A Hybrid Platform Based on a Bispecific Peptide–Antibody Complex for Targeted Cancer Therapy

Peptide‐based therapeutics have suffered from a short plasma half‐life. On the other hand, antibodies suffer from poor penetration into solid tumors owing to their large size. Herein, we present a new molecular form, namely a hybrid complex between a hapten‐labeled bispecific peptide and an anti‐hapten antibody (“HyPEP‐body”), that may be able to overcome the aforementioned limitation. The bispecific peptide containing a cotinine tag was synthesized by linking a peptide specific to fibronectin extra domain B (EDB) and a peptide able to bind and inhibit vascular endothelial growth factor (VEGF), yielding cot‐biPEP_EDB‐VEGF. Simple mixing of cot‐biPEP_EDB‐VEGF and anti‐cotinine antibody (Ab^cot) yielded the hybrid complex, HyPEP_EDB‐VEGF. HyPEP_EDB‐VEGF retained the characteristics of the included peptides, and showed improved pharmacokinetic behavior. Moreover, HyPEP_EDB‐VEGF showed tumor growth inhibition with excellent tumor accumulation and penetration. These findings suggest that the hybrid platform described here offers a solution for most peptide therapeutics that suffer from a short circulation half‐life in blood.     

Stereoselection in radical cyclization of beta-alkoxyvinyl sulfoxides: synthesis of tetrahydrofuranyl allyl carbinols

[reaction: see text] Tetrahydrofuranyl allyl carbinols may be prepared stereoselectively via radical cyclization of beta-alkoxyvinyl sulfoxides, Pummerer rearrangement, and reaction with allylstannane.     

Controllable Growth of Perovskite Films by Room‐Temperature Air Exposure for Efficient Planar Heterojunction Photovoltaic Cells

A two‐step solution processing approach has been established to grow void‐free perovskite films for low‐cost high‐performance planar heterojunction photovoltaic devices. A high‐temperature thermal annealing treatment was applied to drive the diffusion of CH₃NH₃I precursor molecules into a compact PbI₂ layer to form perovskite films. However, thermal annealing for extended periods led to degraded device performance owing to the defects generated by decomposition of perovskite into PbI₂. A controllable layer‐by‐layer spin‐coating method was used to grow “bilayer” CH₃NH₃I/PbI₂ films, and then drive the interdiffusion between PbI₂ and CH₃NH₃I layers by a simple air exposure at room temperature for making well‐oriented, highly crystalline perovskite films without thermal annealing. This high degree of crystallinity resulted in a carrier diffusion length of ca. 800 nm and a high device efficiency of 15.6 %, which is comparable to values reported for thermally annealed perovskite films.     

A color version of the Hinsberg test: 1 degrees -3 degrees amine indicator

The Hinsberg test to recognize the type of amine (1 degrees -3 degrees amines), which has been established for more than 100 years and well documented in textbooks, is not possible without conducting complicated organic reactions. We report for the first time unique chemosensors that are capable of showing selective color changes toward 1 degrees -3 degrees amines as a color version of the Hinsberg test. This simple and straightforward qualitative analysis, using the synthesized novel compounds herein, can be considered a new innovative tool for discriminating 1 degrees -3 degrees amines as an alternative to the historical Hinsberg test.     

Isotope Effects on the Crystallization Kinetics of Selectively Deuterated Poly(ε‐Caprolactone)

Deuterium labeling of semi‐crystalline polymers can dramatically affect their crystallization behaviors. However, the influence of different labeled positions in a partially deuterated polymer on its crystallization is still far from understood. Here, we synthesized a series of selectively deuterated poly(ε‐caprolactones) (PCLs) through ring‐opening polymerization of ε‐caprolactone with controlled deuteration sites, including fully protiated (D0), fully deuterated (D10), tetra deuteration at the 3‐ and 7‐ caprolactone ring positions (D4) and hexa deuteration at the 4‐, 5‐, and 6‐ caprolactone ring positions (D6). All the PCLs showed a similar lamellar structure and parameters. Differential scanning calorimetry (DSC) analysis revealed that the equilibrium melting temperature $T_m^0$, melting temperature T_m , crystallization temperature T_c , and crystallization kinetics changed systemically with the deuterium content except for D4, which indicates that the presence of ? CD₂? moieties on either side of ester group in the polymer chain combined with isotopic inhomogeneity could influence the chain packing. The nonmonotonic trend of T_m as a function of deuterium content could be attributed to the difference in a hydrogen‐bond like intermolecular interaction between different PCLs. Partially deuterated PCLs (D4 and D6) showed an Avrami index near 2. After analyzing the parameters at the same supercooling temperature ΔT_c , the existence of two crystallization regimes of PCLs were detected. © 2019 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2019 , 57, 771–779     

Optical anisotropy of aligned pentacene molecules on a rubbed polymer corresponding to the electrical anisotropy

We report on the optical anisotropy of a pentacene film on a rubbed (poly)vinylalcohol (PVA) layer related to the electrical performances of the pentacene organic field effect transistors (OFETs) depending on the direction of a current flow. The optical anisotropies of the PVA films are negligible with respect to whether or not rubbing process. In the pentacene OFET on the rubbed PVA layer, however, the optical anisotropy is observed and the anisotropy of the electrical performances directly corresponds to the optical anisotropy of the pentacene thin-film on the rubbed PVA layer.     

On extremal sort sequences

A sort sequence S_n is a sequence of all unordered pairs of indices inI _n = {1, 2, ..., n}. With a sort sequenceS_n = (s₁ ,s₂ ,...,s_{( 2ⁿ )} )S_n = (s_1 ,s_2 ,...,s_{\left( {_2^n } \right)} ), one can associate a predictive sorting algorithm A(S_n). An execution of the algorithm performs pairwise comparisons of elements in the input setX in the order defined by the sort sequence S_n except that the comparisons whose outcomes can be inferred from the results of the preceding comparisons are not performed. A sort sequence is said to be extremal if it maximizes a given objective function. First we consider the extremal sort sequences with respect to the objective function ω(S_n) — the expected number of active predictions inS _n. We study ω-extremal sort sequences in terms of their prediction vectors. Then we consider the objective function Ω(S_n) — the minimum number of active predictions in S_n over all input orderings.     

An Expedient Synthesis of β-Chloro-β-nitroolefin Derivatives

β-Chloro-β-nitroolefin derivatives 2 were prepared from the reaction of β-nitroolefins 1 with HCl / DMF / Oxone system in moderate to good yields.

     

Fundamental groups of open K3 surfaces, Enriques surfaces and Fano 3-folds

We investigate when the fundamental group of the smooth part of a K3 surface or Enriques surface with Du Val singularities, is finite. As a corollary we give an effective upper bound for the order of the fundamental group of the smooth part of a certain Fano 3-fold. This result supports Conjecture A below, while Conjecture A (or alternatively the rational-connectedness conjecture in Kollar et al. (J. Algebra Geom. 1 (1992) 429) which is still open when the dimension is at least 4) would imply that every log terminal Fano variety has a finite fundamental group.     

Generalized Obata theorem and its applications on foliations

We prove the generalized Obata theorem on foliations. Let M be a complete Riemannian manifold with a foliation F of codimension q?2 and a bundle-like metric gM. Then (M,F) is transversally isometric to (Sq(1/c),G), where Sq(1/c) is the q-sphere of radius 1/c in (q+1)-dimensional Euclidean space and G is a discrete subgroup of the orthogonal group O(q), if and only if there exists a non-constant basic function f such that for all basic normal vector fields X, where c is a positive constant and ∇ is the connection on the normal bundle. By the generalized Obata theorem, we classify such manifolds which admit transversal non-isometric conformal fields.