. http://dx.doi.org/10.1371/journal.ppat.1008977.

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Evaluating the structure-function relationship of viral envelope (Env) evolution and the development of broadly cross-neutralizing antibodies (bnAbs) in natural infection can inform rational immunogen design. In the present study, we examined the magnitude and specificity of autologous neutralizing antibodies induced in rabbits by a novel HIV-1 clade C Env protein (1PGE-THIVC) vis-à-vis those developed in an elite neutralizer from whom the env sequence was obtained that was used to prepare the soluble Env protein. The novel 1PGE-THIVC Env trimer displayed a native like pre-fusion closed conformation in solution as determined by small angle X-ray scattering (SAXS) and negative stain electron microscopy (EM). This closed spike conformation of 1PGE-THIVC Env trimers was correlated with weak or undetectable binding of non-neutralizing monoclonal antibodies (mAbs) compared to neutralizing mAbs. Furthermore, 1PGE-THIVC SOSIP induced potent neutralizing antibodies in rabbits to autologous virus variants. The autologous neutralizing antibody specificity induced in rabbits by 1PGE-THIVC was mapped to the C3/V4 region (T362/P401) of viral Env. This observation agreed with electron microscopy polyclonal epitope mapping (EMPEM) of the Env trimer complexed with IgG Fab prepared from the immunized rabbit sera. Our study demonstrated neutralization of sequence matched and unmatched autologous viruses by serum antibodies induced in rabbits by 1PGE-THIVC and also highlighted a comparable specificity for the 1PGE-THIVC SOSIP trimer with that seen with polyclonal antibodies elicited in the elite neutralizer by negative-stain electron microscopy polyclonal epitope (ns-EMPEM) mapping.
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Dugar, Sundeep, John W. Clader, Tze-Ming Chan et Harry Davis. « Substituted 2-azaspiro[5.3]nonan-1-ones as potent cholesterol absorption inhibitors : defining a binding conformation for SCH 48461 ». Journal of Medicinal Chemistry 38, no 25 (décembre 1995) : 4875–77. http://dx.doi.org/10.1021/jm00025a002.

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LaPlante, Steven R., James R. Gillard, Araz Jakalian, Norman Aubry, René Coulombe, Christian Brochu, Youla S. Tsantrizos, Martin Poirier, George Kukolj et Pierre L. Beaulieu. « Importance of Ligand Bioactive Conformation in the Discovery of Potent Indole-Diamide Inhibitors of the Hepatitis C Virus NS5B ». Journal of the American Chemical Society 132, no 43 (3 novembre 2010) : 15204–12. http://dx.doi.org/10.1021/ja101358s.

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Birnbaum, George I., Miloś Budéšínsk et Ladislav Novotn. « Structure and Conformation of 5′-Chlorocyclocytidine, a Potent Inhibitor of Nucleic Acid Synthesis : X-Ray,1H and13C NMR Analyses ». Nucleosides and Nucleotides 10, no 8 (décembre 1991) : 1625–40. http://dx.doi.org/10.1080/15257779108043050.

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He, Shan, Cong Li, Ying Liu et Luhua Lai. « Discovery of Highly Potent Microsomal Prostaglandin E2 Synthase 1 Inhibitors Using the Active Conformation Structural Model and Virtual Screen ». Journal of Medicinal Chemistry 56, no 8 (5 avril 2013) : 3296–309. http://dx.doi.org/10.1021/jm301900x.

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