Large numbers of native-fitting and random-coil conformations of a small protein, pancreatic trypsin inhibitor, have been generated as self-avoiding random walks on a face-centred cubic lattice. Randomcoil conformations similar to the native X-ray conformation occur frequently enough to suggest that well-defined kinetic pathways for protein folding are not as necessary as is usually thought.

A thionocephalosporin is shown to be a much poorer substrate of representative serine beta-lactamases of class A (RTEM-2) and class C (Enterobacter cloacae P99) and a much poorer inhibitor of the Streptomyces R61 DD-peptidase than is the analogous oxo beta-lactam. These results provide kinetic evidence for the existence of a catalytic oxyanion hole in these enzymes.

Recent kinetic, binding and crystallographic studies using P-site inhibitors of mammalian adenylate bases provide new insights into the catalytic mechanism of these highly regulated enzymes. Here, Carmen Dessauer and colleagues discuss the conformational states of adenylate cyclase, the structural determinants of inhibitor binding and the potential uses of these inhibitors as pharmacological ag...

3-Methylcyclohexanone is only partially resolved by crystallisation with a chiral diol host compound (ee 40%), but when recrystallised from an equimolar mixture of the chiral diol host and a similar but achiral host we obtain complete resolution. The latter host acts as a nucleation inhibitor and the enhanced resolution is attributed to kinetic effects.

To produce an active metabolite of Chlordiazepoxide by fungal biotransformation in easy and economic way also to develop microbial models for drug metabolism studies. is metabolized the liver CYP3A4 forms major N-desmethyl chlordiazepoxide. The focus study was explore ability six distinct fungi biotransform its metabolites. Induction, Inhibition kinetic studies were conducted find out type capa...

For decades the interaction of the anticholinesterase organophosphorus compounds with acetylcholinesterase has been characterized as a straightforward phosphylation of the active site serine (Ser-203) which can be described kinetically by the inhibitory rate constant k(i). However, more recently certain kinetic complexities in the inhibition of acetylcholinesterase by organophosphates such as p...

Blood function defines bleeding and clotting risks and dictates approaches for clinical intervention. Independent of adding exogenous tissue factor (TF), human blood treated in vitro with corn trypsin inhibitor (CTI, to block Factor XIIa) will generate thrombin after an initiation time (T(i)) of 1 to 2 hours (depending on donor), while activation of platelets with the GPVI-activator convulxin r...

Biosynthesis of ent-kaurene was investigated in extracts of cell suspension cultures and seedlings of castor bean. Both cell-free extracts contain an inhibitor of kaurene synthetase. The inhibition affects mainly the cyclization of geranylgeranyl pyrophosphate to copalyl pyrophosphate (activity A) and has little or no effect on the further cyclization of copalyl pyrophosphate to ent-kaurene (ac...